Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important.
One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. Its expression and function differs from, and in some ways opposes, ESTROGEN RECEPTOR BETA.
One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.
A pharmaceutical preparation containing a mixture of water-soluble, conjugated estrogens derived wholly or in part from URINE of pregnant mares or synthetically from ESTRONE and EQUILIN. It contains a sodium-salt mixture of estrone sulfate (52-62%) and equilin sulfate (22-30%) with a total of the two between 80-88%. Other concomitant conjugates include 17-alpha-dihydroequilin, 17-alpha-estradiol, and 17-beta-dihydroequilin. The potency of the preparation is expressed in terms of an equivalent quantity of sodium estrone sulfate.
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.
2- or 4-Hydroxyestrogens. Substances that are physiologically active in mammals, especially in the control of gonadotropin secretion. Physiological activity can be ascribed to either an estrogenic action or interaction with the catecholaminergic system.
The surgical removal of one or both ovaries.
A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63)
Non-steroidal compounds with estrogenic activity.
Tumors or cancer of the human BREAST.
One of the SELECTIVE ESTROGEN RECEPTOR MODULATORS with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the ENDOMETRIUM.
Steroidal compounds related to ESTRADIOL, the major mammalian female sex hormone. Estradiol congeners include important estradiol precursors in the biosynthetic pathways, metabolites, derivatives, and synthetic steroids with estrogenic activities.
An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.
Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives.
A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed)
The hollow thick-walled muscular organ in the female PELVIS. It consists of the fundus (the body) which is the site of EMBRYO IMPLANTATION and FETAL DEVELOPMENT. Beyond the isthmus at the perineal end of fundus, is CERVIX UTERI (the neck) opening into VAGINA. Beyond the isthmi at the upper abdominal end of fundus, are the FALLOPIAN TUBES.
An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.
The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life.
The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS.
A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.
Compounds that interact with PROGESTERONE RECEPTORS in target tissues to bring about the effects similar to those of PROGESTERONE. Primary actions of progestins, including natural and synthetic steroids, are on the UTERUS and the MAMMARY GLAND in preparation for and in maintenance of PREGNANCY.
PLANT EXTRACTS and compounds, primarily ISOFLAVONES, that mimic or modulate endogenous estrogens, usually by binding to ESTROGEN RECEPTORS.
Certain tumors that 1, arise in organs that are normally dependent on specific hormones and 2, are stimulated or caused to regress by manipulation of the endocrine environment.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.
Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones.
The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.
Phospholipoglycoproteins produced in the fat body of egg-laying animals such as non-mammalian VERTEBRATES; ARTHROPODS; and others. Vitellogenins are secreted into the HEMOLYMPH, and taken into the OOCYTES by receptor-mediated ENDOCYTOSIS to form the major yolk proteins, VITELLINS. Vitellogenin production is under the regulation of steroid hormones, such as ESTRADIOL and JUVENILE HORMONES in insects.
A cell line derived from cultured tumor cells.
Antineoplastic agents that are used to treat hormone-sensitive tumors. Hormone-sensitive tumors may be hormone-dependent, hormone-responsive, or both. A hormone-dependent tumor regresses on removal of the hormonal stimulus, by surgery or pharmacological block. Hormone-responsive tumors may regress when pharmacologic amounts of hormones are administered regardless of whether previous signs of hormone sensitivity were observed. The major hormone-responsive cancers include carcinomas of the breast, prostate, and endometrium; lymphomas; and certain leukemias. (From AMA Drug Evaluations Annual 1994, p2079)
An estrogen antagonist that has been used in the treatment of breast cancer.
Surgical removal or artificial destruction of gonads.
Steroid hormones produced by the GONADS. They stimulate reproductive organs, germ cell maturation, and the secondary sex characteristics in the males and the females. The major sex steroid hormones include ESTRADIOL; PROGESTERONE; and TESTOSTERONE.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
A synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.
Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.
Compounds which contain the methyl radical substituted with two benzene rings. Permitted are any substituents, but ring fusion to any of the benzene rings is not allowed.
3-Phenylchromones. Isomeric form of FLAVONOIDS in which the benzene group is attached to the 3 position of the benzopyran ring instead of the 2 position.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Nucleotide sequences, usually upstream, which are recognized by specific regulatory transcription factors, thereby causing gene response to various regulatory agents. These elements may be found in both promoter and enhancer regions.
Cytoplasmic proteins that bind estradiol, migrate to the nucleus, and regulate DNA transcription.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
Those characteristics that distinguish one SEX from the other. The primary sex characteristics are the OVARIES and TESTES and their related hormones. Secondary sex characteristics are those which are masculine or feminine but not directly related to reproduction.
Exogenous agents, synthetic and naturally occurring, which are capable of disrupting the functions of the ENDOCRINE SYSTEM including the maintenance of HOMEOSTASIS and the regulation of developmental processes. Endocrine disruptors are compounds that can mimic HORMONES, or enhance or block the binding of hormones to their receptors, or otherwise lead to activating or inhibiting the endocrine signaling pathways and hormone metabolism.
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in neoplastic tissue.
The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
The reproductive organ (GONADS) in female animals. In vertebrates, the ovary contains two functional parts: the OVARIAN FOLLICLE for the production of female germ cells (OOGENESIS); and the endocrine cells (GRANULOSA CELLS; THECA CELLS; and LUTEAL CELLS) for the production of ESTROGENS and PROGESTERONE.
In humans, one of the paired regions in the anterior portion of the THORAX. The breasts consist of the MAMMARY GLANDS, the SKIN, the MUSCLES, the ADIPOSE TISSUE, and the CONNECTIVE TISSUES.
The period of cyclic physiological and behavior changes in non-primate female mammals that exhibit ESTRUS. The estrous cycle generally consists of 4 or 5 distinct periods corresponding to the endocrine status (PROESTRUS; ESTRUS; METESTRUS; DIESTRUS; and ANESTRUS).
Therapeutic use of hormones to alleviate the effects of hormone deficiency.
Ducts that serve exclusively for the passage of eggs from the ovaries to the exterior of the body. In non-mammals, they are termed oviducts. In mammals, they are highly specialized and known as FALLOPIAN TUBES.
The period before MENOPAUSE. In premenopausal women, the climacteric transition from full sexual maturity to cessation of ovarian cycle takes place between the age of late thirty and early fifty.
An estrogenic steroid produced by HORSES. It has a total of five double bonds in the A- and B-ring. High concentration of equilenin is found in the URINE of pregnant mares.
Small containers or pellets of a solid drug implanted in the body to achieve sustained release of the drug.
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
DNA sequences which are recognized (directly or indirectly) and bound by a DNA-dependent RNA polymerase during the initiation of transcription. Highly conserved sequences within the promoter include the Pribnow box in bacteria and the TATA BOX in eukaryotes.
A synthetic estrogen that has been used as a hormonal antineoplastic agent.
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.
The period from onset of one menstrual bleeding (MENSTRUATION) to the next in an ovulating woman or female primate. The menstrual cycle is regulated by endocrine interactions of the HYPOTHALAMUS; the PITUITARY GLAND; the ovaries; and the genital tract. The menstrual cycle is divided by OVULATION into two phases. Based on the endocrine status of the OVARY, there is a FOLLICULAR PHASE and a LUTEAL PHASE. Based on the response in the ENDOMETRIUM, the menstrual cycle is divided into a proliferative and a secretory phase.
(6 alpha)-17-Hydroxy-6-methylpregn-4-ene-3,20-dione. A synthetic progestational hormone used in veterinary practice as an estrus regulator.
Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Experimentally induced mammary neoplasms in animals to provide a model for studying human BREAST NEOPLASMS.
A cell surface protein-tyrosine kinase receptor that is overexpressed in a variety of ADENOCARCINOMAS. It has extensive homology to and heterodimerizes with the EGF RECEPTOR, the ERBB-3 RECEPTOR, and the ERBB-4 RECEPTOR. Activation of the erbB-2 receptor occurs through heterodimer formation with a ligand-bound erbB receptor family member.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
Material prepared from plants.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
Enzymes that catalyze the oxidation of estradiol at the 17-hydroxyl group in the presence of NAD+ or NADP+ to yield estrone and NADH or NADPH. The 17-hydroxyl group can be in the alpha- or beta-configuration. EC 1.1.1.62
An estrogen responsive cell line derived from a patient with metastatic human breast ADENOCARCINOMA (at the Michigan Cancer Foundation.)
Elements of limited time intervals, contributing to particular results or situations.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
A class of enzymes that catalyzes the oxidation of 17-hydroxysteroids to 17-ketosteroids. EC 1.1.-.
The measurement of an organ in volume, mass, or heaviness.
A lactogenic hormone secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). It is a polypeptide of approximately 23 kD. Besides its major action on lactation, in some species prolactin exerts effects on reproduction, maternal behavior, fat metabolism, immunomodulation and osmoregulation. Prolactin receptors are present in the mammary gland, hypothalamus, liver, ovary, testis, and prostate.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
MAMMARY GLANDS in the non-human MAMMALS.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Steroidal compounds related to PROGESTERONE, the major mammalian progestational hormone. Progesterone congeners include important progesterone precursors in the biosynthetic pathways, metabolites, derivatives, and synthetic steroids with progestational activities.
An isoflavonoid derived from soy products. It inhibits PROTEIN-TYROSINE KINASE and topoisomerase-II (DNA TOPOISOMERASES, TYPE II); activity and is used as an antineoplastic and antitumor agent. Experimentally, it has been shown to induce G2 PHASE arrest in human and murine cell lines and inhibits PROTEIN-TYROSINE KINASE.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
The surgical removal of one or both testicles.
A pharmaceutical preparation containing a mixture of esterified estrogens derived from estrogen sulfates, principally from ESTRONE sulfate. Esterified estrogen content should be 75-85% of the estrone sulfate and 6-15% of the EQUILIN sulfate.
A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Luteinizing hormone regulates steroid production by the interstitial cells of the TESTIS and the OVARY. The preovulatory LUTEINIZING HORMONE surge in females induces OVULATION, and subsequent LUTEINIZATION of the follicle. LUTEINIZING HORMONE consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH and FSH), but the beta subunit is unique and confers its biological specificity.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
A nuclear receptor coactivator with specificity for ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and THYROID HORMONE RECEPTORS. It contains a histone acetyltransferase activity that may play a role in the transcriptional activation of chromatin regions.
Enzymes which transfer sulfate groups to various acceptor molecules. They are involved in posttranslational sulfation of proteins and sulfate conjugation of exogenous chemicals and bile acids. EC 2.8.2.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST.
A daidzein derivative occurring naturally in forage crops which has some estrogenic activity.
The simultaneous or sequential binding of multiple cell surface receptors to different ligands resulting in coordinated stimulation or suppression of signal transduction.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
An estrogenic steroid produced by HORSES. It has a total of four double bonds in the A- and B-ring. High concentration of euilin is found in the URINE of pregnant mares.
A nuclear receptor coactivator with specificity for ESTROGEN RECEPTORS and PROGESTERONE RECEPTORS. It contains a histone acetyltransferase activity that may play a role in CHROMATIN REMODELING during the process of nuclear receptor-induced transcription. The coactivator has been found at elevated levels in certain HORMONE-DEPENDENT NEOPLASMS such as those found in BREAST CANCER.
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
Development of female secondary SEX CHARACTERISTICS in the MALE. It is due to the effects of estrogenic metabolites of precursors from endogenous or exogenous sources, such as ADRENAL GLANDS or therapeutic drugs.
A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.
Molecular products metabolized and secreted by neoplastic tissue and characterized biochemically in cells or body fluids. They are indicators of tumor stage and grade as well as useful for monitoring responses to treatment and predicting recurrence. Many chemical groups are represented including hormones, antigens, amino and nucleic acids, enzymes, polyamines, and specific cell membrane proteins and lipids.
A synthetic progestational hormone with no androgenic or estrogenic properties. Unlike many other progestational compounds, dydrogesterone produces no increase in temperature and does not inhibit OVULATION.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
An arylsulfatase with high specificity towards sulfated steroids. Defects in this enzyme are the cause of ICHTHYOSIS, X-LINKED.
A small, unpaired gland situated in the SELLA TURCICA. It is connected to the HYPOTHALAMUS by a short stalk which is called the INFUNDIBULUM.
Enzyme that catalyzes the movement of a methyl group from S-adenosylmethionone to a catechol or a catecholamine.
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
A synthetic progestin which is useful for the study of progestin distribution and progestin tissue receptors, as it is not bound by transcortin and binds to progesterone receptors with a higher association constant than progesterone.
A transcription factor that partners with ligand bound GLUCOCORTICOID RECEPTORS and ESTROGEN RECEPTORS to stimulate GENETIC TRANSCRIPTION. It plays an important role in FERTILITY as well as in METABOLISM of LIPIDS.
The determination of the pattern of genes expressed at the level of GENETIC TRANSCRIPTION, under specific circumstances or in a specific cell.
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
Region of hypothalamus between the ANTERIOR COMMISSURE and OPTIC CHIASM.
A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Follicle-stimulating hormone stimulates GAMETOGENESIS and the supporting cells such as the ovarian GRANULOSA CELLS, the testicular SERTOLI CELLS, and LEYDIG CELLS. FSH consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH, and FSH), but the beta subunit is unique and confers its biological specificity.
An amorphous form of carbon prepared from the incomplete combustion of animal or vegetable matter, e.g., wood. The activated form of charcoal is used in the treatment of poisoning. (Grant & Hackh's Chemical Dictionary, 5th ed)
Tumors or cancer of the UTERUS.
Chemical substances having a specific regulatory effect on the activity of a certain organ or organs. The term was originally applied to substances secreted by various ENDOCRINE GLANDS and transported in the bloodstream to the target organs. It is sometimes extended to include those substances that are not produced by the endocrine glands but that have similar effects.
An aspect of personal behavior or lifestyle, environmental exposure, or inborn or inherited characteristic, which, on the basis of epidemiologic evidence, is known to be associated with a health-related condition considered important to prevent.
A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A specialized CONNECTIVE TISSUE that is the main constituent of the SKELETON. The principle cellular component of bone is comprised of OSTEOBLASTS; OSTEOCYTES; and OSTEOCLASTS, while FIBRILLAR COLLAGENS and hydroxyapatite crystals form the BONE MATRIX.
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.
The genital canal in the female, extending from the UTERUS to the VULVA. (Stedman, 25th ed)
The amount of mineral per square centimeter of BONE. This is the definition used in clinical practice. Actual bone density would be expressed in grams per milliliter. It is most frequently measured by X-RAY ABSORPTIOMETRY or TOMOGRAPHY, X RAY COMPUTED. Bone density is an important predictor for OSTEOPOROSIS.
Ventral part of the DIENCEPHALON extending from the region of the OPTIC CHIASM to the caudal border of the MAMMILLARY BODIES and forming the inferior and lateral walls of the THIRD VENTRICLE.
The period in the ESTROUS CYCLE associated with maximum sexual receptivity and fertility in non-primate female mammals.
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.
A glycoprotein migrating as a beta-globulin. Its molecular weight, 52,000 or 95,000-115,000, indicates that it exists as a dimer. The protein binds testosterone, dihydrotestosterone, and estradiol in the plasma. Sex hormone-binding protein has the same amino acid sequence as ANDROGEN-BINDING PROTEIN. They differ by their sites of synthesis and post-translational oligosaccharide modifications.
Studies which start with the identification of persons with a disease of interest and a control (comparison, referent) group without the disease. The relationship of an attribute to the disease is examined by comparing diseased and non-diseased persons with regard to the frequency or levels of the attribute in each group.
Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure.
The male gonad containing two functional parts: the SEMINIFEROUS TUBULES for the production and transport of male germ cells (SPERMATOGENESIS) and the interstitial compartment containing LEYDIG CELLS that produce ANDROGENS.
A prediction of the probable outcome of a disease based on a individual's condition and the usual course of the disease as seen in similar situations.
The application of suitable drug dosage forms to the skin for either local or systemic effects.
Genes whose expression is easily detectable and therefore used to study promoter activity at many positions in a target genome. In recombinant DNA technology, these genes may be attached to a promoter region of interest.
Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.
Achievement of full sexual capacity in animals and in humans.
Cells that line the inner and outer surfaces of the body by forming cellular layers (EPITHELIUM) or masses. Epithelial cells lining the SKIN; the MOUTH; the NOSE; and the ANAL CANAL derive from ectoderm; those lining the RESPIRATORY SYSTEM and the DIGESTIVE SYSTEM derive from endoderm; others (CARDIOVASCULAR SYSTEM and LYMPHATIC SYSTEM) derive from mesoderm. Epithelial cells can be classified mainly by cell shape and function into squamous, glandular and transitional epithelial cells.
Resistance or diminished response of a neoplasm to an antineoplastic agent in humans, animals, or cell or tissue cultures.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
Oral contraceptives which owe their effectiveness to hormonal preparations.
The smooth muscle coat of the uterus, which forms the main mass of the organ.
The rate dynamics in chemical or physical systems.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.

The effects of estrogens and antiestrogens on hormone-responsive human breast cancer in long-term tissue culture. (1/8047)

We have established or characterized six lines of human breast cancer maintained in long-term tissue culture for at least 1 year and have examined these lines for estrogen responsiveness. One of these cell lines, MCF-7, shows marked stimulation of macromolecular synthesis and cell division with physiological concentrations of estradiol. Antiestrogens are strongly inhibitory, and at concentrations greater than 3 X 10(-7) M they kill cells. Antiestrogen effects are prevented by simultaneous treatment with estradiol or reversed by addition of estradiol to cells incubated in antiestrogen. Responsive cell lines contain high-affinity specific estradiol receptors. Antiestrogens compete with estradiol for these receptors but have a lower apparent affinity for the receptor than estrogens. Stimulation of cells by estrogens is biphasic, with inhibition and cell death at concentrations of 17beta-estradiol or diethylstilbestrol exceeding 10(-7) M. Killing by high concentrations of estrogen is probably a nonspecific effect in that we observe this response with 17alpha-estradiol at equivalent concentrations and in the otherwise unresponsive cells that contain no estrogen receptor sites.  (+info)

The effects of androgens and antiandrogens on hormone-responsive human breast cancer in long-term tissue culture. (2/8047)

We have examined five human breast cancer cell lines in continuous tissue culture for androgen responsiveness. One of these cell lines shows a 2- to 4-fold stimulation of thymidine incorporation into DNA, apparent as early as 10 hr following androgen addition to cells incubated in serum-free medium. This stimulation is accompanied by an acceleration in cell replication. Antiandrogens [cyproterone acetate (6-chloro-17alpha-acetate-1,2alpha-methylene-4,6-pregnadiene-3,20-dione) and R2956 (17beta-hydroxy-2,2,17alpha-trimethoxyestra-4,9,11-triene-1-one)] inhibit both protein and DNA synthesis below control levels and block androgen-mediated stimulation. Prolonged incubation (greater than 72 hr) in antiandrogen is lethal. The MCF- cell line contains high-affinity receptors for androgenic steroids demonstrable by sucrose density gradients and competitive protein binding analysis. By cross-competition studies, androgen receptors are distinguishable from estrogen receptors also found in this cell line. Concentrations of steroid that saturate androgen receptor sites in vitro are about 1000 times lower than concentrations that maximally stimulate the cells. Changes in quantity and affinity of androgen binding to intact cells at 37 degrees as compared with usual binding techniques using cytosol preparation at 0 degrees do not explain this difference between dissociation of binding and effect. However, this difference can be explained by conversion of [3H]-5alpha-dihydrotestosterone to 5alpha-androstanediol and more polar metabolites at 37 degrees. An examination of incubation media, cytoplasmic extracts and crude nuclear pellets reveals probable conversion of [3H]testosterone to [3H]-5alpha-dihydrotestosterone. Our data provide compelling evidence that some human breast cancer, at least in vitro, may be androgen dependent.  (+info)

Mrj encodes a DnaJ-related co-chaperone that is essential for murine placental development. (3/8047)

We have identified a novel gene in a gene trap screen that encodes a protein related to the DnaJ co-chaperone in E. coli. The gene, named Mrj (mammalian relative of DnaJ) was expressed throughout development in both the embryo and placenta. Within the placenta, expression was particularly high in trophoblast giant cells but moderate levels were also observed in trophoblast cells of the chorion at embryonic day 8.5, and later in the labyrinth which arises from the attachment of the chorion to the allantois (a process called chorioallantoic fusion). Insertion of the ROSAbetageo gene trap vector into the Mrj gene created a null allele. Homozygous Mrj mutants died at mid-gestation due to a failure of chorioallantoic fusion at embryonic day 8.5, which precluded formation of the mature placenta. At embryonic day 8.5, the chorion in mutants was morphologically normal and expressed the cell adhesion molecule beta4 integrin that is known to be required for chorioallantoic fusion. However, expression of the chorionic trophoblast-specific transcription factor genes Err2 and Gcm1 was significantly reduced. The mutants showed no abnormal phenotypes in other trophoblast cell types or in the embryo proper. This study indicates a previously unsuspected role for chaperone proteins in placental development and represents the first genetic analysis of DnaJ-related protein function in higher eukaryotes. Based on a survey of EST databases representing different mouse tissues and embryonic stages, there are 40 or more DnaJ-related genes in mammals. In addition to Mrj, at least two of these genes are also expressed in the developing mouse placenta. The specificity of the developmental defect in Mrj mutants suggests that each of these genes may have unique tissue and cellular activities.  (+info)

Isolation and purification of rat mammary tumor peroxidase. (4/8047)

7,12-Dimethylbenz(a)anthracene-induced rat mammary tumors often contain high levels of the enzyme perioxidase, a putative marker of estrogen dependence. This enzyme can be effectively extracted with 0.5 M CaCl2, giving rise to a soluble peroxidase with a molecular weight of about 50,000 as determined by gel filtration. This is the same size as the estrogen-induced peroxidase of rat uterus but smaller than other mammalian peroxidases. Further purification of the rat mammary tumor peroxidase by concanavalin A-Sepharose chromatography and hydrophobic interaction chromatography on phenyl Sepharose provides a 640-fold purification of the enzyme.  (+info)

Dominant activity of activation function 1 (AF-1) and differential stoichiometric requirements for AF-1 and -2 in the estrogen receptor alpha-beta heterodimeric complex. (5/8047)

Estrogenic responses are now known to be mediated by two forms of estrogen receptors (ER), ERalpha and ERbeta, that can function as homodimers or heterodimers. As homodimers the two have been recently shown to exhibit distinct transcriptional responses to estradiol (E2), antiestrogens, and coactivators, suggesting that the ER complexes are not functionally equivalent. However, because the three possible configurations of ER complexes all recognize the same estrogen response element, it has not been possible to evaluate the transcriptional properties of the ER heterodimer complex by transfection assays. Using ER subunits with modified DNA recognition specificity, we were able to measure the transcriptional properties of ERalpha-ERbeta heterodimers in transfected cells without interference from the two ER homodimer complexes. We first demonstrated that the individual activation function 1 (AF-1) domains act in a dominant manner within the ERalpha-ERbeta heterodimer: the mixed agonist-antagonist 4-hydroxytamoxifen acts as an agonist in a promoter- and cell context-dependent manner via the ERalpha AF-1, while activation of the complex by the mitogen-activated protein kinase (MAPK) pathway requires only the ERalpha- or ERbeta-responsive MAPK site. Using ligand-binding and AF-2-defective mutants, we further demonstrated that while the ERalpha-ERbeta heterodimer can be activated when only one E2-binding competent partner is present per dimer, two functional AF-2 domains are required for transcriptional activity. Taken together, the results of this study of a retinoid X receptor-independent heterodimer complex, the first such study, provide evidence of different stoichiometric requirements for AF-1 and -2 activity and demonstrate that AF-1 receptor-specific properties are maintained within the ERalpha-ERbeta heterodimer.  (+info)

Estrogen-dependent and independent activation of the P1 promoter of the p53 gene in transiently transfected breast cancer cells. (6/8047)

Loss of p53 function by mutational inactivation is the most common marker of the cancerous phenotype. Previous studies from our laboratory have demonstrated 17 beta estradiol (E2) induction of p53 protein expression in breast cancer cells. Although direct effects of E2 on the expression of p53 gene are not known, the steroid is a potent regulator of c-Myc transcription. In the present studies, we have examined the ability of E2 and antiestrogens to regulate the P1 promoter of the p53 gene which contains a c-Myc responsive element. Estrogen receptor (ER)-positive T47D and MCF-7 cells were transiently transfected with the P1CAT reporter plasmid and levels of CAT activity in response to serum, E2 and antiestrogens were monitored. Factors in serum were noted to be the dominant inducers of chloramphenicol acetyltransferase (CAT) expression in MCF-7 cells. The levels of CAT were drastically reduced when cells were maintained in serum free medium (SFM). However, a subtle ER-mediated induction of CAT expression was detectable when MCF-7 cells, cultured in SFM, were treated with E2. In serum-stimulated T47D cells, the CAT expression was minimal. The full ER antagonist, ICI 182 780 (ICI) had no effect. Treatment with E2 or 4-hydroxy tamoxifen (OHT) resulted in P1CAT induction; OHT was more effective than E2. Consistent with c-Myc regulation of the P1 promoter, E2 stimulated endogenous c-Myc in both cell lines. Two forms of c-Myc were expressed independent of E2 stimuli. The expression of a third more rapidly migrating form was E2-dependent and ER-mediated since it was blocked by the full ER antagonist, ICI, but not by the ER agonist/antagonist OHT. These data demonstrate both ER-mediated and ER-independent regulation of c-Myc and the P1 promoter of the p53 gene, and show differential effects of the two classes of antiestrogens in their ability to induce the P1 promoter of the p53 gene in breast cancer cells.  (+info)

Daidzein and genistein glucuronides in vitro are weakly estrogenic and activate human natural killer cells at nutritionally relevant concentrations. (7/8047)

Daidzein and genistein glucuronides (DG and GG), major isoflavone metabolites, may be partly responsible for biological effects of isoflavones, such as estrogen receptor binding and natural killer cell (NK) activation or inhibition. DG and GG were synthesized using 3-methylcholanthrene-induced rat liver microsomes. The Km and Vmax for daidzein and genistein were 9.0 and 7.7 micromol/L, and 0.7 and 1.6 micromol/(mg protein. min), respectively. The absence of ultraviolet absorbance maxima shifts in the presence of sodium acetate confirmed that the synthesized products were 7-O-glucuronides. DG and GG were further purified by a Sephadex LH-20 column. DG and GG competed with the binding of 17beta-(3H) estradiol to estrogen receptors of B6D2F1 mouse uterine cytosol. The concentrations required for 50% displacement of 17beta-(3H) estradiol (CB50) were: 17beta-estradiol, 1.34 nmol/L; diethylstilbestrol, 1.46 nmol/L; daidzein, 1.6 micromol/L; DG, 14.7 micromol/L; genistein, 0.154 micromol/L; GG, 7.27 micromol/L. In human peripheral blood NK cells, genistein at <0.5 micromol/L and DG and GG at 0.1-10 micromol/L enhanced NK cell-mediated K562 cancer cell killing significantly (P < 0.05). At > 0.5 micromol/L, genistein inhibited NK cytotoxicity significantly (P < 0.05). The glucuronides only inhibited NK cytotoxicity at 50 micromol/L. Isoflavones, and especially the isoflavone glucuronides, enhanced activation of NK cells by interleukin-2 (IL-2), additively. At physiological concentrations, DG and GG were weakly estrogenic, and they activated human NK cells in nutritionally relevant concentrations in vitro, probably at a site different from IL-2 action.  (+info)

Cloning, sequencing, and localization of bovine estrogen receptor-beta within the ovarian follicle. (8/8047)

The potential role of estrogen receptor-beta (ERbeta) in normal ovarian folliculogenesis and in reproductive disorders such as ovarian follicular cysts has not been well defined. Therefore, we were interested in cloning, sequencing, and localizing ERbeta mRNA and protein within the bovine ovary. Bovine ERbeta (bERbeta) was amplified by reverse transcription-polymerase chain reaction (RT-PCR), then cloned and sequenced. Results showed that the open reading frame of bERbeta cDNA spanned 1584 nucleotides encoding a protein of 527 amino acids. The N-terminal region of bERbeta was found to be 80% homologous to human and mouse ERbeta and 79% homologous to rat ERbeta. Bovine ERbeta DNA-binding domain was 100% homologous to human, mouse, and rat ERbeta sequences. The C-terminal/ligand-binding domain of bERbeta was 89% homologous to human, 86% homologous to mouse, and 88% homologous to rat ERbeta. Human and bovine ERbeta amino acid sequences are similar in that their coding region extended farther 5' than initially reported for the published rat ERbeta sequence. Using in situ hybridization and immunohistochemistry, ERbeta mRNA and protein, respectively, were demonstrated to be present in granulosa cells of antral follicles in various stages of follicular growth. These findings suggest a role for bERbeta in ovarian follicular growth and maturation.  (+info)

Background: Estrogen receptor (ER)-negative breast tumors and progesterone receptor (PR)-negative breast tumors occur more commonly in women of African ancestry. Recent research indicates that the effects of reproductive factors may differ by hormone receptor status. We assessed the relation of parity and lactation to incidence of ER−/PR− and ER+/PR+ breast cancer in a cohort of African American women.. Methods: From 1995-2009, 457 incident cases of ER+/PR+ and 318 cases of ER−/PR− breast cancer were confirmed by review of pathology data among 59,000 African American women followed in the Black Womens Health Study through biennial questionnaires. HRs and two-sided 95% CIs for the incidence of breast cancer subtypes were derived from proportional hazards regression models that controlled for age, reproductive variables, and breast cancer risk factors.. Results: Higher parity was associated with an increased risk of ER−/PR− breast cancer (HR = 1.48, 95% CI: 0.98-1.84 for 3+ versus 0 ...
The ligand binding domain of estrogen receptor and estrogen receptor-related receptors. The ligand binding domain of estrogen receptor (ER) and estrogen receptor-related receptors (ERRs): Estrogen receptors are a group of receptors which are activated by the hormone estrogen. Estrogen regulates many physiological processes including reproduction, bone integrity, cardiovascular health, and behavior. The main mechanism of action of the estrogen receptor is as a transcription factor by binding to the estrogen response element of target genes upon activation by estrogen and then recruiting coactivator proteins which are responsible for the transcription of target genes. Additionally some ERs may associate with other membrane proteins and can be rapidly activated by exposure of cells to estrogen. ERRs are closely related to the estrogen receptor (ER) family. But, it lacks the ability to bind estrogen. ERRs can interfere with the classic ER-mediated estrogen signaling pathway, positively or ...
In breast cancer, the presence of the ERα is considered as a good indicator of disease-free survival and prognosis since patients with ERα-positive tumors are candidates for hormonal therapy [3, 4, 6]. In contrast, tumors lacking this receptor have the poorest clinical prognosis [36]. In this study we demonstrated the ability of calcitriol to induce the expression of ERα in both primary and established ERα-negative breast cancer cell lines. This effect was mediated by a VDR-dependent mechanism. In addition, our results demonstrated a fully active calcitriol-induced ER by its ability to increase PRL gene expression. Interestingly, pretreatment of ER-negative breast tumor-derived cells with calcitriol and the further incubation with this secosteroid in combination with tamoxifen or ICI-182,780 resulted in a significantly lower cell growth proliferation.. It is noteworthy to mention that, to our knowledge, this study is the first to demonstrate the ability of calcitriol to induce the expression ...
Pregnancy is safe for women with estrogen receptor positive breast cancerSome people have basic questions about how pregnancy happens. Some may have questions about avoiding a pregnancy
A striking difference between ER+ and ER- disease is emerging at the level of mRNA expression. Although in ER+ disease a significant number of genes have been found that correlate with clinical outcome [5, 10, 18, 22], in ER- disease no such prognostic signatures have thus far been reported. Moreover, although in ER+ tumors subtypes of different prognostic risks, the luminal A and B subtypes, have been defined [21, 22], no such subdivisions have been noted for ER- breast cancer. It is known that the two main subtypes of ER- breast cancer (ER-/HER2+ and basals) have worse prognosis compared with the luminal A subtype, but no outcome differences between the ER-/HER2+ and basal subtypes have been observed [15, 21-23, 26].. We believe that these differences between ER+ and ER- disease are related to the different histopathologic characteristics of the tumors. The prognostic signatures derived for ER+ breast cancer are characterized by genes related to cell cycle and cell proliferation pathways, and ...
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The study is being conducted to determine whether neoadjuvant endocrine therapy with fulvestrant or the combination of anastrozole and fulvestrant, is better than anastrozole when given before surgery to shrink the cancer and stop it from growing. Anastrozole inhibits tumor growth by reducing the levels of estrogen and has been approved by the Food and Drug Administration (FDA) of the United States for use after surgery for postmenopausal women with estrogen receptor positive breast cancer. It is also considered a standard of care to give anastrozole for a few months before surgery to shrink the tumor. Fulvestrant inhibits tumor cell growth by reducing the levels of estrogen receptor in the tumor cell. It is not approved by the FDA for use in women with early stage breast cancer before or after surgery, but is approved by the FDA for patients with advanced (Stage 4) estrogen receptor positive breast cancer that has spread to other parts of the body ...
The study is being conducted to determine whether neoadjuvant endocrine therapy with fulvestrant or the combination of anastrozole and fulvestrant, is better than anastrozole when given before surgery to shrink the cancer and stop it from growing. Anastrozole inhibits tumor growth by reducing the levels of estrogen and has been approved by the Food and Drug Administration (FDA) of the United States for use after surgery for postmenopausal women with estrogen receptor positive breast cancer. It is also considered a standard of care to give anastrozole for a few months before surgery to shrink the tumor. Fulvestrant inhibits tumor cell growth by reducing the levels of estrogen receptor in the tumor cell. It is not approved by the FDA for use in women with early stage breast cancer before or after surgery, but is approved by the FDA for patients with advanced (Stage 4) estrogen receptor positive breast cancer that has spread to other parts of the body ...
Women are believed to be protected from non-alcoholic fatty liver disease (NAFLD) by estrogen, so postmenopausal women with lower estrogen levels have an increased chance of developing the disease. Their risk is even higher if they are on anti-estrogen therapy. Hepatic steatosis (fatty liver) is is an early stage of NAFLD which can lead to […]. View Post ...
TY - JOUR. T1 - Expression of estrogen receptor gene in mouse oocyte and during embryogenesis. AU - Wu, T. C J. AU - Wang, L.. AU - Wan, Yu-Jui Yvonne. PY - 1992. Y1 - 1992. N2 - Estrogen is required for oocyte maturation and embryonic development in vivo; however, the mechanism involved is not clear. Since the effect of estrogen is mediated through the estrogen receptor (ER), we examined the ontogeny and expression of the ER gene in mouse oocytes and embryos of various gestational stages using the highly sensitive reverse transcriptase- polymerase chain reaction (RT-PCR) technique. Total RNA, extracted from 40 ovulated oocytes, 2-cell embryos, morulae, and blastocysts, was reverse transcribed into cDNA. A pair of primers flanking the 453-bp region encoding the hormone-binding domain of ER was used for 30 cycles of PCR. The identity of the amplified product was confirmed by sizing and Southern blot hybridization. The results indicated that ER gene is expressed in unfertilized oocytes and ...
Estrogen receptor-negative (ER(-)) breast cancers have limited treatment options and are associated with earlier relapses. Because glucocorticoid receptor (GR) signaling initiates antiapoptotic pathways in ER(-) breast cancer cells, we hypothesized that activation of these pathways might be associated with poor prognosis in ER(-) disease. Here we report findings from a genome-wide study of GR transcriptional targets in a premalignant ER(-) cell line model of early breast cancer (MCF10A-Myc) and in primary early-stage ER(-) human tumors. Chromatin immunoprecipitation with massively parallel sequencing (ChIP-seq) coupled to time-course expression profiling led us to identify epithelial-to-mesenchymal transition (EMT) pathways as an important aspect associated with GR activation. We validated these findings by carrying out a meta-analysis of primary breast tumor gene expression from 1,378 early-stage breast cancer patients with long-term clinical follow-up, confirming that high levels of GR expression
Summary Two polymorphisms of the aromatase and estrogen receptor genes appeared to interact to influence the risk of hip fractures in women. Introduction Allelic variants of the aromatase gene have been associated with bone mineral density and vertebral fractures. Our objective was to analyze the relationship between two polymorphisms of the aromatase and estrogen receptor genes and hip ...
Estrogen receptors (ERs), including ERα and ERβ, mainly mediate the genotype effect of estrogen. ERα is highly expressed in most breast cancers. Endocrine therapy is the most effective and safety adjunctive therapy for ER positive breast cancers. RNPC1, an RNA binding protein (RBP), post-transcriptionally regulating gene expression, is emerging as a critical mechanism for gene regulation in mammalian cells. In this study, we revealed RNPC1s capability of regulating ERα expression. There was a significant correlation between RNPC1 and ERα expression in breast cancer tissues. Ectopic expression of RNPC1 could increase ERa transcript and expression in breast cancer cells, and vice versa. Consistent with this, RNPC1 was able to bind to ERα transcript to increase its stability. Furthermore, overexpression of ERα could decrease the level of RNPC1 transcript and protein. It suggested a novel mechanism by which ERα expression was regulated via stabilizing mRNA. A regulatory feedback loop ...
Analysis of lipid components of membranes in breast cancer cells was done previously and revealed significantly altered ratio of phospholipids (3), increased level of gangliosides, and components of lipid rafts (4-6) in ER(−) cells. Furthermore, increased circulating levels of gangliosides were found in breast cancer patients when compared with healthy individuals (7). Although association of few membrane and cytoskeletal proteins with the ER status were reported before, no comprehensive analysis of membrane and cytoskeletal proteins in a broad cell panel of breast cancer cells has been done thus far. Among these proteins, vimentin, EGFR, CD44, fascin, and E-cadherin were shown to be highly correlated with ER status both in breast cancer cell lines and in clinical samples (17). EGFR and vimentin were shown to coexpress in specific subset of advanced breast carcinoma distinct from both erbB2(+) and ER(+) cases (17). CD44, moesin, and fascin were also found to express at higher level in advanced ...
While ER- breast cancer risk was markedly reduced in women with a late age at menarche, there was not a clear pattern of increased risk with longer interval between menarche and FLB, as was observed for ER+ breast cancer. These findings indicate that etiologic pathways involving adolescence and preg …
Objective: Breast carcinomas positive for the estrogen receptor (ER+) but negative for the progesterone receptor (PR-) have unfavorable prognostic features and are resistant to tamoxifen therapy. The goal of this study was to highlight the significance of PR-breast carcinomas. ...
New and emerging treatments for estrogen receptor-positive breast cancer: focus on everolimus Elisavet Paplomata, Ruth O’ReganDepartment of Hematology and Medical Oncology, Winship Institute of Emory University, Atlanta, GA, USAAbstract: Management of patients with metastatic hormone receptor-positive breast cancer poses a challenge due to the inevitable development of endocrine resistance. Hormone resistance is associated with a complex interaction of the estrogen receptor with growth factors, transmembrane receptors, and intracellular growth cascades. The PI3K/Akt/mTOR pathway plays a major role in hormone resistance and proliferation of breast cancer. Preclinical and clinical data indicate that inhibitors of human epidermal growth factor receptor-2, epidermal growth factor receptor, insulin-like growth factor-1 receptor, and the mammalian target of rapamycin pathway may act synergistically with hormone therapy to circumvent endocrine resistance. Everolimus is currently approved for combination
Li, J., Gong, Y., Shen, P., Wong, S.P., Yong, E.L., Lee, L., Wise, S.D. (2009). Bioassays for estrogenic activity: Development and validation of estrogen receptor (ERα/ERβ) and breast cancer proliferation bioassays to measure serum estrogenic activity in clinical studies. Assay and Drug Development Technologies 7 (1) : 80-89. [email protected] Repository. https://doi.org/10.1089/adt. ...
Background: Drugs targeting estrogen signaling or production have become useful in preventing estrogen receptor‐positive breast cancers, but not estrogen receptor‐negative (ER‐negative) breast cancers. Our laboratory has demonstrated that rexinoids prevent ER‐negative mammary tumors in transgenic mice by 90%. However, since these agents are not 100% effective, we are investigating the mechanism by which rexinoids prevent cancer to develop more efficacious prevention strategies. We hypothesized that by identifying molecules regulated by the rexinoid LG100268, future chemopreventive agents could be developed to target these molecules alone or in combination with rexinoids to totally prevent breast cancer development. To investigate this hypothesis we utilized an Affymetrix genome array to identify biomarkers regulated by LG100268.. Methods: Cell counts were used to confirm rexinoid‐induced growth suppression in normal human mammary epithelial cells (HMECs). TUNEL analysis was conducted ...
9q31.2-rs865686 as a susceptibility locus for estrogen receptor-positive breast cancer: evidence from the breast cancer association consortium ...
Purpose: The 21-gene breast cancer assay recurrence score (RS) is widely used for assessing recurrence risk and predicting chemotherapy benefit in patients with estrogen receptor (ER) -positive breast cancer. Pathologic and clinical factors such as tumor size, grade, and patient age also provide independent prognostic utility. We developed a formal integration of these measures and evaluated its prognostic and predictive value. Patients and Methods: From the National Surgical Adjuvant Breast and Bowel (NSABP) B-14 and translational research cohort of the Arimidex, Tamoxifen Alone or in Combination (TransATAC) studies, we included patients who received hormonal monotherapy, had ER-positive tumors, and RS and traditional clinicopathologic factors assessed (647 and 1,088, respectively). Individual patient risk assessments from separate Cox models were combined using meta-analysis to form an RS-pathology-clinical (RSPC) assessment of distant recurrence risk. Risk assessments by RS and RSPC were ...
A hormone-receptor-positive (HR+) tumor is a tumor which consists of cells that express receptors for certain hormones. The term most commonly refers to estrogen receptor positive tumors (i.e. tumors that contain estrogen receptor positive cells), but can also include progesterone receptor positive tumors. Estrogen-receptor-positive tumors depend on the presence of estrogen for ongoing proliferation. ...
TY - JOUR. T1 - Estrogen response elements function as allosteric modulators of estrogen receptor conformation. AU - Wood, Jennifer R.. AU - Greene, Geoffrey L.. AU - Nardulli, Ann M.. PY - 1998/4. Y1 - 1998/4. N2 - The estrogen receptor (ER) is a ligand-dependent transcription factor that regulates the expression of estrogen-responsive genes. ER-mediated transcriptional changes are brought about by interaction of the ER with the estrogen response element (ERE). In this study, we examined the interaction of the Xenopus laevis ER DNA binding domain (DBD) and the intact ER with the X. laevis vitellogenin A2 ERE and the human pS2 ERE. Using gel mobility shift, DNase I footprinting, and methylation interference assays, we demonstrated that the DBD bound only as a dimer to the A2 ERE. However, the DBD bound as a monomer to the consensus pS2 ERE half site at lower DBD concentrations and then as a homodimer to the consensus and imperfect pS2 ERE half site at higher DBD concentrations. Antibody ...
Estrogen receptor (ER) has been shown to be involved in several cellular and metabolic pathways. In this study, we reviewed the literature for molecular and physiological roles of estrogen receptor in normal and pathological conditions. We discussed the expression of estrogen receptor in several tissues as well as the potential of using ERb agonists in treating proliferative hematological disorders. The function of estrogen is varied and may look contradicted. Estrogen has multiple roles under physiological conditions including signaling roles in cell growth, reproduction, development and differentiation. Estrogens exert their effects through two distinct estrogen receptors, ER-α and β to which E2 binds strongly. The expression of ERs depends mainly on the type of ER. Although estrogen mainly acts in reproductive system, its receptors are selectively expressed in different tissues. ER-β is highly expressed in the ovary, central nervous system, cardiovascular system, lung, male reproductive
A small number of single biomarkers has been used for several years in various aspects of managing breast cancer, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2 (HER2). Their study in new settings and/or alongside new therapies has extended their applications. The biological importance of these established markers has been reinforced over the last decade by the results from genomic classification in which the presence or absence of these markers identifies the three main groups (7): luminal (estrogen receptor positive), HER2-like (mainly estrogen receptor negative and HER2 positive), and basal-like (mainly estrogen receptor negative, progesterone receptor negative, and HER2 negative), which approximates the so-called triple-negative group of breast cancer as described by Schneider et al. in this issue (8). The development of such different molecular groups according to estrogen receptor status may be determined at least partly by the apparent ...
The role of estrogen receptor β (ERβ) in breast cancer is still under investigation. Various studies have provided evidence that ERβ behaves as a tumor suppressor in breast cancer, whereas some studies of estrogen receptor α (ERα) negative breast cancer reported a positive correlation between high ERβ expression and poor prognostic phenotypes, such as induced proliferation, invasion and metastasis. In the present immunohistochemistry study of 99 ERα/progesterone receptor (PR)-negative breast cancer samples, nuclear expression of ERβ was positively associated with membranous expression of breast cancer resistance protein (BCRP), Ki67 (proliferation marker) and tumor size. Moreover, both endogenous and exogenous ERβ upregulated BCRP expression which induced BCRP-mediated drug resistance and enhanced proliferation of ERα-/PR- breast cancer cells in the presence of 17β-estradiol, whereas these effects were reversed by additional use of tamoxifen (TAM). In addition, the regulation of BCRP ...
Estrogens play a central role in the development of breast cancer. Most breast carcinomas are detected after menopause and despite a low degree of ovarian estrogen production and low levels of serum estrogen these tumors show a high in situ level of estrogens. Enzymes modulating local steroid availability seem to play an important role in the progression of especially estrogen receptor positive breast cancer. The 17ß-hydroxysteroid dehydrogenase (17ß-HSD) enzymes are involved in the interconversion of biologically active and inactive sex steroids and are considered to play a critical role in the in situ metabolism of estrogen.. The aim of this thesis was to investigate the expression of 17ß-HSD type 1 and 2 in breast cancer and correlate this to prognosis, and to analyze if the gene encoding 17ßHSD type 1 exhibits altered gene copy number in breast cancer. We also wanted to examine if the protein levels of aromatase, 17ßHSD type 1 and 17ßHSD type 2 show association with the expression of ...
TY - JOUR. T1 - Novel estrogen receptor ligands based on an anthranylaldoxime structure. T2 - Role of the phenol-type pseudocycle in the binding process. AU - Minutolo, Filippo. AU - Antonello, Michela. AU - Bertini, Simone. AU - Ortore, Gabriella. AU - Placanica, Giorgio. AU - Rapposelli, Simona. AU - Sheng, Shubin. AU - Carlson, Kathryn E.. AU - Katzenellenbogen, Benita S. AU - Katzenellenbogen, John A.. AU - Macchia, Marco. PY - 2003/9/11. Y1 - 2003/9/11. N2 - The 3,4-diphenylsalicylaldoxime system 1 is an estrogen receptor (ER) ligand of unusual structure, having a hydrogen-bonded pseudocyclic A′-ring in place of the paradigmatic phenolic A-ring that is characteristic of most estrogens. We have investigated the role played by the pseudocycle A′ in binding to the ER by preparing 3,4-diphenylbenzaldoxime (4), a compound that completely lacks this ring but still preserves all of the other features of the original molecule 1, as well as a series of 3,4-diphenylanthranylaldoximes (5a-c) in ...
This report provides the insights of the marketed drugs for the Estrogen Receptor Positive (ER+) Breast Cancer which includes the Targeted Therapy, Hormone Therapy and Chemotherapy. In case of Estrogen Receptor Positive (ER+) Breast Cancer, Hormone therapy is the main focus of treatment after surgery and chemotherapy. Hormonal therapy is usually recommended after 5 years of surgery and can be divided into Estrogen blocking hormonal therapy and estrogen lowering hormonal therapy based on the mechanism of action of the hormonal therapy drugs. Of all the late-stage pipeline drugs, Buparlisib is expected to reach the market in the next few years ...
TY - JOUR. T1 - Synthesis and estrogen receptor affinity of a 4-hydroxytamoxifen-labeled ligand for diagnostic imaging. AU - Lashley, Matthew R.. AU - Niedzinski, Edmund J.. AU - Rogers, Jane M.. AU - Denison, Michael S.. AU - Nantz, Michael H.. PY - 2002/12/1. Y1 - 2002/12/1. N2 - A 10-step synthesis of a novel 4-hydroxytamoxifen-DTPA ligand (HOTam-DTPA) is reported. Tamoxifen and its primary metabolite 4-hydroxytamoxifen are common estrogen receptor ligands. Consequently, tamoxifen has found utility as the targeting component of various diagnostic agents for selective imaging of estrogen receptor-rich tissue, specifically breast cancer. An L-aspartic acid-derived DTPA analogue was attached to the ethyl side chain of 4-hydroxy-tamoxifen using N,N′-dimethylethylenediamine as a hydrophilic linker. A competitve estrogen receptor binding assay using [3H]-17β-estradiol was performed to determine the effect of the ethyl side chain modification on estrogen receptor affinity. The results show that ...
HypothesisSome risk factors associated with breast cancer may be more predictive of estrogen receptor (ER)− positive than ER-negative tumors.DesignSurvey of pat
Investigators from the Slone Epidemiology Center at Boston University School of Medicine (BUSM) have reported that African American women who consume more vegetables are less likely to develop estrogen receptor-negative breast cancer than women with low vegetable intake. The study results, published in the American Journal of Epidemiology, were based on data from the Black Womens Health Study (BWHS), a large follow-up study of 59,000 African American women from across the U.S. conducted by investigators at the Slone Epidemiology Center since 1995.. The investigators followed 51,928 participants in the BWHS for 12 years, during which time 1,268 cases of breast cancer developed. Among cases on which hormone receptor status was obtained, 35 percent were estrogen receptor-negative/progesterone receptor-negative (ER-/PR-) breast cancers. The incidence of ER-/PR- breast cancer was 43 percent lower among women consuming at least two vegetables per day compared with women who ate fewer than four ...
Fulvestrant is a synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines. Check for active clinical trials or closed clinical trials using this agent.
who showed paclitaxel once per week comparedwith paclitaxel once every 3 weeks increased pathologic completeresponse-a surrogate of disease-free and overall survival-inthe neoadjuvant setting in operable breast cancer, in both hormonereceptor-positiveandhormonereceptor-negative subsets. In the confirmatorytrial by Sparano et al,2 which evaluated the 5-year diseasefreeand overall survival end points and compared the two taxanesand the two taxane schedules in a 2 x 2 factorial design, paclitaxelonce per week compared with paclitaxel once every 3 weeks significantlyimproved 5-year progression-free survival in hormonereceptor-negative breast cancer, including triple-negative and humanepidermal growth factor receptor 2 (HER2) -positive subsets ofbreast cancer, and hormone receptor-positive breast cancer, whichcombines luminal-A and luminal-B subtypes of breast cancer. Thiswas seen despite the fact that patients with HER2-positive breastcancer (including luminal-B breast cancer, an HER2-positive ...
A small number of single biomarkers has been used for several years in various aspects of managing breast cancer, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2 (HER2). Their study in new settings and/or alongside new therapies has extended their applications. The biological importance of these established markers has been reinforced over the last decade by the results from genomic classification in which the presence or absence of these markers identifies the three main groups (7): luminal (estrogen receptor positive), HER2-like (mainly estrogen receptor negative and HER2 positive), and basal-like (mainly estrogen receptor negative, progesterone receptor negative, and HER2 negative), which approximates the so-called triple-negative group of breast cancer as described by Schneider et al. in this issue (8). The development of such different molecular groups according to estrogen receptor status may be determined at least partly by the apparent ...
Dr. Sharon Glynn is Lecturer Above the Bar in Pathology at NUI Galway. She graduated in 1997 with a BSc in Biotechnology (Dublin City University) and in 2003 with a PhD entitled An investigation of the role of the ErbB receptor family in chemotherapeutic drug resistance and invasion in human breast cancer (Dublin City University). After graduation Dr. Glynn served as a research officer at the National Institute for Cellular Biotechnology in Dublin City University where she studied the efficacy of new therapeutics including cholesterol lowering statins on breast cancer and melanoma proliferation and invasion. From 2005 to 2009 Dr. Glynn worked as an NCI Cancer Prevention Fellow in Bethesda Maryland, USA in the Laboratory of Human Carcinogenesis under the mentorship of Dr. Stefan Ambs, studying the role of inflammation pathways in estrogen receptor negative breast cancer progression using an approach combining molecular epidemiology and basic laboratory science. She discovered a novel role for ...
The primary objective of this study is to determine whether overall response to cetuximab combined with cisplatin is better than overall response to cis
Vega V.B., Lin C.-Y., Lai K.S., Kong S.L., Xie M., Su X., Teh H.F., Thomsen J.S., Yeo A.L., Sung W.K., Bourque G., Liu E.T. (2006). Multiplatform genome-wide identification and modeling of functional human estrogen receptor binding sites. Genome Biology 7 (9) : R82. [email protected] Repository. https://doi.org/10.1186/gb-2006-7-9- ...
Tamoxifen - used alongside traditional chemotherapy and radiotherapy - blocks the female hormone oestrogen that, in certain breast cancers, is required by the tumour to grow; it has been shown to improve cancer survival rates by up to one third.. However, about one third of patients with the appropriate type of breast cancer - known as oestrogen receptor positive breast cancer - do not respond to tamoxifen or develop resistance to the drug. Oestrogen receptor positive breast cancer is the most common form of the disease accounting for 70% of cases.. Now, a team from the University of Manchesters Paterson Institute for Cancer Research has identified a molecular flag that will help doctors predict which patients will respond best to complementary (adjuvant) hormone therapy with tamoxifen.. The identification of molecular flags to classify subgroups of breast cancer and so determine the best treatment for each patient is of increasing importance in cancer therapy, said study lead Professor ...
TY - JOUR. T1 - Proteasome-dependent degradation of the human estrogen receptor. AU - Nawaz, Zafar. AU - Lonard, David M.. AU - Dennis, Andrew P.. AU - Smith, Carolyn L.. AU - OMalley, Bert W.. PY - 1999/3/2. Y1 - 1999/3/2. N2 - In eukaryotic cells, the ubiquitin-proteasome pathway is the major mechanism for the targeted degradation of proteins with short half-lives. The covalent attachment of ubiquitin to lysine residues of targeted proteins is a signal for the recognition and rapid degradation by the proteasome, a large multi-subunit protease. In this report, we demonstrate that the human estrogen receptor (ER) protein is rapidly degraded in mammalian cells in an estradiol-dependent manner. The treatment of mammalian cells with the proteasome inhibitor MG132 inhibits activity of the proteasome and blocks ER degradation, suggesting that ER protein is turned over through the ubiquitin- proteasome pathway. In addition, we show that in vitro ER degradation depends on ubiquitin-activating E1 ...
In approximately two-thirds of cases, ER-positive breast cancer is characterized by the sustained expression of the ER-α (ESR1), making this receptor the most frequently utilized biomarker and therapeutic target for ER-positive disease.. Genetic mutations fuelling ESR1 expression in ER-positive breast cancer have been studied extensively, therefore, in this study the team aimed to look beyond genetic mutations. Utilizing epigenetics, the team observed a significant number of somatic mutations in a set of regulatory elements that have previously been demonstrated to regulate ESR1 expression in 7% of ER-positive breast cancers.. Lead author Mathieu Lupien (Princess Margaret Cancer Centre) commented: By investigating acquired mutations found outside of genes through the power of epigenetics, we have identified that functional regulatory components can be altered to impact the expression of genes to promote breast cancer development.. Lupien believes that this research highlights the importance ...
Deca-bromodiphenyl ether (BDE-209) regulates various aspects of spermatogenesis and male fertility through its effect on estrogen receptor α (ERα
GPER/GPR30 is a seven-transmembrane G protein-coupled estrogen receptor that regulates many aspects of mammalian biology and physiology. We have previously described both a GPER-selective agonist G-1 and antagonist G15 based on a tetrahydro-3H-cyclopenta[c]quinoline scaffold. The antagonist lacks an ethanone moiety that likely forms important hydrogen bonds involved in receptor activation. Computational docking studies suggested that the lack of the ethanone substituent in G15 could minimize key steric conflicts, present in G-1, that limit binding within the ER? ligand binding pocket. In this report, we identify low-affinity cross-reactivity of the GPER antagonist G15 to the classical estrogen receptor ER?. To generate an antagonist with enhanced selectivity, we therefore synthesized an isosteric G-1 derivative, G36, containing an isopropyl moiety in place of the ethanone moiety. We demonstrate that G36 shows decreased binding and activation of ER?, while maintaining its antagonist profile ...
In vertebrates, estrogens and estrogen mimicking chemicals modulate gene expression mainly through a genomic pathway mediated by the estrogen receptors (ERs). Although the existence of an ER orthologue in the mollusc genome has been known for some time, its role in estrogen signalling has yet to be deciphered. This is largely due to its constitutive (ligand-independent) activation and a limited mechanistic understanding of its regulation. To fill this knowledge gap, we cloned and characterised an ER cDNA (sgER) and the 5′-flanking region of the gene from the Sydney rock oyster Saccostrea glomerata. The sgER cDNA is predicted to encode a 477-amino acid protein that contains a DNA-binding domain (DBD) and a ligand-binding domain (LBD) typically conserved among both vertebrate and invertebrate ERs. A comparison of the sgER LBD sequence with those of other ligand-dependent ERs revealed that the sgER LBD is variable at several conserved residues known to be critical for ligand binding and receptor
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TY - JOUR. T1 - Abnormal vascular function and hypertension in mice deficient in estrogen receptor β. AU - Zhu, Yan. AU - Bian, Zhao. AU - Lu, Ping. AU - Karas, Richard H.. AU - Bao, Lin. AU - Cox, Daniel. AU - Hodgin, Jeffrey. AU - Shaul, Philip W.. AU - Thorén, Peter. AU - Smithies, Oliver. AU - Gustafsson, Jan Åke. AU - Mendelsohn, Michael E.. PY - 2002/1/18. Y1 - 2002/1/18. N2 - Blood vessels express estrogen receptors, but their role in cardiovascular physiology is not well understood. We show that vascular smooth muscle cells and blood vessels from estrogen receptor β (ERβ) - deficient mice exhibit multiple functional abnormalities. In wild-type mouse blood vessels, estrogen attenuates vasoconstriction by an ERβ-mediated increase in inducible nitric oxide synthase expression. In contrast, estrogen augments vasoconstriction in blood vessels from ERβ-deficient mice. Vascular smooth muscle cells isolated from ERβ-deficient mice show multiple abnormalities of ion channel function. ...
TY - JOUR. T1 - Estrogen receptor β protects against in vivo injury in RPE cells. AU - Elliot, Sharon J.. AU - Catanuto, Paola. AU - Espinosa-Heidmann, Diego G.. AU - Fernandez, Pedro. AU - Hernandez, Eleut. AU - Saloupis, Peter. AU - Korach, Kenneth. AU - Karl, Michael. AU - Cousins, Scott W.. N1 - Funding Information: This work was supported in part by National Institutes of Health, National Eye Institute Grant RO1 EY1447-04 (SJE, MK, and SWC). PY - 2010/1. Y1 - 2010/1. N2 - Epidemiological data suggest that estrogen deficiency in postmenopausal women may contribute to the severity of AMD. We discovered that 17β-estradiol (E2) was a crucial regulator of the severity of extracellular matrix turnover (ECM) dysregulation both in vivo and in vitro. We also found in vitro that the presence of estrogen receptor (ER)β regulates MMP-2 activity. Therefore in an attempt to delineate the role of the ER subtypes, female estrogen receptor knockout (ERKO) mice were fed a high-fat diet, and the eyes were ...
TY - JOUR. T1 - Functional synergy between the transcription factor Sp1 and the estrogen receptor. AU - Porter, W.. AU - Saville, B.. AU - Hoivik, D.. AU - Safe, S.. PY - 1997. Y1 - 1997. N2 - A GC-rich oligonucleotide containing an estrogen responsive element (ERE) half-site from the heat shock protein 27 (Hsp 27) gene promoter (-105 to -84) [i.e. GGGCGGG(N)10GGTCA; Sp1(N)10ERE] forms a complex with the Sp1 and estrogen receptor (ER) proteins. Moreover, promoter-reporter constructs containing this sequence (-108 to -84 or -108 to +23) are also estrogen-responsive. Mutation of the ERE half-site in the Hsp 27-derived oligonucleotides did not result in loss of estrogen responsiveness in transient transfection studies, suggesting that estrogen inducibility was mediated through the Sp1-DNA motif. Gel mobility shift assays using 32P- labeled wild type and ERE mutant Sp1(N)10ERE and consensus Sp1 oligonucleotides showed that Sp1 protein formed a DNA-protein complex with all three nucleotides, and the ...
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. Abstract: The estrogen receptor (ER) is a nuclear hormone receptor that regulates a variety of genes which promote both cell proliferation and cell cycle progression. In the clinical setting ER positive breast cancer accounts for approximately 2/3 of all breast cancer diagnoses. Anti-estrogen therapies, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AI), are the core treatment modalities in patients with ER positive breast cancer. Although a large proportion of patients respond positive to endocrine therapy, resistance to these drug treatments remains an impediment to durable clinical response. Selective estrogen receptor degraders (SERDs) that remove the receptor have been shown to be effective in this setting. We describe the discovery of LSZ102, a potent, orally available SERD found to inhibit ER ...
One-hundred and seventy patients with estrogen receptor positive (≥10 pmol/g protein) advanced breast cancer have been treated in a prospective randomized study either with continuous tamoxifen 30 mg × 1 daily (TAM), or with TAM 30 mg × 1 daily for 8 weeks alternating with medroxyprogesterone acetate 500 mg × 2 daily for 8 weeks (TAM/HD-MPA). The response rate was 62% in the group treated with cyclic TAM/HD-MPA versus 41% in the TAM alone group (p = 0.02). There was no significant difference in duration of remissions or survival.
Introduction- Estrogen-related receptor gamma (ERRγ) is an orphan nuclear receptor that has biological roles mainly in metabolism and it controls metabolic switching in perinatal heart. In adult heart diseases, however, the functional roles of ERRγ have not yet been elucidated.. Hypothesis- In the present study, we aimed to characterize the role of ERRγ in cardiac hypertrophy. Here we show that ERRγ provokes cardiac hypertrophy by inducing GATA4 and that its inverse agonist, GSK-5182, prevents cardiac hypertrophy.. Methods and Results- The functional roles of ERRγ in association with development of cardiac hypertrophy were examined in primarily cultured cardiomyocytes, in animal models, and in heart samples from human hypertrophic cardiomyopathy patients. ERRγ expression was increased in hearts obtained from human hypertrophic cardiomyopathy patients and in both agonist-induced cellular models and aortic banding-induced animal models of cardiac hypertrophy. Transgenic overexpression in ...
Despite progress in the management of breast cancer, the molecular underpinnings of clinically aggressive subtypes of the disease are not well-understood. Here, we show that activation of Notch developmental signaling in estrogen receptor (ER)-negative breast cancer cells results in direct transcriptional up-regulation of the apoptosis inhibitor and cell cycle regulator survivin. This response is associated with increased expression of survivin at mitosis, enhanced cell proliferation, and heightened viability at cell division. Conversely, targeting Notch signaling with a peptidyl gamma-secretase inhibitor suppressed survivin levels, induced apoptosis, abolished colony formation in soft agar, and inhibited localized and metastatic tumor growth in mice, without organ or systemic toxicity. In contrast, ER+ breast cancer cells, or various normal cell types, were insensitive to Notch stimulation. Therefore, ER- breast cancer cells become dependent on Notch-survivin signaling for their maintenance, in vivo.
Triple Negative Breasts Cancer tumor (TNBC) is a heterogeneous disease that predicated on immunohistochemistry (IHC) is estrogen receptor (ER) detrimental, progesterone receptor (PR) detrimental and individual epidermal growth aspect receptor 2 (HER2) detrimental. Triple Negative Breasts Cancer (TNBC) is normally a subtype of breasts cancer that predicated on immunohistochemistry (IHC) is normally estrogens receptor (ER) detrimental, progesterone receptor (PR) detrimental and individual epidermal growth aspect receptor 2 (HER2) detrimental [1]. TNBC is normally seen as a its exclusive molecular profile, intense nature, distinctive metastatic patterns and insufficient targeted therapies. Its estimated that from the world-wide breast cancer tumor burden, around 170,000 situations are TNBC and take into account ~10-20% of intrusive breast malignancies [1,2]. Molecular Profile and IHC Phenotype Breasts cancers are usually categorized into seven subtypes (3): luminal A (ER positive and histologic ...
The Ets-1 transcription factor is a candidate breast cancer oncogene that regulates the expression of genes involved in tumor progression and metastasis. Ets-1 signaling has also been linked to the development of a basal-like breast cancer phenotype. We recently described a nitric oxide (NO)-induced gene signature that is associated with poor disease outcome in estrogen receptor-negative (ER-) breast cancer and contains both stem cell-like and basal-like components. Thus, we examined the role of Ets-1 in NO signaling and NO-induced phenotypes in ER- human breast cancer cells. Promoter region analyses were performed on genes upregulated in inducible nitric oxide synthase (NOS2) high expressing tumors for Ets-binding sites. In vitro mechanisms were examined in human basal-like breast cancer cells lines. NO signaling effects were studied using either forced NOS2 expression or the use of a chemical NO-donor, diethlylenetriamine NONOate (DETANO). Promoter region analysis of genes that are up-regulated in
Estrogen receptor negative (ER(−)) breast cancer is aggressive, responds poorly to current treatments and has a poor prognosis. The NF-κB signaling pathway is implicated in ER(−) tumorigenesis. Aspirin (ASA) is chemopreventive against ER(+) but not for ER(−) breast cancers. Nitric oxide-releasing aspirin (NO-ASA) is a safer ASA where ASA is linked to an NO-releasing moiety through a spacer. In vitro, we investigated anti-proliferation effects of NO-ASA (para- and meta-isomers) against ER(−) breast cancer cells MDA-MB-231 and SK-BR-23, effects on NF-κB signaling, and reactive oxygen species by standard techniques. In vivo, effects of NO-ASA were evaluated in a mouse xenograft model using MDA-MB-231 cells. p-NO-ASA inhibited the growth of MDA-MB-231 and SK-BR-3 cells at 24 h, the respective IC50s were 13 ± 2 and 17 ± 2 μM; ASA had an IC50 of |3000 μM in both cell lines. The IC50s for m-NO-ASA in MDA-MB-231 and SK-BR-3 were 173 ± 15 and 185 ± 12 μM, respectively, therefore, implying p-NO
Title: GPER and ER: Estrogen Receptors with Distinct Biological Roles in Breast Cancer. VOLUME: 11 ISSUE: 4. Author(s):Edward J. Filardo. Affiliation:Rhode Island Hospital, Department of Medicine, 593 Eddy Street, Aldrich Building Rm 708, Providence, RI 02903, USA.. Keywords:Estrogen, G-protein-coupled estrogen receptor (GPER), seven transmembrane receptors, estrogen receptors (ERs), nuclear steroid hormone receptors, tamoxifen, faslodex, epidermal growth factor receptors (EGFRs), aromatase inhibitors, breast cancer. Abstract: Comparative clinical studies indicate that blockade of estrogen biosynthesis by the use of aromatase inhibitors may have benefit over estrogen receptor (ER) antagonism as a strategy for treating breast cancer. One plausible explanation for this idea is that more than one type of estrogen receptor may promote the biological effects of estrogen. Recent findings that G-protein-coupled receptor-30, (GPR30/GPER) promotes specific estrogen binding and manifests plasma ...
What is Triple Negative Breast Cancer? Triple negative breast cancer is not your normal form of breast cancer. It is often referred to as basal cell cancer because it does not express the three genes normally associated with breast cancer. These genes are estrogen receptor (ER), progesterone receptor (PR), or (HR)2.
TY - JOUR. T1 - Reliability of clinical estrogen receptor assays performed on tumor tissue biopsied from sites previously treated with radiotherapy. AU - Valenstein, Steven L.. AU - Voigt, Walter. AU - Vogel, Charles L.. AU - Thomsen, Sharon. AU - Sugarbaker, Everett V.. AU - Castro, Albert. AU - Gupta, Vicram. AU - Charyulu, Komanduri. PY - 1979/6. Y1 - 1979/6. N2 - The present retrospective analysis was done to determine whether previous radiotherapy to a biopsy site could be a source of false-negative estrogen receptor assays as suggested in earlier reports. The present study population included 56 women who had estrogen receptor assays done on tumor tissue obtained from skin, subcutaneous, or lymph node metastases. Tissue was taken from a previously irradiated area in 14 patients and from an unirradiated area in 42. Fifty-seven percent of the former and 50% of the latter patients had positive estrogen receptor assays, and quantitative levels of estrogen receptor also were comparable between ...
TY - JOUR. T1 - Triple negative breast cancer. T2 - A multi-omics network discovery strategy for candidate targets and driving pathways. AU - Karagoz, Kubra. AU - Sinha, Raghu. AU - Arga, Kazim Yalcin. PY - 2015/2/1. Y1 - 2015/2/1. N2 - Triple negative breast cancer (TNBC) represents approximately 15% of breast cancers and is characterized by lack of expression of both estrogen receptor (ER) and progesterone receptor (PR), together with absence of human epidermal growth factor 2 (HER2). TNBC has attracted considerable attention due to its aggressiveness such as large tumor size, high proliferation rate, and metastasis. The absence of clinically efficient molecular targets is of great concern in treatment of patients with TNBC. In light of the complexity of TNBC, we applied a systematic and integrative transcriptomics and interactomics approach utilizing transcriptional regulatory and protein-protein interaction networks to discover putative transcriptional control mechanisms of TNBC. To this ...
Clinical trial for Stage IB Breast Cancer | Estrogen Receptor-negative Breast Cancer | Stage II Breast Cancer | Triple Negative Breast Cancer | Progesterone Receptor-negative Breast Cancer | Stage IA Breast Cancer , MRI and Mammography Before Surgery in Patients With Stage I-II Breast Cancer
TY - JOUR. T1 - Body mass index, mammographic density, and breast cancer risk by estrogen receptor subtype. AU - Shieh, Yiwey. AU - Scott, Christopher G.. AU - Jensen, Matthew R.. AU - Norman, Aaron D.. AU - Bertrand, Kimberly A.. AU - Pankratz, V. Shane. AU - Brandt, Kathleen R. AU - Visscher, Daniel W. AU - Shepherd, John A.. AU - Tamimi, Rulla M.. AU - Vachon, Celine M. AU - Kerlikowske, Karla. PY - 2019/4/3. Y1 - 2019/4/3. N2 - Background: Obesity and elevated breast density are common risk factors for breast cancer, and their effects may vary by estrogen receptor (ER) subtype. However, their joint effects on ER subtype-specific risk are unknown. Understanding this relationship could enhance risk stratification for screening and prevention. Thus, we assessed the association between breast density and ER subtype according to body mass index (BMI) and menopausal status. Methods: We conducted a case-control study nested within two mammography screening cohorts, the Mayo Mammography Health Study ...
TY - JOUR. T1 - Repression of translation of human estrogen receptor α by G-quadruplex formation. AU - Balkwill, Graham D.. AU - Derecka, Kamila. AU - Garner, Thomas P.. AU - Hodgman, Charlie. AU - Flint, A. P F. AU - Searle, Mark S.. PY - 2009/12/8. Y1 - 2009/12/8. N2 - Tissue-specific expression of the human estrogen receptor α gene (ESR1) is achieved through multiple promoter sequences resulting in various mRNA transcripts encoding a common protein but differing in their 5′-untranslated region (5′-UTR). Many cancers are estrogen-sensitive with neoplastic growth stimulated through the estrogen receptor, a transcription factor that regulates developmental genes. We demonstrate that the human ESR1 gene is rich in potential quadruplex-forming sequences with 3 of 20 identified within exonic regions. In particular,we show using CD, UV, and NMR spectroscopy that a stable DNAG-quadruplex motif is formed within the exon C gene sequence. This motif, which PCR shows is transcribed in normal and ...
The final results are in-and they show that 500 mg of Faslodex® (fulvestrant) provides a significant advantage in overall survival compared to 250 mg of the drug in postmenopausal women with locally advanced or metastatic estrogen receptor-positive breast cancer recurring or progressing after prior endocrine therapy. The results were published online in the Journal of the National Cancer Institute.. Each year roughly 200,000 U.S. women are diagnosed with breast cancer. Many of these breast cancers will be hormone receptor-positive, meaning that they are stimulated to grow by the circulating female hormones estrogen and/or progesterone. Treatment of hormone receptor-positive breast cancer often involves hormonal therapies that suppress or block the action of estrogen.. Faslodex-a type of hormonal therapy known as an estrogen receptor antagonist-blocks the actions of estrogen. Its used for the treatment of metastatic, hormone receptor-positive breast cancer in postmenopausal women who experience ...
摘要Estrogen is well known to have a modulatory role on gastrointestinal tract, particularly through its interaction with nuclear estrogen receptors (ERs), alpha and beta (ERα/β). Recent functional studies also indicate that estrogen can activate a G-protein coupled estrogen receptor, GPR30, or GPER1. The present study was designed to identify either the presence or absence of nuclear ERs and GPR30 in the myenteric plexus of the stomach, duodenum, jejunum, ileum and colon of female and male mice. Immunofluorescence staining revealed a high expression of GPR30 in the cytoplasm but not within the nucleus of enteric neurons in female and male mice. ERβ localization was similar to GPR30, where it was expressed in cytoplasm of enteric neurons, but was absent from nuclei, opening up the possibility that ERβ and GPR30 might work together to manifest estrogenic effects. Comparatively, ERα was mainly located in the nuclei of enteric neurons. ERα, ERβ and GPR30 were also expressed in the ...
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Cheung CP, Yu S, Wong KB, Chan LW, Lai FM, Wang X, Suetsugi M, Chen S, Chan FL (Mar 2005). Expression and functional study of estrogen receptor-related receptors in human prostatic cells and tissues. The Journal of Clinical Endocrinology and Metabolism. 90 (3): 1830-44. doi:10.1210/jc.2004-1421. PMID 15598686 ...
In this follow-up study of African American women, oral contraceptive use was more strongly associated with an increased risk of ER−PR− breast cancer than of ER+PR+ breast cancer. The incidence of ER−PR− breast cancer increased significantly among recent users as the duration of use increased, with the largest increase (2.5-fold) among recent users whose duration of use was 10 or more years. However, there were some inconsistencies in that the incidence of ER−PR− cancer was also significantly increased for some shorter-duration and nonrecent categories of use. For ER+PR+ cancer, results were null for most categories of interval since last use and duration but there was a significant increase (1.66-fold) for recent users with 10 or more years of use. Results for ER+PR− tumors were null, but the numbers were small.. The present results strengthen the evidence that there is a stronger association of oral contraceptive use with ER− cancer than with ER+ cancer (32). In several ...
Triple-negative breast cancer (TNBC) is an aggressive clinical subtype of breast cancer that is characterized by the lack of estrogen receptor (ER) and progesterone receptor (PR) expression as well as human epidermal growth factor receptor 2 (HER2) overexpression. The TNBC subtype constitutes approximately 10%-20% of all breast cancers, but has no effective molecular targeted therapies. Previous meta-analysis of gene expression profiles of 587 TNBC cases from 21 studies demonstrated high expression of Wnt signaling pathway-associated genes in basal-like 2 and mesenchymal subtypes of TNBC. In this study, we investigated the potential of Wnt pathway inhibitors in effective treatment of TNBC. Activation of Wnt pathway was assessed in four TNBC cell lines (BT-549, MDA-MB-231, HCC-1143 and HCC-1937), and the ER+ cell line MCF-7 using confocal microscopy and Western blot analysis of pathway components. Effectiveness of five different Wnt pathway inhibitors (iCRT-3, iCRT-5, iCRT-14, IWP-4 and XAV-939) on cell
Experimental evidence shows cross-talk in mammary cells between estrogen, insulin-like growth factor I (IGF-I) and their respective receptors and possible synergistic effects of estrogen receptor (ER) activation and increased IGF-I signaling with regard to breast tumor development, and epidemiological evidence suggests that circulating IGF-I levels may be related more to the risk of ER-positive than ER-negative breast cancer. Using a case-control study nested within the prospective European EPIC cohort (938 breast cancer cases and 1,394 matched control subjects), we analyzed the relationships of prediagnostic serum IGF-I levels with the risk of estrogen and progesterone receptor-positive and -negative breast tumors. IGF-I levels were positively associated with the risk of ER+ breast tumors overall (pre- and postmenopausal women combined, odds ratio (OR) Q4-Q1 = 1.41 [95% confidence interval (CI) 1.01-1.98] for the highest vs. lowest quartile; OR = 1.17 [95% CI 1.04-1.33] per 1-standard deviation (SD)
Experimental evidence shows cross-talk in mammary cells between estrogen, insulin-like growth factor I (IGF-I) and their respective receptors and possible synergistic effects of estrogen receptor (ER) activation and increased IGF-I signaling with regard to breast tumor development, and epidemiological evidence suggests that circulating IGF-I levels may be related more to the risk of ER-positive than ER-negative breast cancer. Using a case-control study nested within the prospective European EPIC cohort (938 breast cancer cases and 1,394 matched control subjects), we analyzed the relationships of prediagnostic serum IGF-I levels with the risk of estrogen and progesterone receptor-positive and -negative breast tumors. IGF-I levels were positively associated with the risk of ER+ breast tumors overall (pre- and postmenopausal women combined, odds ratio (OR) Q4-Q1 = 1.41 [95% confidence interval (CI) 1.01-1.98] for the highest vs. lowest quartile; OR = 1.17 [95% CI 1.04-1.33] per 1-standard deviation (SD)
Breast cancer is one of the most common cancer deaths in female. Estrogen receptor(ER)-negative breast cancer constitutes approximately 30 % of breast cancer cases. Triple-negative is defined as a subgroup with ER, PR(progesterone receptor) and human epidermal growth factor receptor 2 (HER2) all negative. TNBC are assumed importance for its molecular characters, aggressive progress and distinct tranfer ability [1, 2]. Beneficial results of current anti-HER2 or hormonal therapy could not improve the curative effect of chemotherapy. In the absence of proper treatments, TNBC often progresses to metastatic lesions in the brain and lung in three years. Once being with metastasis, the 5-year survival rate of TNBC would be less than 30 %. Newly therapies are urgently needed to improve the prognosis for TNBC patients. Actually, TNBCs exhibit a high level of molecular heterogeneity without high-frequency driver mutations. About 60-70 % of TNBCs has mutations of p53. For PIK3CA mutations, it would be 11 ...
TY - JOUR. T1 - Estrogen receptor binding affinity and uterotrophic activity of triphenylhaloethylenes. AU - DeSombre, Eugene R.. AU - Mease, Ronnie C.. AU - Sanghavl, Jigi. AU - Singh, Tej. AU - Seevers, Robert H.. AU - Hughes, Alun. N1 - Funding Information: Acknowledgements-Wteh ank RestitutoD izon for his able supportin the animal studies,D r S. John Gatley for his analysiso f the metabolicp roductso f the diacetatesa, nd Johanna Darden for her help in preparationo f the manuscript. Supported by the NIH (CA27476, CA14599, HD15513), DOE Contract W-31-109-ENG-38a nd the Julius J. Reingold Fellowship Fund.. PY - 1988/6. Y1 - 1988/6. N2 - Radiohalogenated estrogens have considerable potential for estrogen receptor-directed imaging and therapy for cancers which contain such receptors. In an effort to evaluate the potential of the triphenyl ethylene structure for such purposes we have synthesized 3 series of 2-halosubstituted triphenylethylenes containing oxygen functions in the 4 position of both ...
[77 Pages Report] Check for Discount on Estrogen Receptor (ER Alpha or Estradiol Receptor or Nuclear Receptor Subfamily 3 Group A Member 1 or NR3A1 or ESR1) - Pipeline Review, H2 2017 report by Global Markets Direct. Estrogen Receptor (ER Alpha or Estradiol Receptor or Nuclear Receptor...
Objective To evaluate the frequency of the estrogen receptor (ER) gene PvuII and XbaI polymorphisms and their associations with bone mineral density (BMD) in a group of postmenopausal Turkish women. ...
Uncommon mutations in three genes in estrogen receptor positive breast cancer have a negative impact on disease prognosis reports a team of British and Australian researchers in |i||link https://www.nature.com/articles/s41467-018-05914-x|Nature Communications|/link|. |/i| |i||br /||/i|
Aromatase is one of the important target for drugs that interfere with production of estrogen in the treatment of estrogen receptor positive breast cancer. Therefore the discovery of novel aromatase inhibitors that can kill the growth of cancer cells selectively with minimal toxic effects on normal healthy cells is desirable. In the present study, novel 5-(4-bromophenyl)-1,3-oxazole derivatives were synthesized, characterized and screened for their biological effect. A series of novel 5-(4-bromophenyl)-1,3-oxazole derivatives OXZ-1 to 12 were docked by Auto Dock tool to evaluate their aromatase inhibition. All the derivatives were synthesized by using versatile and convenient route. Spectroscopic techniques have characterized the synthesized compounds in order to validate their structures. A total of 12 compounds were synthesized and evaluated for their in-vitro aromatase inhibitory activity and all derivatives were tested to assess their cytotoxic effect against breast cancer cell lines ...
This article reported on a rather large trial known as ATLAS that involved almost 7,000 women, from over 30 countries, with estrogen receptor positive breast cancer. They were randomized to tamoxifen for 10 years versus those who stopped after the traditional 5 year time period. The group who took tamoxifen for 10 years had less recurrence of their breast cancer even after they stopped tamoxifen at the 10 year time frame. In addition, there were fewer women who died in the group that took tamoxifen for 10 years versus those who took it for 5 years. There were slightly more cases of uterine cancer in the women who took tamoxifen for the extra 5 years. However, the number of deaths from this was much smaller than the incremental number of deaths from breast cancer.. ...
Estrogen receptor (ER) positive rates in breast cancer may be influenced by grade, stage, age and race. This study reviews the ER positive rates over a 15-year period at the University Malaya Medical Centre, Kuala Lumpur, Malaysia. Data on ER status of 3557 patients from 1994 to 2008 was analyzed. ER status was determined by immunohistochemistry with a cut-off point of 10%. ER positivity increased by about 2% for every 5-year cohort, from 54.5% in 1994-1998 to 58.4% in 2004-2008. Ethnicity and grade were significantly associated with ER positivity rates: Malay women were found to have a higher risk of ER negative tumors compared with Chinese women. Grade 1 cancers were nine times more likely to be ER positive compared with grade 3 cancers. In summary, the proportion of ER positive cancers increased with each time period, and ethnicity and grade were independent factors that influenced ER positive rates. ...
TY - JOUR. T1 - Estrogen receptor alpha signaling promotes Sle1-induced loss of tolerance and immune cell activation and is responsible for sex bias in B6.Sle1 congenic mice. AU - Yoachim, Shayla D. AU - Nuxoll, Jenny S.. AU - Bynoté, Kimberly K.. AU - Gould, Karen A. PY - 2015/6/1. Y1 - 2015/6/1. N2 - Sex bias in lupus incidence is thought to be due, in part, to the ability of estrogens to promote loss of tolerance. Previously, we showed that estrogens promote lupus via estrogen receptor α (ERα). C57BL/6 (B6) mice carrying the Sle1 lupus susceptibility locus (B6.Sle1) display loss of tolerance and develop anti-nuclear antibodies and immune cell hyperactivation. The incidence of loss of tolerance in B6.Sle1 females is greater than in males. Here, we show that a deficiency of either estrogens or ERα attenuates loss of tolerance and autoantibody development in B6.Sle1 females. Furthermore, we demonstrate that immune cell activation in B6.Sle1 mice shows sex bias and that ERα deficiency ...
Estrogen receptors (ERs) are steroid hormone receptors important in development, growth, and reproduction. The 2 well characterized ERs, alpha and beta, interact with a variety of receptor coregulators. These coregulators bind and direct the ERs to specific promoters, varying the ER target genes transcribed to modulate signaling responses. ERs play a large role in cancers of the female reproductive system, especially breast cancer. ER positive breast cancers can be treated with antiestrogen therapy, often yielding an improved prognosis. These types of treatments use selective estrogen receptor modulators to diminish side effects on other organs expressing estrogen receptors. In addition, estrogen signaling plays a role in other pathophysiological conditions such as osteoporosis and obesity. The mechanisms of estrogen receptor signaling are not entirely understood since there are many coregulators as well as a myriad of target genes ...
TY - JOUR. T1 - Prognostic Impact of HOTAIR Expression is Restricted to ER-Negative Breast Cancers. AU - Gökmen-Polar, Yesim. AU - Vladislav, I. Tudor. AU - Neelamraju, Yaseswini. AU - Janga, Sarath C.. AU - Badve, Sunil. PY - 2015. Y1 - 2015. N2 - Expression of HOX transcript antisense intergenic RNA (HOTAIR), a large intergenic noncoding RNA (lincRNA), has been described as a metastases-associated lincRNA in various cancers including breast, liver and colon cancer cancers. We sought to determine if expression of HOTAIR could be used as a surrogate for assessing nodal metastases and evaluated RNA in situ hybridization (RNA-ISH) assay in a tissue microarray constructed from 133 breast cancer patients. The prognostic value of HOTAIR was further validated in large cohorts using The Cancer Genome Atlas (TCGA) breast cancer subjects. RNA-ISH analysis was successful in 94 cases (17% cases scored 0, 32.9% scored 1, 30.8% scored 2, and 19.1% scored 3). The expression of HOTAIR did not correlate with ...
Background The aim of this retrospective study was to determine whether progesteron receptor (PgR) status have an influence on the prognosis of estrogen receptor positive (ER+)/HER2-negative breast carcinoma (BC).. Methods We retrospectively reviewed the medical files of 1680 operable BC patients (pts) diagnosed between 1996 and 2011 and 456 of whom ER,PgR and HER2 status known were included in this study. Patients were categorized into 2 groups; as group A (ER + /PgR-/HER2-negative) and group B (ER + /PgR + /HER2-negative). Twenty one percent (97 pts) of the pts were in group A.. Results Median follow up was 33.5 (0-177) months. Median age was 54 (21-90) years. Sixty-one percent (278) of the pts had node-positive BC. Sixty percent (276) of the pts were postmenopausal. Eighty percent (365) of the pts received adjuvant chemotherapy (ACT). Adjuvant hormonotherapy (AHT) was recommended to nearly all patients (mostly tamoxifen). Pts in group A had significantly higher lymph node positive disease as ...
The majority of breast cancers are also sensitive to estrogen, meaning that estrogen promotes tumor growth.. These cancers are called hormone receptor positive breast cancers.. For people with these cancers, treatments to lower estrogen levels or block estrogen production can be used to help prevent cancer recurrence after surgery, or to slow cancer growth.. According to Breast Cancer.org, alcohol can increase a womans risk of hormone-receptor-positive breast cancer.. Alcohol also enhances the effects of estrogen in driving the growth of breast cancer cells, according to 2016 research at the University of Houston.. Endometriosis is another estrogen-dependent disease.. Reducing estrogen levels and providing non-estrogen treatments have all been considered for the treatment of endometriosis.. The problem is that reducing the levels of estrogen in women can lead to infertility.. A study by the Womens Health Initiative showed that BY REDUCING HORMONES -. ( SPECIFICALLY ESTROGEN )- had significant ...
The majority of breast cancers are also sensitive to estrogen, meaning that estrogen promotes tumor growth.. These cancers are called hormone receptor positive breast cancers.. For people with these cancers, treatments to lower estrogen levels or block estrogen production can be used to help prevent cancer recurrence after surgery, or to slow cancer growth.. According to Breast Cancer.org, alcohol can increase a womans risk of hormone-receptor-positive breast cancer.. Alcohol also enhances the effects of estrogen in driving the growth of breast cancer cells, according to 2016 research at the University of Houston.. Endometriosis is another estrogen-dependent disease.. Reducing estrogen levels and providing non-estrogen treatments have all been considered for the treatment of endometriosis.. The problem is that reducing the levels of estrogen in women can lead to infertility.. A study by the Womens Health Initiative showed that BY REDUCING HORMONES -. ( SPECIFICALLY ESTROGEN )- had significant ...
From: NAME: Les Davies FUNC: Therapeutic Goods Admin TEL: (06)289 7182 - MDP 88 ,DAVIES LES at [email protected], To: mx%bioforum at [email protected] at [email protected] Message-id: D752IOD2V16Y From: NAME: Les Davies FUNC: Therapeutic Goods Admin TEL: (06)289 7182 - MDP 88 ,DAVIES LES at [email protected], Subject: (1) Estrogen receptor assays & (2) the nervous system Date: 04-Nov-1996 Posted-date: 04-Nov-1996 Precedence: 1 To: mx5biosci-request at [email protected] at [email protected] (1) Estrogen receptor assays Noted a reply to Raymond Pierre (from JS Amenta?) about receptor binding assays for estrogen receptors - the comment that the point is to inhibit non-specific binding and not affect the specific receptor binding is not really correct - non-specific binding is not inhibitable. In receptor binding assays, an excess of a known receptor binding compound is added (to a separate set of assay tubes from the control binding tubes) to make sure that specific receptors are fully saturated and then no tritiated label ...
The healthy breast is a tissue composed of centrally located milk producing glands connected to the nipple by ducts, surrounded by fat tissue and connective tissue. The growth of the breast is primarily mediated by the estrogens, while the androgens mediate tissue homeostasis and protect against growth signals. In breast cancer, the cells of the glands or ducts undergo malignant transformation, and start proliferating in an uncontrollable fashion. Breast cancer is the most common malignancy in women, and it is estimated that 10% of all women will be diagnosed with breast cancer during their life-time. The primary classification of breast cancer is based mainly on the expression of the estrogen receptor, and 70-80% of breast cancers are estrogen receptor positive, and are classified as luminal. The remaining breast cancers are classified into HER2 positive or triple negative breast cancer. Out of all breast cancers, ~80% are androgen receptor positive. This varies in different subtypes, however, ...
TY - JOUR. T1 - Alfa and beta estrogen receptors and the biliary tree. AU - Alvaro, Domenico. AU - Alpini, G.. AU - Onori, P.. AU - Franchitto, A.. AU - Glaser, S. S.. AU - Le Sage, G.. AU - Folli, F.. AU - Attili, A. F.. AU - Gaudio, E.. N1 - Funding Information: Supported by the grant MURST 2000 (40% funds) # MM06215421/2 and by an NIH grant DK58411 and by VA Merit Award to Dr. G. Alpini.. PY - 2002/7/31. Y1 - 2002/7/31. N2 - This manuscript summarizes recent data showing that estrogens and their receptors play an important role in modulating cholangiocyte proliferation. We have recently demonstrated that rat cholangiocytes express both estrogen receptors (ER)-α and -β subtypes, while hepatocytes only express ER-α. ER and especially the ER-β subtype, are overexpressed in cholangiocytes proliferating after bile duct ligation (BDL) in the rat, in association with enlarged bile duct mass and with enhanced estradiol serum levels. Cholangiocyte proliferation, during BDL, is impaired by estrogen ...
TY - JOUR. T1 - A gene expression signature from human breast cancer cells with acquired hormone independence identifies MYC as a mediator of antiestrogen resistance. AU - Miller, Todd W.. AU - Balko, Justin M.. AU - Ghazoui, Zara. AU - Dunbier, Anita. AU - Anderson, Helen. AU - Dowsett, Mitch. AU - González-Angulo, Ana M.. AU - Mills, Gordon B.. AU - Miller, William R.. AU - Wu, Huiyun. AU - Shyr, Yu. AU - Arteaga, Carlos L.. PY - 2011/4/1. Y1 - 2011/4/1. N2 - Purpose: Although most patients with estrogen receptor α (ER)-positive breast cancer initially respond to endocrine therapy, many ultimately develop resistance to antiestrogens. However, mechanisms of antiestrogen resistance and biomarkers predictive of such resistance are underdeveloped. Experimental Design: We adapted four ER+ human breast cancer cell lines to grow in an estrogen-depleted medium. A gene signature of estrogen independence was developed by comparing expression profiles of long-term estrogen-deprived (LTED) cells to ...
Recently in the pig hypothalamus a vasopressin- and oxytocin-containing nucleus was identified which, like the supraoptic nucleus, becomes sexually dimorphic after puberty. Following the increase in circulating steroids at puberty, the vasopressin- and oxytocin-containing nucleus becomes twice as large in both males and females. In adulthood, the vasopressin- and oxytocin-containing nucleus of females is approximately twice as large as that in males. Because these alterations are possibly due to an influence of gonadal steroids, i.e. estrogens, the vasopressin- and oxytocin-containing the presence of estrogen receptors. In addition to the area of the vasopressin- and oxytocin-containing nucleus, the present study documented the distribution of estrogen receptors in the septal area and other parts of the hypothalamus of intact post-pubertal male and female pigs, by utilizing immunocytochemical methodology. Intense nuclear estrogen receptor staining was found in a number of areas, i.e. the medial preoptic
TY - JOUR. T1 - Estrogen receptor α wields treatment-specific enhancers between morphologically similar endometrial tumors. AU - Droog, Marjolein. AU - Nevedomskaya, Ekaterina. AU - Dackus, Gwen M.. AU - Fles, Renske. AU - Kim, Yongsoo. AU - Hollema, Harry. AU - Mourits, Marian. AU - Nederlof, Petra M.. AU - Van Boven, Hester H.. AU - Linn, Sabine C.. AU - Van Leeuwen, Flora E.. AU - Wessels, Lodewyk F.A.. AU - Zwart, Wilbert. PY - 2017/2/21. Y1 - 2017/2/21. N2 - The DNA-binding sites of estrogen receptor α (ERα) show great plasticity under the control of hormones and endocrine therapy. Tamoxifen is a widely applied therapy in breast cancer that affects ERα interactions with coregulators and shifts the DNA-binding signature of ERα upon prolonged exposure in breast cancer. Although tamoxifen inhibits the progression of breast cancer, it increases the risk of endometrial cancer in postmenopausal women. We therefore asked whether the DNA-binding signature of ERα differs between endometrial ...
Receptors are proteins on cells that may attach to hormones that circulate in the blood. Normal breast cells and some breast cancer cells have receptors that attach to estrogen and progesterone. These two hormones often fuel the growth of breast cancer cells.. A biopsy can check to see if the cells have estrogen or progesterone receptors.. Cancer cells may contain neither, one, or both of these receptors. Breast cancers that contain estrogen receptors are called ER-positive (ER+) cancers, while those containing progesterone receptors are called PR-positive (PR+) cancers.. Women with hormone receptor-positive cancers tend to have a better prognosis and are much more likely to respond to hormone therapy than women with cancers without these receptors.. The ACS says that about one of five breast cancers have too much of a growth-promoting protein called HER2. The HER2 gene instructs the cells to make this protein. Tumors with increased levels of HER2 are referred to as HER2-positive.. Because ...
Breast cancer is a major cause of death worldwide. Human cytochrome P450 (CYP) 1B1 is a key enzyme in the metabolism of 17β-estradiol, and CYP1B1-metabolized 4-hydroxyestradiol is a marker for breast cancer. Furthermore, overexpression of cyclooxygenase-2 (COX-2), which produces prostaglandin E2 (PGE2), has been detected in invasive breast carcinomas. However, the interaction between PGE2 and CYP1B1 expression in human breast cancer is unclear. Here, we investigated the effect of PGE2 on CYP1B1 expression and its mechanism in breast cancer cells. PGE2 significantly increased CYP1B1 protein and messenger RNA expression and dose dependently enhanced CYP1B1 promoter activity in human breast cancer MCF-7 cells. Transient transfection with human CYP1B1 (hCYP1B1) deletion promoter constructs and cotreatment with inhibitors revealed that the estrogen response element contributed to the effects of PGE2. CYP1B1 expression was not affected by PGE2 in estrogen receptor (ER) α-negative MDA-MB-231 breast ...
Oncogenesis in breast cancer is often associated with excess estrogen receptor α(ERα) activation and overexpression of its coactivators. LRP16 is both an ERα target gene and an ERα coactivator, and plays a crucial role in ERα activation and proliferation of MCF-7 breast cancer cells. However, the regulation of the functional availability of this coactivator protein is not yet clear. Yeast two-hybrid screening, GST pulldown and coimmunoprecipitation (CoIP) identified the cytoplasmic intermediate filament protein keratin 18 (K18) as a novel LRP16-interacting protein. Fluorescence analysis revealed that GFP-tagged LRP16 was primarily localized in the nuclei of mock-transfected MCF-7 cells but was predominantly present in the cytoplasm of K18-transfected cells. Immunoblotting analysis demonstrated that the amount of cytoplasmic LRP16 was markedly increased in cells overexpressing K18 whereas nuclear levels were depressed. Conversely, knockdown of endogenous K18 expression in MCF-7 cells significantly
The amounts of estrogen receptor (ER) and progesterone receptor (PgR) in a primary tumor are predictive of the response to endocrine therapies of breast cancer. Several patients with ER-positive primary tumors relapse after adjuvant endocrine therapy with no ER expression in the recurrent tissue; much fewer with a recurrent disease after an ER-negative primary tumor may become endocrine responsive. These sequences of events indicate that a phenotype based on ER expression may not be a permanent feature of breast cancer. Ten patients with advanced breast cancer whose tumors overexpressed HER-2, but not ER or PgR, were treated with weekly trastuzumab at standard doses with or without chemotherapy. Three out of 10 patients showed overexpression of ERs first appearing after 9, 12 and 37 weeks, respectively, from the initiation of trastuzumab. Two of these patients were subsequently treated with endocrine therapy alone: one of them received letrozole for 3 years without evidence of progression. Therapeutic
The cytotoxic activity of PINO on human breast tumour cells is a debated issue. Previously, Chin et al. [25] described that PINO has a cytotoxic effect against MCF7 breast cancer cells (ED50 = 4.74 μM); however, in a later article [21], the same author found no cytotoxic effects. Surprisingly, the range of concentrations used in both studies was not specified. In addition, the cytotoxic effects of PINO in MDA-MB-231 cells have not been previously reported. In contrast, we tested a wide range of PINO concentrations and showed that there was cytotoxic activity at different concentrations in both human breast tumour cells tested. While PINO showed cytotoxic activity in both types of human breast tumour cells tested, the effect was more pronounced in negative oestrogen receptor tumour cells compared to oestrogen receptor-positive tumour cells (Figs. 4 and 5). In addition, for the first time, we describe the effects of PINO on human mammary epithelial cells. Our results suggest that PINO ranging ...
TY - JOUR. T1 - ERβ1 represses FOXM1 expression through targeting ERα to control cell proliferation in breast cancer. AU - Horimoto, Yoshiya. AU - Hartman, Johan. AU - Millour, Julie. AU - Pollock, Steven. AU - Olmos, Yolanda. AU - Ho, Ka-Kei. AU - Coombes, R Charles. AU - Poutanen, Matti. AU - Mäkelä, Sari I. AU - El-Bahrawy, Mona. AU - Speirs, Valerie. AU - Lam, Eric W-F. N1 - Copyright © 2011 American Society for Investigative Pathology. Published by Elsevier Inc. All rights reserved.. PY - 2011/9. Y1 - 2011/9. N2 - In this study, we investigated the effects of ectopic estrogen receptor (ER)β1 expression in breast cancer cell lines and nude mice xenografts and observed that ERβ1 expression suppresses tumor growth and represses FOXM1 mRNA and protein expression in ERα-positive but not ERα-negative breast cancer cells. Furthermore, a significant inverse correlation exists between ERβ1 and FOXM1 expression at both protein and mRNA transcript levels in ERα-positive breast cancer ...
Selective estrogen receptor modulators[edit]. SERMs are a category of drugs, either synthetically produced or derived from a ... Low-dose prescription vaginal estrogen products such as estrogen creams are generally a safe way to use estrogen topically, to ... that act selectively as agonists or antagonists on the estrogen receptors throughout the body. The most commonly prescribed ... is the use of estrogen in women without a uterus and estrogen plus progestin in women who have an intact uterus.[70] ...
Resistance to selective estrogen receptor modulator drugs[edit]. Selective estrogen receptor modulators (SERMs) are a commonly ... "Changes in estrogen receptor, progesterone receptor, and pS2 expression in tamoxifen-resistant human breast cancer". Cancer Res ... Loss of estrogen receptor alpha (ERα)[110] *Although this may be a mechanism of resistance in a minority of women, most ERα+ ... Mutations in estrogen receptors. *Alterations in co-regulatory proteins *Interactions between the SERM, ER, and co-regulatory ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... V Craig Jordan (27 May 2013). Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health: Progress and Promise ... They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production.[1][2] Antiestrogens are ... Estrogen receptor modulators. Androgens and antiandrogens. Progestogens and antiprogestogens. List of estrogens. ...
Godfrey SE (May 1989). "Estrogen receptors". American Journal of Clinical Pathology. 91 (5): 629-30. doi:10.1215/15228517-2008- ... metastatic or recurrent non-squamous non-small cell lung cancer with Epidermal Growth Factor Receptor (EGFR) activating ... or primary peritoneal cancer who have not received prior therapy with bevacizumab or other VEGF inhibitors or VEGF receptor- ...
... or G-Protein-Coupled Estrogen Receptor (GPER)". Estrogen Receptors. Methods in Molecular Biology. 1366. pp. 11-7. doi:10.1007/ ... G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505-40. doi:10.1124/pr. ... 2-Methoxyestradiol is derived from estradiol, although it interacts poorly with the estrogen receptors (2,000-fold lower ... it retains activity as a high-affinity agonist of the G protein-coupled estrogen receptor (GPER) (10 nM, relative to 3-6 nM for ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Estrogen receptor modulators. Androgens and antiandrogens. Progestogens and antiprogestogens. List of estrogens. ... Acolbifene (INN) (developmental code names EM-652, SCH-57068) is a nonsteroidal selective estrogen receptor modulator (SERM) ... a pure selective estrogen receptor modulator. Study of nitrogen substitution". Journal of enzyme inhibition and medicinal ...
Selective estrogen-receptor modulators. [8] Erythropoiesis-stimulating agents. [8] Acute medical illness. [8] ... Estrogen-based oral contraceptive. discontinuation reduces risk. [8][11][14] Hormone replacement therapy. discontinuation ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Estrogen receptor modulators. Androgens and antiandrogens. Progestogens and antiprogestogens. List of estrogens. ... List of selective estrogen receptor modulators. References[edit]. *^ V. H. T. James; J. R. Pasqualini (22 October 2013). ... nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group[1] that has been used in Europe as a ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans ... "Role of estrogen receptors and g protein-coupled estrogen receptor in regulation of hypothalamus-pituitary-testis axis and ... the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have ...
SERM (selective estrogen receptor modulators) *Raloxifene. *Vasodilators *Minoxidil. *Neuroleptics (antipsychotics) *Droperidol ...
However, in contrast to androstenediol, its affinity for the estrogen receptors is very low, with less than 0.01% of the ... "DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ... "Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... Thus, theca cells and granulosa cells work together to form estrogens. Androstanedione is a 5α-reduced metabolite of 4- ...
... acts as a selective estrogen receptor modulator (SERM), or as a partial agonist of the estrogen receptors (ERs). It ... September 2007). "Estrogen prevents bone loss via estrogen receptor alpha and induction of Fas ligand in osteoclasts". Cell. ... "Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health" Imperial College Press, Singapore. ... Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ...
"Molecular aspects of phytoestrogen selective binding at estrogen receptors". Journal of Pharmaceutical Sciences. 96 (8): 1879- ... "Nicotinic acetylcholine receptors: Introduction". IUPHAR Database. International Union of Basic and Clinical Pharmacology. ... The alkaloid nicotine from tobacco binds directly to the body's Nicotinic acetylcholine receptors, accounting for its ... Polyphenols include phytoestrogens (top and middle), mimics of animal estrogen (bottom).[71] ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Estradiol affects target tissues mainly by interacting with two nuclear receptors called estrogen receptor α (ERα) and estrogen ... The estrogen receptor, as well as the progesterone receptor, have been detected in the skin, including in keratinocytes and ... Fritz F. Parl (2000). Estrogens, Estrogen Receptor and Breast Cancer. IOS Press. pp. 4-. ISBN 978-0-9673355-4-4.. ...
Thus, GH exerts some of its effects by binding to receptors on target cells, where it activates the MAPK/ERK pathway.[35] ... Estrogen. *Clonidine and L-DOPA by stimulating GHRH release[23]. *α4β2 nicotinic agonists, including nicotine, which also act ... Lin-Su K, Wajnrajch MP (December 2002). "Growth Hormone Releasing Hormone (GHRH) and the GHRH Receptor". Reviews in Endocrine ... Yi S, Bernat B, Pál G, Kossiakoff A, Li WH (July 2002). "Functional promiscuity of squirrel monkey growth hormone receptor ...
The cells express estrogen/progesterone-receptors. Undifferentiated uterine sarcoma, or undifferentiated (high-grade) ...
Kapley's early studies investigated estrogen receptors. After moving to CSIR National Environmental Engineering Research ... "Cholesterol inhibits the nuclear entry of estrogen receptor activation factor (E-RAF) and its dimerization with the ... nonactivated estrogen receptor (naER) in goat uterus". Journal of Cellular Biochemistry. 77 (3): 382-395. doi:10.1002/(SICI) ... studies at the University of Hyderabad researching endogenous factors that regulate the DNA binding of the receptor-estrogen ...
Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... C. acnes' ability to bind and activate a class of immune system receptors known as toll-like receptors (TLRs), especially TLR2 ... It is usually combined with an estrogen to avoid menstrual irregularities and estrogen deficiency.[113] The medication appears ... In women, the use of combined birth control pills can improve acne.[100] These medications contain an estrogen and a progestin. ...
"Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists". Molecular ... Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist-antagonist of the estrogen receptor ... and of invasive estrogen receptor-positive breast cancer by 84%. Conversely, it does not reduce the risk of estrogen receptor- ... Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ...
CTA is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. It is a high- ... CTA is a high-efficacy partial agonist of the estrogen receptor. As such, it is a selective estrogen receptor modulator (SERM ... efficacy partial estrogen and shows some properties of a selective estrogen receptor modulator, with predominantly estrogenic ... Luniwal A, Jetson R, Erhardt P (2012). "Selective Estrogen Receptor Modulators". In Fischer J, Ganellin CR, Rotella DP (eds.). ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Synthesis of Non-steroidal Estrogen Receptor Proteolysis Targeting Chimeric Molecules (PROTACS). ProQuest. 2008. pp. 11-. ISBN ... Cytoplasmic and Nuclear Receptors-Advances in Research and Application: 2012 Edition. ScholarlyEditions. 26 December 2012. pp. ... Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50-. ISBN 978-3- ...
They typically have estrogen and/or progesterone receptors. The prognosis for low-grade endometrial stromal sarcoma is good, ... If a tumor is well-differentiated and known to have progesterone and estrogen receptors, progestins may be used in treatment. ... This treatment is effective in endometrial stromal sarcomas because they typically have estrogen and/or progestin receptors. ... Whereas taking estrogen alone increases the risk of endometrial cancer, taking both estrogen and a progestogen in combination, ...
7α-OH-DHEA has weak estrogenic activity, selectively activating the estrogen receptor ERβ. In addition, 7α-OH-DHEA may be ... "DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ...
7β-OH-DHEA has weak antiestrogenic activity, selectively antagonizing the estrogen receptor ERβ. 7β-OH-DHEA is on the World ... "DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ...
Ariazi EA, Ariazi JL, Cordera F, Jordan VC (2006). "Estrogen receptors as therapeutic targets in breast cancer". Curr Top Med ... It has been documented rarely with the selective estrogen receptor modulators (SERMs) tamoxifen and raloxifene. The phenomenon ... One proposed theory for the mechanism is that the sensitivity of breast cells to estrogens shifts with estrogen deprivation, ... endogenous estrogen acts in the manner of high-dose estrogen therapy in the breast to inhibit breast cancer growth and induce ...
One study involved estrogen receptors and differential splicing. The article entitled, "Alternative splicing of the human ... Ferro P, Forlani A, Muselli M, Pfeffer U (September 2003). "Alternative splicing of the human estrogen receptor alpha primary ... explains that 1785 nucleotides of the region in the DNA that codes for the estrogen receptor alpha (ER-alpha) are spread over a ... estrogen receptor alpha primary transcript: mechanisms of exon skipping" by Paola Ferro, Alessandra Forlani, Marco Muselli and ...
"DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ...
It is an estrogen, or an agonist of the estrogen receptors, the biological target of estrogens like estradiol. Methylestradiol ... Methylestradiol is an estrogen, or an agonist of the estrogen receptor. It shows somewhat lower affinity for the estrogen ... Feenstra A, Vaalburg W, Nolten GM, Reiffers S, Talma AG, Wiegman T, van der Molen HD, Woldring MG (1983). "Estrogen receptor ... methylestradiol has been studied for use as a radiopharmaceutical for the estrogen receptor. Methylestradiol is used in ...
... to 60-fold increased affinity for the estrogen receptor and reduced partial estrogen agonistic activity. The affinity of ... 165-. ISBN 978-0-470-69703-0. Grese TA, Dodge JA (February 1998). "Selective estrogen receptor modulators (SERMs)". Current ... Wittliff, J. L., Kerr II, D. A., & Andres, S. A. (2005). "Estrogens IV: Estrogen-Like Pharmaceuticals". In Wexler, P. (ed.). ... is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that was developed originally in ...
... both have measurable affinity for the estrogen receptor and are able to activate the receptor and induce progesterone receptor ... ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site". Steroids. 62 (3 ... Brooks SC, Wappler NL, Corombos JD, Doherty LM, Horwitz JP (1987). "Estrogen structure-receptor function relationships". In ... Schwartz JA, Skafar DF (September 1993). "Ligand-mediated modulation of estrogen receptor conformation by estradiol analogs". ...
2.1) Nuclear receptor (Cys4). .mw-parser-output .nobold{font-weight:normal}. subfamily 1. *Thyroid hormone *α ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Selected biological properties of endogenous estrogens in rats Estrogen. ER RBA (%). Uterine weight (%). Uterotrophy. LH levels ... ER RBA = Relative binding affinity to estrogen receptors of rat uterine cytosol. Uterine weight = Percentage change in uterine ... Oettel M, Schillinger E (6 December 2012). Estrogens and Antiestrogens I: Physiology and Mechanisms of Action of Estrogens and ...
Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ... Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat • ... GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1 ...
T4 and T3 bind to thyroid receptor proteins in the cell nucleus and cause metabolic effects through the control of DNA ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor modulators. Estrogen receptor modulators. ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... Progesterone receptor modulators. Androgens and antiandrogens. Estrogens and antiestrogens. List of progestogens. ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Melatoninski receptor 1C (MTNR1C) je protein koji je kodiran Mtnr1c genom. Ovaj receptor je identifikovan kod riba, vodozemaca ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... 2000). „Melatonin receptor mRNA expression in human granulosa cells". Mol. Cell. Endocrinol. 156 (1-2): 107-10. PMID 10612428. ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ... Adrenergički receptor. Reference[uredi - уреди , uredi izvor]. *↑ Ruuskanen JO, Xhaard H, Marjamäki A, Salaneck E, Salminen T, ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... but not estrogens, increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... Again it was noted that AHN was not increase via activation of the estrogen receptors.[13] ...
... activities by activating estrogen receptors. Quercetin activates both estrogen receptor alpha (ERα) and beta (ERβ)[23] with ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).[26][27] ... "Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on ... "The stimulation of cell proliferation by quercetin is mediated by the estrogen receptor". (primary). Molecular Nutrition & Food ...
... and are analogous to selective estrogen receptor degraders (SERDs) like fulvestrant (a drug used to treat estrogen receptor- ... Androgen receptor degradersEdit. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... and estrogens like estradiol, estradiol esters, ethinylestradiol, conjugated estrogens, diethylstilbestrol, and bifluranol.[2][ ... Combined Estrogen-progestogen Contraceptives and Combined Estrogen-progestogen Menopausal Therapy. World Health Organization. ...
"The interaction of canrenone with oestrogen and progesterone receptors in human uterine cytosol". British Journal of Clinical ... Main articles: Progesterone receptor A, Progesterone receptor B, and Progesterone receptor C ... steroid hormone receptor activity. • steroid binding. • protein binding. • enzyme binding. • receptor binding. • lipid binding ... The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Gama-hidroksibuteratni receptor, ili GHB receptor (GHBR), originalno identifikovan kao GPR172A, je G protein-spregnuti receptor ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... Nakon otkrića orfan G-protein spregnutog receptora GPR172A, utvrđeno je da je on zapravo GHB receptor.[1] GHB receptor pacova ...
Holtorf prescribes naltrexone, an opioid receptor blocker, used most often to treat opiate addiction, and buproprion ( ... North American Menopause, Society (2010). "Estrogen and progestogen use in postmenopausal women: 2010 position statement of the ...
Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Receptor ukusa tip 2 član 19 je protein koji je kod ljudi kodiran TAS2R19 genom.[1] ... Fischer A, Gilad Y, Man O, Pääbo S (2005). "Evolution of bitter taste receptors in humans and apes.". Mol. Biol. Evol. 22 (3): ...
"High RAD51 mRNA expression characterize estrogen receptor-positive/progesteron receptor-negative breast cancer and is ... Breast cancer (progesteron receptor negative). Over-expression. -. messenger RNA. [16]. Breast cancer. Under-expression. 30%. ...
Estrogen insensitivity syndrome. *X-linked adrenal hypoplasia congenita. *MODY 1. *Familial partial lipodystrophy 3 ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1 ... an unusual member in the family of hormone receptors with seven transmembrane segments". Genomics. 26 (2): 334-44. PMID 7601460 ...
選擇性雌激素受體調節物(SERM)是一種人工合成或是從植物提煉的藥物,可以 選擇性的成為雌激素受体(英语:estrogen receptor)的激动剂或拮抗剂,進行調節作用。最常見的有雷洛昔芬(英语:raloxifene)及諾瓦得士。雷洛昔芬在骨骼和脂质 ... The Woman's Health Program Monash University, Oestrogen and Progestin as Hormone Therapy (页面存档备份,存于互联
Low-density lipoproteins are taken into the cell by LDL receptor-mediated endocytosis in clathrin-coated pits, and then ... estrogens, and testosterone (the sex hormones), and their derivatives. It provides the basic structure of all the steroids. In ... By serving as ligands for specific receptors on cell membranes, the apolipoproteins that reside on the surface of a given ... Among the genes transcribed are the LDL receptor and HMG-CoA reductase. The former scavenges circulating LDL from the ...
"Estrogen receptor alpha interacts with mitochondrial protein HADHB and affects beta-oxidation activity". Molecular & Cellular ... and the interaction may play an important role in the estrogen-mediated lipid metabolism in animals and humans.[14] ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ... cell surface receptor signaling pathway. • vasculature development. • regulation of autophagy of mitochondrion. • branching ...
第三亚族(甾类激素(英语:Steroid hormone receptor)(雄激素、雌激素(α、β)、糖皮质激素、盐皮质激素、孕酮)、雌激素相关(英语:Estrogen related receptor)(α、β、γ)). 第四亚族NUR(英语:Nur ... 第一亚族:甲状腺激素受体(英语:Thyroid hormone receptor)(α、β)、CAR、FXR
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... "In vivo estrogen bioactivities and in vitro estrogen receptor binding and transcriptional activities of anticoagulant synthetic ... Prolame, also known as 17β-((3-hydroxypropyl)amino)estradiol, is a synthetic, steroidal estrogen and a 17β-aminoestrogen with ... an amino-estrogen with prolonged anticoagulant and brief estrogenic effects". Steroids. 45 (2): 151-7. PMID 3841424.. ...
The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... receptor binding. • neurotrophin TRKB receptor binding. • growth factor activity. • GO:0001948 protein binding. ... regulation of receptor activity. • activation of phospholipase C activity. • neurotrophin TRK receptor signaling pathway. • ... NMDA receptor activity[edit]. NMDA receptor activation is essential to producing the activity-dependent molecular changes ...
GnRH and gonadotropin receptor modulators. Androgens and antiandrogens. Estrogens and antiestrogens. Progestogens and ... See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators • GnRH and gonadotropins ... is achieved through receptor downregulation by internalization of receptors.[11] Generally this induced and reversible ... They are agonists of the GnRH receptor and work by increasing or decreasing the release of gonadotropins and the production of ...
Ethinylestradiol is a semi-synthetic estrogen. Specific compounds that have partial agonist activity for steroid receptors, and ... estrogens, and progestogens. Their effects are mediated by slow genomic mechanisms through nuclear receptors as well as by fast ... Guerriero, G (April 2009). "Vertebrate sex steroid receptors: evolution, ligands, and neurodistribution". Annals of the New ... In many contexts, the two main classes of sex hormones are androgens and estrogens, of which the most important human ...
... activation of the D2 receptor promoter by members of the retinoic acid receptor-retinoid X receptor family". Proceedings of the ... Isotretinoin has a low affinity for retinoic acid receptors (RAR) and retinoid X receptors (RXR), but may be converted ... transcriptional activation of the dopamine D2 receptor - in addition to serotonin and glutamate receptors - is regulated by ... Isotretinoin is also thought to affect the serotonergic system - it increases expression of 5-HT1A receptors in the pre- ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Nociceptinski receptor (NOP, orfaninski FQ receptor, kapa tip 3 opioidni receptor) je protein koji je kod čoveka kodiran OPRL1 ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... Opioid Receptors: NOP". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. ...
Human megakaryocytes and platelets contain the estrogen receptor beta and androgen receptor (AR): testosterone regulates AR ... Monoclonal antibodies to human estrogen receptor. G L Greene, C Nolan, J P Engler, and E V Jensen ... Extranuclear estrogen receptor protein (estrophilin) of MCF-7 human breast cancer cells was purified by passage of the cytosol ... Estrogen Receptor Status by Immunohistochemistry Is Superior to the Ligand-Binding Assay for Predicting Response to Adjuvant ...
Other articles where Estrogen-receptor-positive breast cancer is discussed: breast cancer: Types of breast cancer: ER positive ...
Estrogen receptor/progesterone receptor tests look for receptors that attach to the hormones estrogen and/or progesterone in ... Breast cancers that have these receptors often respond well to some types of treatments. Learn more. ... Receptors are proteins that attach to certain substances. ... What are estrogen receptor/progesterone receptor (ER/PR) tests? ... medlineplus.gov/lab-tests/estrogen-receptor-progesterone-receptor-tests/ Estrogen Receptor, Progesterone Receptor Tests. ...
... block the effects of estrogen in breast tissue. Learn more about ERDs today. ... ERDs sit in the estrogen receptors in breast cells. If an ERD is in the estrogen receptor, there is no room for estrogen and it ... ERDs keep estrogen from latching onto hormone receptors. Hormone receptors are like ears or antennae on a cell. Estrogen sends ... Cells with estrogen receptors grow and multiply when estrogen attaches to the receptors. But ERDs like Faslodex break down ...
InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites. We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their individual strengths to produce a powerful integrated database and diagnostic tool.
... block the effects of estrogen in the breast tissue. Learn more about SERMs today. ... Selective estrogen receptor modulators, called SERMs for short, ... also have estrogen receptors. But each estrogen receptor has a ... So breast cell estrogen receptors are different from bone cell estrogen receptors and both of those estrogen receptors are ... SERMs work by sitting in the estrogen receptors in breast cells. If a SERM is in the estrogen receptor, there is no room for ...
Nearly 75 percent of all breast cancers are estrogen-receptor positive, which means the presence of estrogen triggers tumor ... Estrogen receptors are proteins found on the surface of cells that receive signals from the hormone to direct activity within ... To treat ER-positive breast cancer, doctors use hormone therapy to block estrogen from binding to receptors in the cancer cells ... Research Title: Multifaceted modeling of estrogen receptor. Funding Source: National Institutes of Health. Website: theyanglab. ...
The estrogen receptor alpha (ERα) is a classical ligand-activated transcription factor with well-known physiological effects on ... explored the gene regulatory activity of estrogen receptor β, a similar molecule with quite distinct antiproliferative and anti ... Estrogen receptor β binds to and regulates three distinct classes of target genes. J. Biol. Chem. 285, 22059-22066 (2010). [ ... were regulated by the unbound receptor but showed potentiated effects in the presence of estrogen. Furthermore, analysis of ERβ ...
Estrogen receptor (ER)3 gene expression in breast epithelium is an intricately regulated event. The human ER gene is ... Estrogen receptor variants J Mammary Gland Biol Neoplasia. 1998 Jan;3(1):73-83. doi: 10.1023/a:1018726418931. ... Estrogen receptor (ER)3 gene expression in breast epithelium is an intricately regulated event. The human ER gene is ...
Estrogen-related receptor gamma functions as a tumor suppressor in gastric cancer. [Nat Commun. 2018] Estrogen-related receptor ... estrogen-related receptor gamma isoform 2 [Homo sapiens] estrogen-related receptor gamma isoform 2 [Homo sapiens]. gi,343780860 ... This gene encodes a member of the estrogen receptor-related receptor (ESRR) family, which belongs to the nuclear hormone ... Influence of estrogen-related receptor γ (ESRRG) rs1890552 A , G polymorphism on changes in fasting glucose and arterial ...
Estrogens are well-known regulators of the immune responses. Most of their effects are mediated by two receptors: estrogen ... Estrogen receptor profiles in human peripheral blood lymphocytes.. Pierdominici M1, Maselli A, Colasanti T, Giammarioli AM, ... In conclusion our data could provide new insights as concerns the estrogen-related mechanisms of immune system modulation. They ... receptor (ER)alpha and ERbeta. Up to date the presence of intracellular ER in human immune cells represents a controversial ...
Expected for release later this year, the 2019 "Estrogen and Progesterone Receptor Testing in Breast Cancer: American Society ... Testing of Estrogen and Progesterone Receptors (ER/PgR) in Breast Cancer. During the open comment period, April15-29, 2019, the ... Estrogen and Progesterone Receptor Testing in Breast Cancer Guideline Update Estrogen and Progesterone Receptor Testing in ...
This is the summary of results of the estrogen receptor assay. ... and Estrogen Receptor Summary. Source item number: Derived from ... and Estrogen Receptor Summary and is the summary of results of the estrogen receptor (ER) assay. ... Estrogen Receptor Summary from Site-Specific Data Item) ...
If alpha estrogen receptors can be used as a drug target, then perhaps the gamma estrogen-related receptor subtype can as well ... estrogen receptors that the drug is designed to bind on to and inhibit, but many more "gamma" estrogen-related receptors, which ... tamoxifen is approved to treat both early and advanced breast cancer that is estrogen-receptor positive. (Estrogen-receptor ... Tamoxifen binds to the estrogen receptors (alpha) that stud tumors and other breast tissue, not allowing estrogen to latch on ...
Air pollution Breast cancer Cancer survival Estrogen receptor Particulate matter This is a preview of subscription content, log ... and estrogen-disrupting activity in human breast carcinoma cell lines. J Environ Sci Health, Part A: Tox Hazard Subst Environ ...
Regulating Estrogen Receptors Cytoplasmic Partners Message Subject. (Your Name) has forwarded a page to you from Science ... The estrogen (E2) receptor is best known for its actions as a transcriptional activator, but evidence continues to accumulate ... Arginine methylation of estrogen receptor alpha promotes its interaction with cytoplasmic signaling proteins. ... Arginine methylation of estrogen receptor alpha promotes its interaction with cytoplasmic signaling proteins. ...
Estrogen Receptor Positive - ER+. Breast cancer cells that have a protein (receptor molecule) to which estrogen will attach. ... Breast cancer cells that are ER+ need the hormone estrogen to grow and will usually respond to hormone (antiestrogen) therapy ... that blocks these receptor sites, is clearly explained in Medindia s glossary of medical terms ... Estrogen Receptor Positive. Ans : ER+. Breast cancer cells that have a protein (receptor molecule) to which estrogen will ...
An estrogen-dependent four-gene micronet regulating social recognition: A study with oxytocin and estrogen receptor-{alpha} and ... In the nervous system, estrogen signals are transduced by both nuclear estrogen receptors (ERα and ERβ), which act as ... estrogen receptor;. WT,. wild type;. OF,. open field;. BLA,. basolateral amygdala;. LTP,. long-term potentiation;. GAD,. ... We propose that estrogen nuclear receptors may be key mediators of these regulatory functions of estrogen. Moreover, ERβ may be ...
Estrogen receptor-α (ERα) and transforming growth factor (TGF)-β signaling pathways are major regulators during mammary gland ... The estrogen receptor beta-isoform (ERbeta) of the human estrogen receptor modulates ERalpha transcriptional activity and is a ... Phosphorylation of estrogen receptor alpha blocks its acetylation and regulates estrogen sensitivity. Cancer Res. 2004;64:9199- ... Estrogen receptor null mice: what have we learned and where will they lead us? Endocr Rev. 1999;20:358-417.PubMedCrossRefGoogle ...
Estrogen receptor antagonists. Class Summary. Inhibit estrogen effects by competitively binding to the estrogen receptor. ... Competitively binds to the estrogen receptor, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen ... Estrogen-receptor protein in intracranial meningiomas. J Neurosurg. 1979 Apr. 50(4):499-502. [Medline]. ...
Receptors, Estrogen: Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription ... Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important. ...
XERE stands for Xenopus Estrogen Receptor ERE. XERE is defined as Xenopus Estrogen Receptor ERE very rarely. ... www.acronymfinder.com/Xenopus-Estrogen-Receptor-ERE-(XERE).html. *Chicago style: Acronym Finder. S.v. "XERE." Retrieved ... www.acronymfinder.com/Xenopus-Estrogen-Receptor-ERE-(XERE).html,XERE,/a,. ... www.acronymfinder.com/Xenopus-Estrogen-Receptor-ERE-(XERE).html ... Xenopus Estrogen Receptor (genetics). *XML Encoding Rules for ...
... arylidene aryl ether compounds for treating diseases or disorders mediated through modulation of estrogen related receptor ... ERR-α, an orphan receptor, is the first of the three identified members of the estrogen receptor related subfamily of orphan ... A sub-class of these receptors where no natural ligand has been identified is for the estrogen related receptors (ERRs). ... and conditions mediated by estrogen related receptor alpha (ERR-α) activity. BACKGROUND OF THE INVENTION Nuclear receptors are ...
Estrogen Receptors in Moms Placenta Critical During Viral Infection. January 21, 2021. Duke University ... Estrogen levels are much higher during pregnancy, making the GPER1 receptor even better able to suppress interferon signaling ... 15 in Science, they identify a key player in this pathway as a cell-surface estrogen receptor called GPER1 that is especially ... The researchers tried blocking this particular estrogen receptor in pregnant mice with a compound called G15. They found ...
Estrogen receptor. Estrogen receptor refers to a group of receptors that are activated by the hormone 17β-estradiol (estrogen ... This article refers to the nuclear hormone receptor ER.. The main function of the estrogen receptor is as a DNA binding ... Two types of estrogen receptor exist: ER which is a member of the nuclear hormone family of intracellular receptors and the ... However, the estrogen receptor has additional functions independent of DNA binding.. This text uses material from Wikipedia, ...
... are a class of medication that acts on the estrogen receptor.[1] A ... Selective estrogen receptor modulator Selective Estrogen Receptor Modulators (SERMs) ... Selective Estrogen Receptor Modulators (SERMs) are a class of medication that acts on the estrogen receptor.[1] A ... the conformation of the estrogen receptor induced by drug binding which in turn determines how strongly the drug/receptor ...
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular ... Estrogen receptorUniRule annotation. ,p>Information which has been generated by the UniProtKB automatic annotation system, ... R-DRE-8931987 RUNX1 regulates estrogen receptor mediated transcription. R-DRE-8939211 ESR-mediated signaling. R-DRE-9018519 ... R-DRE-8931987 RUNX1 regulates estrogen receptor mediated transcription. R-DRE-8939211 ESR-mediated signaling. R-DRE-9018519 ...
Because of its tissue selectivity, raloxifene may have fewer side effects than are typically observed with estrogen therapy. ... Raloxifene is a selective estrogen receptor modulator that produces both estrogen-agonistic effects on bone and lipid ... metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. ... Raloxifene is a selective estrogen receptor modulator that produces both estrogen-agonistic effects on bone and lipid ...
Estrogen Dominance. Estrogen dominance is a condition with relatively high levels of estrogen and diminished progesterone ... Postmenopausal Osteoporosis: Clinical Guide on Selective Estrogen Receptor Modulators. by Kathy Jones on March 2, 2012 at 8:55 ... This clinical guide details the role of selective estrogen receptor modulators (SERMs) against postmenopausal osteoporosis as ... Furthermore what agent is used (estrogen, SERM, bisphosphonates) may vary over a womans life time. The clinical guide from the ...
Estrogen receptor, ER (ER-alpha) (Estradiol receptor) (Nuclear receptor subfamily 3 group A member 1) ... ER-alpha (Estradiol receptor) (Estrogen receptor) (Nuclear receptor subfamily 3 group A member 1) ... Estrogen receptorImported. ,p>Information which has been imported from another database using automatic procedures.,/p> ,p>,a ... tr,H0Y4W6,H0Y4W6_HUMAN Estrogen receptor OS=Homo sapiens OX=9606 GN=ESR1 PE=1 SV=2 ...
  • Selective estrogen receptor modulators, called SERMs for short, block the effects of estrogen in the breast tissue. (breastcancer.org)
  • SERMs work by sitting in the estrogen receptors in breast cells. (breastcancer.org)
  • Selective Estrogen Receptor Modulators ( SERMs ) are a class of medication that acts on the estrogen receptor . (bionity.com)
  • Breast - all SERMs decrease breast cancer risk, and tamoxifen is mainly used for its ability to inhibit growth in estrogen receptor-positive breast cancer. (bionity.com)
  • The search for this "ideal" compound has led to the development of a class of drugs termed "selective estrogen receptor modulators" (SERMs). (aafp.org)
  • Because SERMs are capable of inducing specific changes in the estrogen receptor, it is not surprising that they may mediate specific pharmacologic activity through their unique agonist or antagonist properties. (aafp.org)
  • This clinical guide details the role of selective estrogen receptor modulators (SERMs) against postmenopausal osteoporosis as the European Medicines Agency (EMA) has approved the use of bazedoxifene and lasofoxifene. (medindia.net)
  • Additional benefits of different agents (i.e. climacteric symptom improvement with estrogens, breast cancer prevention for SERMS) must be considered when selecting the anti-osteoporosis drug. (medindia.net)
  • The finding supports the idea that selective estrogen receptor modulators, or SERMs, are worth pursuing as therapeutics for AD and other cognitive disorders, and that they might yield better results than natural estrogens, which have so far proved disappointing in clinical trials. (alzforum.org)
  • Selective estrogen receptor modulators (SERMs) are a diverse group of -nonsteroidal compounds that function as agonists or antagonists for estrogen receptors (ERs) in a target gene-specific and tissue-specific fashion. (dovepress.com)
  • We examine the role of estrogen therapy in skin aging treatment, discussing successively the indications of hormone replacement therapy (HRT), topical estrogen treatment, and new drugs called selective estrogen receptor modulators (SERMs). (redorbit.com)
  • There is growing evidence that the action of some of these prenylated isoflavonoids is tissue-specific, suggesting that they act like selective estrogen receptor modulators (SERMs), such as the well-known chemically synthesized raloxifene and tamoxifen . (rsc.org)
  • Here, we demonstrate that a single biochemical assay is able to predict the tissue-selective pharmacology of an array of selective estrogen receptor modulators (SERMs). (rcsb.org)
  • In the typical estrogen pathway (i) estrogen or other selective estrogen receptor modulators (SERMs) are bound to the estrogen receptor (ER) via the coregulatory proteins (CoReg) in the nucleus. (wikipedia.org)
  • Selective Estrogen Receptor Modulator or SERMs, are often called designer estrogens. (americanbonehealth.org)
  • SERMs have some effects similar to estrogen on bone, cholesterol and other blood fats. (americanbonehealth.org)
  • SERMs decrease the effects of estrogen on certain tissues like the breast and uterus, and may be used with people who are at risk for developing these cancers. (americanbonehealth.org)
  • Extranuclear estrogen receptor protein (estrophilin) of MCF-7 human breast cancer cells was purified by passage of the cytosol fraction of a cell homogenate through an affinity column of estradiol linked to Sepharose by a substituted di-n-propyl sulfide bridge in the 17 alpha position. (pnas.org)
  • Serum from a Lewis rat immunized with this partially purified estradiol-receptor complex contained antiestrophilin antibodies that reacted not only with nuclear and extranuclear estradiol-receptor complexes from MCF-7 cells but also with estrophilin from rat, calf, and monkey uterus, hen oviduct, and human breast cancers. (pnas.org)
  • Mood fluctuations, depression, irritability, and anxiety have often been associated with low levels of estradiol in postmenopausal women ( 1 , 2 ), whereas estrogen replacement therapy ameliorates these psychological conditions ( 1 - 3 ). (pnas.org)
  • Estrogen receptor refers to a group of receptors that are activated by the hormone 17β-estradiol (estrogen). (phys.org)
  • Raloxifene (Evista) has the ability to bind to and activate the estrogen receptor while exhibiting tissue-specific effects distinct from estradiol. (aafp.org)
  • A fluorescently labeled estradiol, N'-fluoresceino-N'-(17 beta-estradiol hemisuccinamide) thiourea (FE) was used for measuring estrogen receptor content per cell in tumor cells. (sciencemag.org)
  • An alternative approach to reaping a neurologic benefit from estrogen signaling is to selectively target estrogen receptors, something estradiol itself doesn't do. (alzforum.org)
  • The sc administration of [ 3 H]estradiol to groups of immature rats showed (Fig. 1) ⇓ that the estrogen target tissues ( e.g. , uterus and vagina) bound and retained the [ 3 H] label, but traditional nontarget tissues ( e.g. , muscle, kidney, liver) did not retain the radioactivity. (aacrjournals.org)
  • Natural estrogens such as 17β-estradiol, a nonselective agonist of ERα, ERβ, and GPER, 8 modulate vasoconstrictor prostanoid activity and the expression of TP receptors and prostanoid synthases. (ahajournals.org)
  • 20 - 26 Furthermore, inhibitory effects of 17β-estradiol on COX-dependent responses to vasoconstrictors have suggested a role of estrogen receptors, 27 although the specific estrogen receptor(s) involved in endothelium-dependent vasoconstriction have not been identified. (ahajournals.org)
  • Isoflavonoids are abundant in Leguminosae , and many of them can bind to the human estrogen receptor (hER) with affinities similar to or lower than that of estradiol . (rsc.org)
  • They are receptors that are activated by the hormone estrogen (17β-estradiol). (wikipedia.org)
  • Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors estrone, and raloxifene bind preferentially to the alpha receptor estriol, and genistein to the beta receptor Subtype selective estrogen receptor modulators preferentially bind to either the α- or the β-subtype of the receptor. (wikipedia.org)
  • Estrogen receptors (ERα and ERβ) are ligand activated nuclear receptor proteins that mediate the action of estradiol and structurally related compounds. (aacrjournals.org)
  • ER-α is a 17β-estradiol-activated steroid receptor member of the nuclear receptor superfamily of transcription factors. (nursa.org)
  • Furthermore, because estradiol may protect the brain through estrogen receptor-mediated mechanisms, we examined expression of both receptor subtypes ERα and ERβ in the normal and injured brain. (jneurosci.org)
  • Estradiol benzoate is asynthetic ester, specifically the 3-benzoyl ester, of the natural estrogen, estradiol. (selleckchem.com)
  • Estradiol is the major estrogen secreted by the premenopausal ovary. (selleckchem.com)
  • Receptors are proteins that attach to certain substances. (medlineplus.gov)
  • Estrogen receptors are proteins found on the surface of cells that receive signals from the hormone to direct activity within the cell. (osc.edu)
  • A classic example of bifunctional transcription factors is the family of Nuclear Receptor (NR) proteins. (nih.gov)
  • Examination of tyrosine phosphorylated proteins associated with the activated receptor identified focal adhesion kinase as a new component in the complex. (sciencemag.org)
  • Arginine methylation of estrogen receptor alpha promotes its interaction with cytoplasmic signaling proteins. (sciencemag.org)
  • Despite sharing structural homology with the Estrogen Receptor family of proteins, ERRs do not bind estrogen and thus allow for transcription regulation by small lipophilic molecules which can act as agonists or inverse agonists. (kenyon.edu)
  • WAY-200070, the more brain-soluble of the two, also increased levels of the glutamate receptor GluR1 and postsynaptic density 95, two proteins important in synaptic activity. (alzforum.org)
  • This specific uptake suggested that these cells must contain binding proteins, which he called "estrogen receptors. (uchicago.edu)
  • These proteins are members of the nuclear receptor family, characterized by distinct structural and functional domains, and participate in the regulation of different biological processes, including cell growth, survival and differentiation. (mdpi.com)
  • Like other steroid hormone receptors, Estrogen Receptors are intracellular proteins. (novusbio.com)
  • ER gene consists of more than 140kb of genomic DNA divided into 8 exons, being translated into a protein with six functionally discrete domains required for transcription activation function, binding to estrogen response element (ERE) constitutive dimerization, binding to heat shock proteins, and ligand recognition. (fishersci.com)
  • Estrogen receptors (ERs) are a group of proteins found inside cells. (wikipedia.org)
  • The concept of selective estrogen receptor modulators is based on the ability to promote ER interactions with different proteins such as transcriptional coactivator or corepressors. (wikipedia.org)
  • Alternately, the estrogen or SERM complexes may occur through the ER located adjacent to the plasma membrane (ii) with the help of adaptor proteins such as caveolin 1 or SHC1, which target the ER complexes to the plasma membrane. (wikipedia.org)
  • Binding of ligand activates ERs, by a mechanism that involves dissociation of heat shock proteins and dimerization of receptor proteins. (atlasgeneticsoncology.org)
  • Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. (abcam.com)
  • NEW YORK (GenomeWeb) - Mutations in the estrogen receptor gene ESR1 appear to be linked to more aggressive disease and poorer patient outcomes in individuals with estrogen receptor-positive metastatic breast cancer, according to a study published today in JAMA Oncology . (genomeweb.com)
  • There are two different forms of the estrogen receptor, usually referred to as α and β, each encoded by a separate gene (ESR1 and ESR2, respectively). (wikipedia.org)
  • In humans, the two forms of the estrogen receptor are encoded by different genes, ESR1 and ESR2 on the sixth and fourteenth chromosome (6q25.1 and 14q23.2), respectively. (wikipedia.org)
  • Both of these are nuclear receptors activated by the sex hormone, estrogen, and encoded by the ESR1 (Estrogen Receptor 1) gene. (wikipedia.org)
  • There are two different forms of the estrogen receptor, alpha and beta, encoded by separate genes (ESR1 and ESR2, respectively). (thermofisher.com)
  • Estrogen receptor-alpha (ESR1) is highly expressed in the efferent ductules of all species studied as well as in the epididymal epithelium in mice and other select species. (bioone.org)
  • Tamoxifen is the oldest and most-prescribed selective estrogen receptor modulator (SERM). (breastcancer.org)
  • Several studies have compared tamoxifen with aromatase inhibitors to see which type of medicine was more effective in treating early-stage, hormone-receptor-positive breast cancer in postmenopausal women. (breastcancer.org)
  • When treating early-stage, hormone-receptor-positive breast cancer, aromatase inhibitors have more benefits and fewer serious side effects than tamoxifen. (breastcancer.org)
  • For premenopausal women diagnosed with hormone-receptor-positive breast cancer, the SERM tamoxifen is the hormonal therapy treatment standard. (breastcancer.org)
  • In the November 1 issue of the journal Cancer Research , the researchers show that breast cancer cells that are resistant to tamoxifen display few of the "alpha" estrogen receptors that the drug is designed to bind on to and inhibit, but many more "gamma" estrogen-related receptors, which tamoxifen seems to activate. (medicalnewstoday.com)
  • But what the researchers found in invasive lobular carcinomas - the specific cancer they studied - may also be true of tamoxifen resistance in other cancer types," she said "No one has looked for gamma estrogen-related receptors in tamoxifen resistance in invasive ductal carcinoma. (medicalnewstoday.com)
  • In addition to its use as a cancer preventive, tamoxifen is approved to treat both early and advanced breast cancer that is estrogen-receptor positive. (medicalnewstoday.com)
  • The G-protein coupled estrogen receptor (GPER), an alternate estrogen receptor (ER) with a structure distinct from the two canonical ERs, being ERα, and ERβ, is expressed in 50% to 60% of breast cancer tissues and has been presumed to be associated with the development of tamoxifen resistance in ERα positive breast cancer. (mdpi.com)
  • Tamoxifen is useful because it blocks estrogen from the cancer cells via competitive antagonism, and since some breast cancers require estrogen to grow, it thereby inhibits cancer growth. (kenyon.edu)
  • This disappearing act may help explain why ovarian cancers are often typically resistant to anti-estrogen drugs including Tamoxifen. (innovations-report.com)
  • Presence of ER in breast tumors indicates an increased likelihood of response to anti-estrogen (e.g. tamoxifen) therapy. (fishersci.com)
  • Tamoxifen, a selective estrogen receptor (ER) modulator that has antiestrogenic effects in the breast, decreases mammographic density ( 8 -10 ). (aacrjournals.org)
  • Because of their dependency on estrogen, most ER-positive cancers respond well to anti-estrogen therapies, such as Tamoxifen. (health.am)
  • Researchers have shown how estrogen receptor-positive breast cancer tumors become resistant to tamoxifen, the only approved hormonal therapy for premenopausal patients with this type of breast cancer. (health.am)
  • I am looking for an anti-human estrogen receptor antibody. (bio.net)
  • Immunoprecipitation of ERα from the human breast cancer cell line MCF-7 with this antibody showed that methylation of the receptor was increased within 5 min of treatment of cells with E 2 and that the methylated form of the receptor was found exclusively in the cytoplasm (although the bulk of ERα was localized in the nucleus). (sciencemag.org)
  • Ensure accurate, reproducible results in immunohistochemistry and western blotting experiments with Thermo Scientific Estrogen Receptor (SP1), Rabbit Monoclonal Antibody. (fishersci.com)
  • Ensure accurate, reproducible results in immunohistochemistry, western blotting and immunoprecipitation experiments with Thermo Scientific Estrogen Receptor Ab-17, Rabbit Polyclonal Antibody. (fishersci.com)
  • Typically, the antibody used for this experiment is the anti-estrogen Receptor (ER) (SP1) Rabbit Monoclonal Antibody. (wikipedia.org)
  • The following product was used in this experiment: Estrogen Receptor alpha Monoclonal Antibody (33) from Thermo Fisher Scientific, catalog # MA1-310, RRID AB_325422. (thermofisher.com)
  • Competitively binds to the estrogen receptor, producing a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. (medscape.com)
  • The "bridge" identified in the new study links two key receptor parts: one that binds estrogen, and one that attaches to DNA and controls genes in response to estrogen levels. (eurekalert.org)
  • Among the glucosides, sissotorin binds both receptors and the binding is stronger than genistin. (go.jp)
  • The C domain, also known as the DNA-binding domain, binds to estrogen response elements in DNA. (wikipedia.org)
  • This compound binds to the human and murine estrogen receptor α (ERα), and chicken ER with IC50 values in the range of 22-28 nM. (selleckchem.com)
  • The estrogen receptor beta-isoform (ERbeta) of the human estrogen receptor modulates ERalpha transcriptional activity and is a key regulator of the cellular response to estrogens and antiestrogens. (springer.com)
  • Activating just the β isoform of the estrogen receptor (ERβ) is enough to improve learning and memory in mice, according to a paper published in the February 24 Nature Neuroscience. (alzforum.org)
  • Estrogen receptor downregulators, called ERDs for short, block the effects of estrogen in breast tissue. (breastcancer.org)
  • The estrogen (E 2 ) receptor is best known for its actions as a transcriptional activator, but evidence continues to accumulate for rapid nongenomic effects of estrogen receptors outside the nucleus as well. (sciencemag.org)
  • 6 , 7 Other significant side effects of estrogen replacement are vaginal bleeding and breast swelling and tenderness. (aafp.org)
  • These agents may provide the beneficial effects of estrogen replacement therapy without some of its bothersome or potentially serious side effects. (aafp.org)
  • In mammals, the effects of estrogen are mainly mediated by two different estrogen receptors, ERα and ERβ. (mdpi.com)
  • In this article, we review the effects of estrogen on skin biology and particularly its ability to prevent skin aging. (redorbit.com)
  • These monoclonal antibodies should prove useful in the study of estrogen receptors of human reproductive tissues, in particular for the radioimmunochemical assay and immunocytochemical localization of receptors in breast cancers. (pnas.org)
  • About 70 percent of all breast cancers in women have receptors that attach to estrogen and/or progesterone. (medlineplus.gov)
  • About 80 percent to 90 percent of breast cancers in men have these receptors. (medlineplus.gov)
  • Cancers that have one or both types of these receptors. (medlineplus.gov)
  • Nearly 75 percent of all breast cancers are estrogen-receptor positive, which means the presence of estrogen triggers tumor growth. (osc.edu)
  • Researchers at the Icahn School of Medicine at Mount Sinai have identified a protein that can be targeted to suppress growth of a common type of breast cancer known as "estrogen receptor positive" (ER+), including ER+ cancers that are resistant to standard treatments. (eurekalert.org)
  • Approximately 65 percent of all breast cancers express the estrogen receptor (ER +) and/or the progesterone receptor (PR+). (eurekalert.org)
  • Moreover, since the receptor has structural similarities to other hormone receptors central to ovarian, prostate, and endometrial cancers, the new study and the assay could have widespread implications for drug discovery. (eurekalert.org)
  • With the loss of ER beta in ovarian cells, ovarian cancers shed the restrictive properties of this steroid receptor in the regulation of cell growth, death and motility. (innovations-report.com)
  • To confirm that estrogen (ER) and progesterone receptors are present in human lung cancers, 19 resected lung cancers were examined for receptors using a prelabeled sucrose gradient method. (aacrjournals.org)
  • If mammographic density is a risk factor for breast cancer because it represents cumulative effect of both endogenous and exogenous estrogens on the breast and estrogen is associated with an increased risk of ER-positive breast cancer, then mammographic breast density should be a stronger risk factor for ER-positive than ER-negative breast cancers. (aacrjournals.org)
  • ER-positive cancers rely on a source of estrogen to encourage proliferation (increase the number) of cancer cells. (health.am)
  • The estrogen receptor alpha (ERα) is a classical ligand-activated transcription factor with well-known physiological effects on reproduction, bone physiology, and other functions. (sciencemag.org)
  • In the nervous system, estrogen signals are transduced by both nuclear estrogen receptors (ERα and ERβ), which act as transcription factors, and by a nongenomic pathway, which has yet to be identified. (pnas.org)
  • The main function of the estrogen receptor is as a DNA binding transcription factor that regulates gene expression. (phys.org)
  • The proliferative concentrations of glyphosate that induced the activation of estrogen response element (ERE) transcription activity were 5-13 fold of control in T47D-KBluc cells and this activation was inhibited by an estrogen antagonist, ICI 182780, indicating that the estrogenic activity of glyphosate was mediated via ERs. (nih.gov)
  • Estrogen Receptor alpha is a ligand-activated transcription factor that, when bound to estrogen, induces a conformational change that allows dimerization and binding to estrogen response element sequences. (novusbio.com)
  • When bound to DNA, Estrogen Receptor alpha can positively or negatively regulate gene transcription. (novusbio.com)
  • Steroid receptors (SRs) are a superfamily of ligand-dependent nuclear transcription factors that activate responsive genes response to hormone. (novusbio.com)
  • Endogenous estrogens beneficially modulate the activity of endothelial factors by increasing the transcription of the endothelial NO synthase (eNOS) gene 6 and acutely stimulating NO production through eNOS. (ahajournals.org)
  • These coregulators make a bridge between the basal transcription machinery and the receptors by protein-protein interaction. (novapublishers.com)
  • Both progenitor cells and mature DC subsets express estrogen receptors (ERs), which are ligand-dependent transcription factors. (frontiersin.org)
  • Once activated by estrogen, the ER is able to translocate into the nucleus and bind to DNA to regulate the activity of different genes (i.e. it is a DNA-binding transcription factor). (wikipedia.org)
  • The N-terminal A/B domain is able to transactivate gene transcription in the absence of bound ligand (e.g., the estrogen hormone). (wikipedia.org)
  • The ERβ isoforms receptor subtypes can transactivate transcription only when a heterodimer with the functional ERß1 receptor of 59 kDa is formed. (wikipedia.org)
  • ER alpha and ER beta belong to the superfamily of nuclear receptors and specifically to the family of steroid receptors that act as ligand-regulated transcription factors. (atlasgeneticsoncology.org)
  • Estrogen-modulated gene transcription is exerted via different mechanisms: the genomic and the nongenomic pathways. (atlasgeneticsoncology.org)
  • As hormone receptors for sex steroids (steroid hormone receptors), ERs, androgen receptors (ARs), and progesterone receptors (PRs) are important in sexual maturation and gestation. (wikipedia.org)
  • This gene encodes a protein with sequence similarity to the estrogen receptor , a member of nuclear hormone receptor family of steroid hormone receptors . (wikidoc.org)
  • ABSTRACT Estrogens have a profound influence on skin. (redorbit.com)
  • However, the study was unable to show whether this was the case for women with oestrogen receptor positive (ER+) disease - potentially the sub-group most likely to be affected by an increase in the hormone caused by pregnancy. (health.am)
  • Their risk is even higher if they are on anti-estrogen therapy. (rainbow.coop)
  • Anti-estrogen receptor antibodies were among the first of biomarkers which introduced a semi-quantitative assessment of the ER activity. (wikipedia.org)
  • The ERT immunohistochemical assessment is a semi-quantitative method used to predict the likelihood of success to anti-estrogen therapy in breast carcinoma. (wikipedia.org)
  • The anti-estrogen therapies work by blocking the cancer cells' estrogen receptors, effectively cutting off their nourishment. (health.am)
  • An expert panel was convened to consider new evidence that might prompt changes to clinical practices that were established with the 2010 Guideline Recommendations for Immunohistochemical (IHC) Testing of Estrogen and Progesterone Receptors (ER/PgR) in Breast Cancer. (cap.org)
  • [1] A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues. (bionity.com)
  • 3 Acetylcholine and other agonists also stimulate the production of EDCF, including cyclooxygenase (COX)-derived prostanoids that activate thromboxane prostanoid (TP) receptors on vascular smooth muscle cells (VSMC). (ahajournals.org)
  • While we are starting to understand the interaction between estrogen receptors and its ligands contributes to the development of various diseases, the discovery of sub-isoforms of estrogen receptor alpha and beta has further complicated the mechanism of estrogen receptors. (novapublishers.com)
  • Unlike the effects of ERα, which regulated gene expression only when cells were exposed to estrogen, induced expression of ERβ alone, without addition of ligand, regulated hundreds (453) of genes. (sciencemag.org)
  • A still smaller subset of genes (83) were regulated by the unbound receptor but showed potentiated effects in the presence of estrogen. (sciencemag.org)
  • Furthermore, analysis of ERβ binding to examples of the three classes of responsive genes showed that differential binding of the receptor is not the main determinant of responsiveness, because ERβ bound to all three classes of genes. (sciencemag.org)
  • Thus, the authors conclude that unlike ERα, which primarily has a single class of responsive genes, which require ligand-activated receptor for regulation, ERβ has three classes of responsive genes. (sciencemag.org)
  • Although the exact mechanism of action of raloxifene and other similar compounds has not yet been determined, it has been hypothesized that these agents work by inducing conformational changes in the estrogen receptor, resulting in differential expression of specific estrogen-regulated genes in different tissues. (aafp.org)
  • Estrogen-related Receptor-γ (ERR γ) is a nuclear receptor protein that has demonstrated regulatory control over genes in the breast and bone. (kenyon.edu)
  • With this method, Jensen showed that when estrogen bound to this receptor, the compound then migrated to the nucleus where it bound avidly and activated specific genes, stimulating new RNA synthesis. (uchicago.edu)
  • The two estrogen receptor (ER) subtypes are generated from two distinct genes and have partially distinct expression patterns. (mdpi.com)
  • Discover related pathways, diseases and genes to Estrogen Receptor. (novusbio.com)
  • There are two genes that encode for two different estrogen receptors, alpha and beta. (sharecare.com)
  • Find genes regulated by this molecule using Transcriptomine , a tool created by NURSA for mining tissue-specific NR, NR ligand, and coregulator transcriptomes based on published genome wide transcriptional profiling experiments in the field of nuclear receptor signaling. (nursa.org)
  • This results in exponential multiplication of replications of the mutated genes, along with large amounts of genotoxic waste in response to this estrogen metabolism pathway. (wikipedia.org)
  • Cells in other tissues in the body, such as bones and the uterus, also have estrogen receptors. (breastcancer.org)
  • In a paper appearing Jan. 15 in Science, they identify a key player in this pathway as a cell-surface estrogen receptor called GPER1 that is especially abundant in the placenta and fetal tissues. (scienceblog.com)
  • The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. (uniprot.org)
  • In 1958, using a radioactive marker, he showed that only the tissues that respond to estrogen, such as those of the female reproductive tract, were able to concentrate injected estrogen from the blood. (uchicago.edu)
  • In 1967, Jensen and Jack Gorski of the University of Wisconsin showed that these putative receptors were macromolecules that could be extracted from these tissues. (uchicago.edu)
  • Androgen receptors (ARs) are found in a wide variety of tissues, including reproductive organs, central ner. (novusbio.com)
  • Different cells and tissues have shown divergent responses to these two estrogen receptors. (novapublishers.com)
  • ERR-γ is a constitutively active orphan nuclear receptor, and unlike ERR-α and -β, it is selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal muscles, as well as in a variety of tumors with hypermetabolic demand and abundant vasculature. (ahajournals.org)
  • By 1968, Jensen had devised a reliable test for the presence of estrogen receptors in breast cancer cells. (uchicago.edu)
  • In addition, the presence of estrogen receptor levels in acne patients indicates a possible therapy by anti-estrogens or estrogens. (unboundmedicine.com)
  • Estrogen Receptors (ER) are members of the steroid/thyroid hormone receptor superfamily of nuclear receptors. (thermofisher.com)
  • In many of these diseases, estrogen mediates its effects through the estrogen receptor (ER), which serves as the basis for many therapeutic interventions. (jci.org)
  • However, advances in radioisotope chemistry and detection techniques for tritium, facilitated the identification of a receptor protein that mediates the diverse actions of estrogen without metabolic alteration of the hormone itself. (aacrjournals.org)
  • Briefly, estrogen mediates its multiple functions in the brain through two well-characterized receptors: ERá and ERâ. (novapublishers.com)
  • Estrogen mediates their effects through two receptors, estrogen receptors (ERs) ERα and ERβ, which are members of the nuclear receptor super family ( 3 ). (frontiersin.org)
  • This receptor was regarded as the only ER that mediates estrogenic effects, until a second ER, now known as ER beta, was cloned from rat prostate. (atlasgeneticsoncology.org)
  • This study focuses on the effects of pure glyphosate on estrogen receptors (ERs) mediated transcriptional activity and their expressions. (nih.gov)
  • The eukaryotic nuclear receptors (NRs) super-family of transcriptional factors include the estrogen-related receptors (ERRs) that have diverse roles in control of cellular energy balance, general metabolism, growth and development, immunity etc. (urotoday.com)
  • The canonical model for ER-mediated regulation of gene expression involves the direct binding of dimeric ER to DNA sequences known as estrogen response elements (EREs), followed by recruitment of a variety of coregulators to alter chromatin structure and facilitate recruitment of the RNA polymerase II (Pol II) transcriptional machinery. (atlasgeneticsoncology.org)
  • Estrogens are powerful modulators of neuronal physiology and in humans may affect a broad range of functions, including reproductive, emotional, and cognitive behaviors. (pnas.org)
  • The question of whether estrogen alternatives such as phytoestrogens and selective estrogen receptor modulators are effective estrogens for the prevention of skin aging in postmenopausal women remains unanswered. (redorbit.com)
  • We describe an approach to classify estrogen receptor (ER) modulators based on dynamics of the receptor-ligand complex as probed with hydrogen/deuterium exchange (HDX) mass spectrometry. (rcsb.org)
  • We demonstrate that analysis of dynamics of the receptor-ligand complex facilitates binning of ER modulators into distinct groups based on structural dynamics. (rcsb.org)
  • In summary, HDX provides a sensitive and rapid approach to classify modulators of the estrogen receptor that correlates with their pharmacological profile. (rcsb.org)
  • ER which is a member of the nuclear hormone family of intracellular receptors and the estrogen G protein coupled receptor GPR30 (GPER), which is a G-protein coupled receptor. (phys.org)
  • Two classes of ER exist: nuclear estrogen receptors (ERα and ERβ), which are members of the nuclear receptor family of intracellular receptors, and membrane estrogen receptors (mERs) (GPER (GPR30), ER-X, and Gq-mER), which are mostly G protein-coupled receptors. (wikipedia.org)
  • however, the role of estrogen receptors in this response has not yet been clarified. (ahajournals.org)
  • Furthermore, the role of estrogen and its receptors are explained in the context of aging. (novapublishers.com)
  • Estrogen regulation of apoptosis: how can one hormone stimulate and inhibit? (springer.com)
  • Inhibit estrogen effects by competitively binding to the estrogen receptor. (medscape.com)
  • The set-up represents a new assay to screen small molecule drugs designed to therapeutically inhibit estrogen receptor function inside cancer cells. (eurekalert.org)
  • Caffeine and Caffeic Acid Inhibit Growth and Modify Estrogen Receptor and Insulin-like Growth Factor I Receptor Levels in Human Breast Cancer. (greenmedinfo.com)
  • There are two main types of estrogen receptors: estrogen receptor alpha (ERα) also known as NR3B1, and estrogen receptor beta (ER-β) also known as NR3A2. (wikipedia.org)
  • Kao, S.-H. G-Protein Coupled Estrogen Receptor in Breast Cancer. (mdpi.com)
  • Hsu L-H, Chu N-M, Lin Y-F, Kao S-H. G-Protein Coupled Estrogen Receptor in Breast Cancer. (mdpi.com)
  • This study investigated whether the intracellular transmembrane G protein-coupled estrogen receptor (GPER) regulates vascular reactivity in mice. (ahajournals.org)
  • 7 , 9 - 11 Estrogens also bind to the novel, 7-transmembrane spanning intracellular G protein-coupled estrogen receptor (GPER, previously termed GPR30) 8 , 12 cloned from human endothelial cells 13 and expressed throughout the cardiovascular system. (ahajournals.org)
  • G protein-coupled estrogen receptor: A new therapeutic targe. (lww.com)
  • G protein-coupled estrogen receptor A new therapeutic target in stroke and traumatic brain/spinal cord injury? (lww.com)
  • The present book covers estrogen, its receptors and estrogen mediated gene regulation in the brain. (novapublishers.com)
  • Upon binding with estrogen, ER recruits coregulators, which are responsible for tissue specific regulation. (novapublishers.com)
  • Further analysis of the influence of the co-activators on the conformation of ERα/ERβ will define the regulation of receptor conformation in controlling estrogenic function in normal and cancer cells. (aacrjournals.org)
  • For example, raloxifene is classified as a SERM because it (like estrogen) prevents bone loss and lowers serum cholesterol but unlike estrogen, does not stimulate the uterus to grow a lining. (cancer.org)
  • If a SERM is in the estrogen receptor, there is no room for estrogen and it can't attach to the cell. (breastcancer.org)
  • This increase in estrogen can produce gynecomastia, so body builders will usually cycle a SERM after a steroid cycle to ensure that their body is not flooded with excess estrogen. (bionity.com)
  • Furthermore what agent is used (estrogen, SERM, bisphosphonates) may vary over a woman's life time. (medindia.net)
  • Estrogen-related receptor gamma functions as a tumor suppressor in gastric cancer. (nih.gov)
  • In contrast to other estrogen receptor assays, this new technique requires a small sample size (about 5000 cells) and permits the assessment of heterogeneity in estrogen receptor expression among tumor cells. (sciencemag.org)
  • The tumor biopsy I had showed that tumor was highly estrogen receptor positive, so my oncologist told me to avoid soy. (cancer.org)
  • An important receptor for estrogen in ovarian cells has been shown to suppress tumor growth, according to a new study published in the August 15 issue of the journal Cancer Research. (innovations-report.com)
  • The estrogen receptor test (ERT) uses the estrogen receptor (ER) tumor marker that allows for immunohistochemical techniques to be performed for diagnostic purposes. (wikipedia.org)
  • Most of their effects are mediated by two receptors: estrogen receptor (ER)alpha and ERbeta. (nih.gov)
  • In fact, they track how, as resistance develops over time, breast cancer cells gradually lose the alpha receptors while gaining the estrogen-related receptor gamma subtype. (medicalnewstoday.com)
  • provide evidence that interaction of estrogen receptor alpha (Erα) with phosphoinositide 3-kinase (PI3K) and the tyrosine kinase Src depends on covalent modification of ERα by arginine methylation. (sciencemag.org)
  • Therapeutic methods of using certain heterocyclic arylidene aryl ether compounds for treating diseases or disorders mediated through modulation of estrogen related receptor alpha are described. (freepatentsonline.com)
  • Vitamin C and alpha-naphthoflavone prevent estrogen-induced mammary tumors and decrease oxidative stress in female rats. (greenmedinfo.com)
  • Synthetic peptide within Human Estrogen Receptor alpha conjugated to keyhole limpet haemocyanin. (abcam.com)
  • Your search returned 209 Estrogen Receptor 1 (alpha) ELISA ELISA Kit across 10 suppliers. (biocompare.com)
  • Estrogen Receptor alpha is a 65 kDa protein and a member of the steroid family of nuclear receptors. (novusbio.com)
  • There are two classic estrogen receptors: alpha and beta. (novapublishers.com)
  • Recognizes a protein of 67 kDa, which is identified as estrogen receptor (ER) alpha. (fishersci.com)
  • Cellular signaling of estrogen is mediated through two estrogen receptors (ERs), ER alpha and ER beta. (atlasgeneticsoncology.org)
  • MA1-310 detects both the steroid occupied and unoccupied forms of the estrogen receptor (ER) alpha from human samples. (thermofisher.com)
  • Test results are frequently referred to as the hormone receptor status. (medlineplus.gov)
  • If your hormone receptor status shows you have one or both of these receptors on your cancer cells, you may respond well to certain types of treatments. (medlineplus.gov)
  • Knowing your hormone receptor status will help your health care provider decide how to treat it. (medlineplus.gov)
  • This gene encodes a member of the estrogen receptor-related receptor (ESRR) family, which belongs to the nuclear hormone receptor superfamil. (nih.gov)
  • This article refers to the nuclear hormone receptor ER. (phys.org)
  • Nuclear hormone receptor. (abcam.com)
  • Belongs to the nuclear hormone receptor family. (abcam.com)
  • Dandelion extract up-regulates reproductive hormone receptor expression in mice. (greenmedinfo.com)
  • This hormone-receptor complex then travels to the cell nucleus, where it regulates gene expression. (uchicago.edu)
  • Fulvestrant is a selective estrogen receptor degrader that targets the function of the hormone receptor so, unlike aromatase inhibitors such as anastrozole, it does not interfere with estrogen levels themselves. (indianexpress.com)
  • Epidemiologic studies indicate that dietary factors, such as coffee, may influence breast cancer and modulate hormone receptor status. (greenmedinfo.com)
  • Today, ER analysis is one of many routinely performed immunohistochemical assays performed to classify the hormone receptor status and to serve as a means of insight in the determination of cancer prognosis and management. (wikipedia.org)
  • In an effort to broaden the treatment options available to postmenopausal women, research efforts have been directed at the development of compounds that maintain the vasomotor, skeletal and cardiovascular benefits of estrogen replacement therapy but have little to no significant adverse effect on reproductive organs and the clotting processes. (aafp.org)
  • With the correlation noted between skin collagen decline and postmenopausal years, studies have attempted to decipher the effects of estrogens on skin collagen. (redorbit.com)
  • Women are believed to be protected from non-alcoholic fatty liver disease (NAFLD) by estrogen, so postmenopausal women with lower estrogen levels have an increased chance of developing the disease. (rainbow.coop)
  • Formulations of postmenopausal hormone replacement therapy (HRT) that include estrogen plus progesterone increase mammographic density ( 5 -7 ). (aacrjournals.org)
  • One small, previous study found significant improvements in verbal memory in postmenopausal women with schizophrenia treated with estrogen replacement. (psychiatrictimes.com)
  • Raloxifene is a selective estrogen receptor modulator approved for the treatment of osteoporosis in postmenopausal women and for breast cancer in women. (psychiatrictimes.com)
  • So breast cell estrogen receptors are different from bone cell estrogen receptors and both of those estrogen receptors are different from uterine estrogen receptors. (breastcancer.org)
  • Competition of FE for binding sites is observed with estrogens, but not with progestins, androgens, or glucocorticosteroids, indicating the specificity of FE binding. (sciencemag.org)
  • The identification of the estrogen receptor (ER) in the laboratory provided a mechanism to describe the target site specificity of estrogen action in uterus, vagina, pituitary gland, and breast cancer. (aacrjournals.org)
  • The laboratory question then became, "how do estrogens exert their tissue specificity, and is there a target that can be identified to block estrogen action? (aacrjournals.org)
  • Androgen Receptor: What Makes a Man? (novusbio.com)
  • We hypothesized that a selected subset of chemicals used in natural gas drilling operations and also surface and ground water samples collected in a drilling-dense region of Garfield County, Colorado, would exhibit estrogen and androgen receptor activities. (wellnessresources.com)
  • Water samples were collected, solid-phase extracted, and measured for estrogen and androgen receptor activities using reporter gene assays in human cell lines. (wellnessresources.com)
  • Estrogen and androgen receptor activities of hydraulic fracturing chemicals and surface and ground water in a drilling-dense region. (wellnessresources.com)
  • Specific estrogen and androgen receptor levels were assayed under conditions resulting in the estimation of unoccupied receptor levels, and the charcoal technique was utilized. (unboundmedicine.com)
  • On the other hand, 31 and 48%, respectively, of the male and female acne patients were androgen receptor-positive, and their receptor levels were between 35 and 213 fmol/mg cytosol protein. (unboundmedicine.com)
  • A correlation of r = 0.71 between estrogen and androgen receptor levels was noted in the female subjects, but no correlation was found in the male subjects. (unboundmedicine.com)
  • A correlation between testosterone serum levels and androgen receptor levels of r = 0.77 and r = 0.66, respectively, was noted in the female and male acne patients. (unboundmedicine.com)
  • The results of the present investigation suggest that androgen receptor levels play an important role in acne patients with normal testosterone serum levels. (unboundmedicine.com)
  • See also aromatase inhibitors , estrogen , uterus . (cancer.org)
  • 4 The risk of endometrial cancer is also increased in women with an intact uterus who take unopposed estrogen for long periods. (aafp.org)
  • However, the recognition of selective ER modulation, i.e. , estrogen-like action in bones and lowering circulating cholesterol but antiestrogenic actions in breast and uterus, has resulted in the development of multifunctional medicines with the goal of preventing not only breast and uterine cancer but also osteoporosis and coronary heart disease. (aacrjournals.org)
  • The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation. (freepatentsonline.com)
  • Raloxifene is a selective estrogen receptor modulator that produces both estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue. (aafp.org)
  • Silymarin exhibits antiosteoporotic and selective estrogen receptor modulator activity in ovariectomized rats. (greenmedinfo.com)
  • It is a selective estrogen receptor modulator. (selleckchem.com)
  • Treatment with a selective estrogen receptor modulator in adjunct to antipsychotics was associated with improvements in attention and memory in men and women with schizophrenia in a recent trial. (psychiatrictimes.com)
  • Benzophenone-3 (oxybenzone) and benzophenone-2 are structurally related to steroid receptor ligands and may act as endocrine disruptor. (greenmedinfo.com)
  • We present the structure-based optimization of a series of estrogen receptor-beta (ERbeta) selective ligands. (rcsb.org)
  • This effect of estrogens likely contributes to the greater proficiency of women's pDCs than men's as regards the production of type I IFNs elicited by TLR7 ligands. (frontiersin.org)
  • In addition, the different estrogen receptor combinations may respond differently to various ligands, which may translate into tissue selective agonistic and antagonistic effects. (wikipedia.org)
  • Our results provide insights into the folding/unfolding of ERα and ERβ and the conformational transitions of these receptors under the influence of ligands such as E 2 and the ERE. (aacrjournals.org)
  • Estrogen receptor (ER)3 gene expression in breast epithelium is an intricately regulated event. (nih.gov)
  • 10 Activation of the estrogen receptor by these compounds may involve multiple molecular pathways that may result in gene expression of ligand-, tissue- and/or gene-specific receptors. (aafp.org)
  • We investigated the estrogenic activities of isoflavone derivatives in competition binding assays with human estrogen receptor (hER) α or hER β protein, and in a gene expression assay using a yeast system. (go.jp)
  • We found that chronic GPER deficiency is associated with increased endothelial prostanoid-mediated vasoconstriction but has no effect on endothelial nitric oxide bioactivity, gene expression of endothelial nitric oxide synthase and thromboxane prostanoid (TP) receptor, or vascular structure. (ahajournals.org)
  • Endogenous estrogens mediate protective effects in the cardiovascular system, affecting both endothelium-dependent and endothelium-independent mechanisms. (ahajournals.org)
  • Endogenous and exogenous estrogen exposure increases the risk of estrogen receptor (ER)-positive breast cancer. (aacrjournals.org)
  • Nevertheless, continuing efforts in the study of estrogen receptors have helped us to define their roles in diseases and to develop novel therapies against these disorders. (novapublishers.com)
  • Sichun Yang, Ph.D., assistant professor at Case Western Reserve University, is working to understand the signaling mechanisms of two critical domains in estrogen receptors, using computer modeling resources at OSC. (osc.edu)
  • In conclusion our data could provide new insights as concerns the estrogen-related mechanisms of immune system modulation. (nih.gov)
  • Little is known, however, about either the mechanisms or sites of estrogen actions in these modulatory processes, or the neurotransmitter systems involved in these regulations. (pnas.org)
  • They suspect the receptor triggers other downstream mechanisms that come into play. (scienceblog.com)
  • A better understanding of the GPER, its role in breast cancer, and the interactions with the ER and epidermal growth factor receptor will be beneficial for the disease management and prevention in the future. (mdpi.com)
  • GPER deletion also increases TP receptor-mediated contraction. (ahajournals.org)
  • In conclusion, this study identifies GPER as the first estrogen receptor with inhibitory activity on endothelium-dependent contractility. (ahajournals.org)
  • 15 - 19 Moreover, G-1-dependent relaxation is absent in GPER knockout (GPER 0 ) mice, further corroborating the requirement of this receptor to mediate vascular responses. (ahajournals.org)
  • In this review, we discuss and summarize the in vitro and in vivo effects of certain phytoestrogens and their potential roles in the interaction with estrogen receptors. (mdpi.com)
  • He had seen that Faslodex in a 500 mL dose not only improved progression free survival for estrogen receptor positive metastatic breast cancer, but also improved overall survival. (sharecancersupport.org)
  • Activation of this pathway may confer some of the CNS-mediated benefits of estrogen without the feminizing side effects and may offer a new therapeutic approach for diseases with cognitive deficits such as Alzheimer's disease and schizophrenia," they write. (alzforum.org)
  • The schematic below models the activity pathway of the estrogen receptor. (wikipedia.org)
  • Estrogen receptor/progesterone receptor (ER/PR) tests are used to help guide breast cancer treatment. (medlineplus.gov)
  • ER/PR tests look for receptors that attach to the hormones estrogen and progesterone in a sample of breast cancer tissue. (medlineplus.gov)
  • ER/PR tests will show whether there are ER and/or PR receptors on your breast cancer cells. (medlineplus.gov)
  • Estrogen sends signals through the receptors that tell breast cancer cells to grow. (breastcancer.org)
  • A critical first step oncologists must take after finding a patient has breast cancer is to look for overexpressed hormone receptors in the cancer cells. (osc.edu)
  • While it is well known that point mutations of hormone receptors are associated with several types of cancer, still elusive is a mechanistic understanding of how these receptors function at the molecular level. (osc.edu)
  • To treat ER-positive breast cancer, doctors use hormone therapy to block estrogen from binding to receptors in the cancer cells, reducing their chance of survival and proliferation. (osc.edu)
  • Expected for release later this year, the 2019 "Estrogen and Progesterone Receptor Testing in Breast Cancer: American Society of Clinical Oncology / College of American Pathologists Clinical Practice Guideline Update" will include reaffirmations and updated recommendations. (cap.org)
  • Does breast cancer run along some continuum from estrogen-receptor positive to estrogen-receptor negative tumors? (oncolink.org)
  • If you have an ER- cancer: strategies to increase or decrease estrogen levels will have no bearing on your recurrence risk. (oncolink.org)
  • One is a clearer understanding of the importance of the gamma estrogen-related receptor in breast cancer. (medicalnewstoday.com)
  • Until now, this receptor has not been viewed to be of much importance in any type of breast cancer," Riggins says. (medicalnewstoday.com)
  • All that was known is that there were more of these receptors in breast cancer than in normal breast tissue, we hadn't gone much further than that. (medicalnewstoday.com)
  • Atmospheric particulate matter and breast cancer survival: estrogen receptor triggered? (springer.com)
  • Breast cancer cells that have a protein (receptor molecule) to which estrogen will attach. (medindia.net)
  • Breast cancer cells that are ER+ need the hormone estrogen to grow and will usually respond to hormone (antiestrogen) therapy that blocks these receptor sites. (medindia.net)
  • Stimulation of c-myc oncogene expression associated with estrogen-induced proliferation of human breast cancer cells. (springer.com)
  • Downstream targets of growth factor and oestrogen signalling and endocrine resistance: the potential roles of c-Myc, cyclin D1 and cyclin E. Endocr Relat Cancer. (springer.com)
  • A recent reanalysis of 90 percent of worldwide observational data on the relationship between hormone replacement therapy and breast cancer showed that the risk of this cancer may be increased in women who are taking estrogen. (aafp.org)
  • Many breast cancer drugs block estrogen receptors inside cancer cells. (eurekalert.org)
  • In Nature Communications , researchers describe a "burning the bridge" strategy to disrupting the estrogen receptor, and how to screen breast cancer drugs designed to do it. (eurekalert.org)
  • Yang, who is also a member of the Case Comprehensive Cancer Center, and colleagues integrated genetic engineering, proteomics, and computer modeling to reveal the full estrogen receptor structure. (eurekalert.org)
  • I talked to my onco last week and asked him the type of cancer cells I had in regard to estrogen reception. (cancer.org)
  • To understand how the loss of ER beta affected the ovarian cells during cancer progression, the gene for ER beta was replaced in ovarian cancer cell lines that no longer expressed the estrogen-triggered nuclear receptor. (innovations-report.com)
  • The ER beta reintroduced into the cancer cell lines did not share the classic functions attributed to estrogen receptors, including induction of progesterone receptor expression and fibuline-1C, and it s ability to decrease the expression of the cyclin D1 gene was completely opposite of it s counterpart, ER beta. (innovations-report.com)
  • Glyphosate exerted proliferative effects only in human hormone-dependent breast cancer, T47D cells, but not in hormone-independent breast cancer, MDA-MB231 cells, at 10⁻¹² to 10⁻⁶M in estrogen withdrawal condition. (nih.gov)
  • EDITOR-Mayor reports the findings of a postal survey showing an alarming wide variation in rates of oestrogen receptor positivity in women with breast cancer. (bmj.com)
  • How Are Estrogen Receptors Related to Breast Cancer Treatment? (sharecare.com)
  • Video / HealthMakers / Robert Clarke, PhD, DSc / How Are Estrogen Receptors Related to Breast Cancer Treatment? (sharecare.com)
  • In this video, HealthMaker and oncology professor Robert Clarke, PhD, DSc, explains how estrogen receptors can affect a woman's breast cancer treatment. (sharecare.com)
  • How Is Estrogen-Receptor-Positive Breast Cancer Treated? (sharecare.com)
  • The purpose of this translational study was to investigate how coffee may affect breast cancer growth in relation to estrogen receptor-α (ER) status. (greenmedinfo.com)
  • Background: The density of breast tissue on a mammogram is a strong predictor of breast cancer risk and may reflect cumulative estrogen effect on breast tissue. (aacrjournals.org)
  • The association between mammographic density and breast cancer may be due to factors besides estrogen exposure. (aacrjournals.org)
  • Thus, high mammographic density may be associated with breast cancer because it is a marker of estrogen effects on breast tissue ( 11 ). (aacrjournals.org)
  • High expression of soluble CD155 in estrogen receptor-negative breast cancer. (medworm.com)
  • New research has shown for the first time that it is safe for women who have been diagnosed with oestrogen receptor positive breast cancer to become pregnant, despite doctors' previous fears that pregnancy could boost levels of oestrogen in the body and cause the cancer to return. (health.am)
  • Breast cancer s that are estrogen-receptor-positive (ER-positive) are those that have estrogen receptors present on many of the cancer cells. (health.am)
  • Finding out that your breast cancer cells do have estrogen receptors can be useful in determining an effective course of treatment. (health.am)
  • Estrogens can have profound effects on prostate growth and differentiation as well as in the pathogenesis of prostate cancer. (atlasgeneticsoncology.org)
  • Estrogen receptors are involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. (thermofisher.com)
  • The next step of a drug discovery project is to identify environmental substances that may have an effect in humans similar to an effect produced by a naturally occurring estrogen. (osc.edu)
  • ERDs sit in the estrogen receptors in breast cells. (breastcancer.org)
  • Cells with estrogen receptors grow and multiply when estrogen attaches to the receptors. (breastcancer.org)
  • Researchers have engineered new sensors that fluoresce in the presence of compounds that interact with estrogen receptors in human cells. (phys.org)
  • The cells were then treated with quercetin, estrogen, or an estrogen receptor (ER) antagonist (which was also administered in the presence of quercetin or estrogen) for 7 or 21 days. (hindawi.com)
  • The in vitro model of GM-CSF-induced DC differentiation shows that CD11c + CD11b int Ly6c neg cells depend on ERα activation by estrogen for their development, and for the acquisition of competence to activate naive CD4 + T lymphocytes and mount a robust pro-inflammatory cytokine response to CD40 stimulation. (frontiersin.org)
  • In this model, estrogen signaling in conjunction with GM-CSF is necessary to promote early interferon regulatory factor ( Irf ) -4 expression in macrophage-DC progenitors and their subsequent differentiation into IRF-4 hi CD11c + CD11b int Ly6c neg cells, closely related to the cDC2 subset. (frontiersin.org)
  • Many studies have shown that mature cells both from the innate and the adaptive immune system express ERs, particularly ERα in mouse ( 4 - 10 ) suggesting that estrogens could regulate their effector functions. (frontiersin.org)
  • Caffeine also reducedthe insulin-like growth factor-I receptor (IGFIR) and pAkt levels in both ER(+) and ER(-) cells. (greenmedinfo.com)
  • This receptor has been directly implicated in pathological depression and anxiety ( 24 , 25 ) and thus provides another possible mechanism of estrogen action in the amygdala. (pnas.org)
  • Further, it explains the mechanism of estrogen action and dysfunction leading to diseases. (novapublishers.com)
  • They also report that ERβ-selective compounds developed at Wyeth (WAY-200070 and WAY-202779) mimic the effect of estrogen on the hippocampus in ways that the ERα agonist PPT (4,4',4''-[4-propyl-(1H)-pyrazole-1,3,5-triyl]trisphenol) does not. (alzforum.org)
  • For example, when given to ovariectomized animals, the Wyeth compounds cause nuclear estrogen receptor levels in the hippocampus to rise-this indicates receptor activation. (alzforum.org)
  • Airborne particulate collected from central Taiwan induces DNA strand breaks, Poly(ADP-ribose) polymerase-1 activation, and estrogen-disrupting activity in human breast carcinoma cell lines. (springer.com)