Receptors estrogen. Medical search

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)

Estrogen receptors also occur within the cell nucleus, and both estrogen receptor subtypes have a DNA-binding domain and can ... As hormone receptors for sex steroids (steroid hormone receptors), ERs, androgen receptors (ARs), and progesterone receptors ( ... nuclear estrogen receptors (ERα and ERβ), which are members of the nuclear receptor family of intracellular receptors, and ... "Identification of a third distinct estrogen receptor and reclassification of estrogen receptors in teleosts". Proceedings of ...

https://en.wikipedia.org/wiki/Estrogen_receptor

There are two main types of estrogen receptors: estrogen receptor alpha (ERα) also known as NR3B1, and estrogen receptor beta ( ... In the typical estrogen pathway (i) estrogen or other selective estrogen receptor modulators (SERMs) are bound to the estrogen ... The estrogen receptor test (ERT) uses the estrogen receptor (ER) tumor marker that allows for immunohistochemical techniques to ... Both of these are nuclear receptors activated by the sex hormone, estrogen, and encoded by the ESR1 (Estrogen Receptor 1) gene ...

https://en.wikipedia.org/wiki/Estrogen_receptor_test

"Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists". ... nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor-a nuclear receptor which is ... "Human estrogen receptor beta binds DNA in a manner similar to and dimerizes with estrogen receptor alpha". The Journal of ... "Estrogen receptor-beta agonist diarylpropionitrile counteracts the estrogenic activity of estrogen receptor-alpha agonist ...

https://en.wikipedia.org/wiki/Estrogen_receptor_beta

ERRalpha+estrogen-related+receptor at the US National Library of Medicine Medical Subject Headings (MeSH) estrogen+receptor- ... They are named because of sequence homology with estrogen receptors, but do not appear to bind estrogens or other tested ... Sladek R, Bader JA, Giguère V (September 1997). "The orphan nuclear receptor estrogen-related receptor alpha is a ... "Orphan nuclear receptor estrogen-related receptor alpha is essential for adaptive thermogenesis". Proceedings of the National ...

https://en.wikipedia.org/wiki/Estrogen-related_receptor

In humans, ERα is encoded by the gene ESR1 (EStrogen Receptor 1). The estrogen receptor (ER) is a ligand-activated ... April 2004). "ERBP, a novel estrogen receptor binding protein enhancing the activity of estrogen receptor". Biochemical and ... Curtis Hewitt S, Couse JF, Korach KS (2000). "Estrogen receptor transcription and transactivation: Estrogen receptor knockout ... nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor (mainly ...

https://en.wikipedia.org/wiki/Estrogen_receptor_alpha

Membrane estrogen receptors (mERs) are a group of receptors which bind estrogen. Unlike the estrogen receptor (ER), a nuclear ... Membrane steroid receptor Soltysik K, Czekaj P (April 2013). "Membrane estrogen receptors - is it an alternative way of ... Micevych PE, Kelly MJ (2012). "Membrane estrogen receptor regulation of hypothalamic function". Neuroendocrinology. 96 (2): 103 ... v t e (G protein-coupled receptors, Human proteins, Human female endocrine system, All stub articles, Receptor stubs). ...

https://en.wikipedia.org/wiki/Membrane_estrogen_receptor

"Estrogen-related receptor-gamma and peroxisome proliferator-activated receptor-gamma coactivator-1alpha regulate estrogen- ... a third member of the estrogen receptor-related receptor (ERR) subfamily of orphan nuclear receptors: tissue-specific isoforms ... Estrogen-related receptor gamma (ERR-gamma), also known as NR3B3 (nuclear receptor subfamily 3, group B, member 3), is a ... Gao M, Sun P, Wang J, Zhao D, Wei L (2006). "Expression of estrogen receptor-related receptor isoforms and clinical ...

https://en.wikipedia.org/wiki/Estrogen-related_receptor_gamma

A selective estrogen receptor degrader or downregulator (SERD) is a type of drug which binds to the estrogen receptor (ER) and ... They are used to treat estrogen receptor-sensitive or progesterone receptor-sensitive breast cancer, along with older classes ... "Rintodestrant , oral selective estrogen receptor degrader (SERD) , G1 Therapeutics, Inc". www.g1therapeutics.com. Retrieved ... v t e (Selective estrogen receptor degraders, Antiestrogens, Hormonal antineoplastic drugs, All stub articles, Genito-urinary ...

https://en.wikipedia.org/wiki/Selective_estrogen_receptor_degrader

August 2004). "Differential and opposing regulation of PAI-1 promoter activity by estrogen receptor alpha and estrogen receptor ... Estrogen-related receptor beta (ERR-β), also known as ESRRB or NR3B2 (nuclear receptor subfamily 3, group B, member 2), is a ... March 2005). "Expression and functional study of estrogen receptor-related receptors in human prostatic cells and tissues". The ... "Transcriptional profiling of estrogen-regulated gene expression via estrogen receptor (ER) alpha or ERbeta in human ...

https://en.wikipedia.org/wiki/Estrogen-related_receptor_beta

... estrogen receptor modulators Selective androgen receptor modulator Selective estrogen receptor degrader Selective receptor ... Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs), are a class of ... Feng Q, O'Malley BW (Nov 2014). "Nuclear receptor modulation--role of coregulators in selective estrogen receptor modulator ( ... Pickar JH, Komm BS (Sep 2015). "Selective estrogen receptor modulators and the combination therapy conjugated estrogens/ ...

https://en.wikipedia.org/wiki/Selective_estrogen_receptor_modulator

"Transcriptional targets shared by estrogen receptor- related receptors (ERRs) and estrogen receptor (ER) alpha, but not by ... Estrogen receptor alpha (ERα) and estrogen-related receptor alpha (ERRα) have been found to regulate many of the same genes. ... Estrogen Related Receptor Alpha) gene. ERRα was originally cloned by DNA sequence homology to the estrogen receptor alpha (ERα ... "Transcriptional activities of the orphan nuclear receptor ERR alpha (estrogen receptor-related receptor-alpha)". Molecular ...

https://en.wikipedia.org/wiki/Estrogen-related_receptor_alpha

This is a list of selective estrogen receptor modulators (SERMs). SERMs that have been approved for medical use include ... ISBN 978-94-011-4439-1. Taylor, Hugh S. (2009). "Designing the ideal selective estrogen receptor modulator-an achievable goal ... to be a SERM due to its structural similarity to tamoxifen but it was subsequently found not to bind to the estrogen receptor ( ... Selective estrogen receptor modulators, Biology-related lists). ...

https://en.wikipedia.org/wiki/List_of_selective_estrogen_receptor_modulators

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- ...

https://en.wikipedia.org/wiki/Bevacizumab

... or G-Protein-Coupled Estrogen Receptor (GPER)". Estrogen Receptors. Methods in Molecular Biology. Vol. 1366. pp. 11-7. doi: ... 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 ...

https://en.wikipedia.org/wiki/2-Methoxyestradiol

Nuclear receptors Subfamily 3: Estrogen Receptor-like Group A: Estrogen receptor (Sex hormones: Estrogen) 1: Estrogen receptor- ... Estrogen receptor-β (ERβ; NR3A2, ESR2) Group C: 3-Ketosteroid receptors 1: Glucocorticoid receptor (GR; NR3C1) (Cortisol) 2: ... GPR30 binds estrogen, and upon binding estrogen this pathway activates adenylyl cyclase and epidermal growth factor receptor. ... G Protein-Coupled Receptor 30 (GPR30) binds estrogen, Membrane Progestin Receptor (mPR) binds progesterone, G Protein-Coupled ...

https://en.wikipedia.org/wiki/Steroid_hormone_receptor

Estrogen upregulates FSH receptor sites. In turn, FSH stimulates granulosa cells to produce estrogens. This synergistic ... The follicle-stimulating hormone receptor or FSH receptor (FSHR) is a transmembrane receptor that interacts with the follicle- ... The longer the receptor remains active, the more kinases are activated, the more receptors are phosphorylated.[citation needed ... "Glycoprotein Hormone Receptors: FSH". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...

https://en.wikipedia.org/wiki/Follicle-stimulating_hormone_receptor

The cells express estrogen/progesterone-receptors. Undifferentiated uterine sarcoma, or undifferentiated (high-grade) ...

https://en.wikipedia.org/wiki/Endometrial_stromal_sarcoma

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 ...

https://en.wikipedia.org/wiki/Atya_Kapley

... women tend to have better prognosis due to the presence of estrogen receptor beta. However, this is a continued study that may ... "Estrogen Receptors and Melanoma: A Review". Cells. 8 (11): 1463. doi:10.3390/cells8111463. PMC 6912660. PMID 31752344. Seely, ... In cutaneous melanoma, estrogen was evaluated to determine its effect on a steroid hormone-sensitive cancer. While no ... It is hypothesized that this may be due to the protective effects of estrogens and the harmful effects of testosterone on the ...

https://en.wikipedia.org/wiki/Health_survival_paradox

Estrogens are agonists of the estrogen receptors, the biological targets of endogenous estrogens like estradiol. They have ... Estrogens act as selective agonists of the estrogen receptors (ERs), the ERα and the ERβ. They may also bind to and activate ... Stone JC, Clark J, Cuneo R, Russell AW, Doi SA (June 2014). "Estrogen and selective estrogen receptor modulators (SERMs) for ... Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ...

https://en.wikipedia.org/wiki/Estrogen_(medication)

"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". ...

https://en.wikipedia.org/wiki/Raloxifene

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 ... Selective estrogen receptor modulators, Synthetic estrogens, Triphenylethylenes, Bis(4-hydroxyphenyl)methanes). ...

https://en.wikipedia.org/wiki/Chlorotrianisene

... estrogen enters passively into the cell where it binds to and activates the estrogen receptor. The estrogen:ER complex binds to ... The actions of estrogen are mediated by the estrogen receptor (ER), a dimeric nuclear protein that binds to DNA and controls ... Additionally, estrogens bind to and activate rapid-signaling membrane estrogen receptors (mERs), such as GPER (GPR30). In ... Note that in males, estrogen is also produced by the Sertoli cells when FSH binds to their FSH receptors. Estrogens are plasma ...

https://en.wikipedia.org/wiki/Estrogen

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, ...

https://en.wikipedia.org/wiki/Endometrial_cancer

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 ... Estrogens, Ketones, World Anti-Doping Agency prohibited substances). ...

https://en.wikipedia.org/wiki/7α-Hydroxy-DHEA

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- ...

https://en.wikipedia.org/wiki/Androstenedione

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 ...

https://en.wikipedia.org/wiki/7β-Hydroxy-DHEA

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 ...

https://en.wikipedia.org/wiki/Antiestrogen_withdrawal_response

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 ...

https://en.wikipedia.org/wiki/Primary_transcript

"DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ...

https://en.wikipedia.org/wiki/16α-Hydroxy-DHEA

... the estrogen receptor modulator drug, tamoxifen, or various aromatase inhibitors of the estrogen receptor) has been used as the ... strongly express the estrogen receptor in most cases and that PDCIS with tumor cells that do not express the estrogen receptor ... expressed the estrogen receptor, progesterone receptor, and HER2/neu protein. More resent reports find that these tumor cells ... do not express estrogen receptors, progesterone receptors, or HER2/neu protein. Gene analyses studies have reported that EPS ...

https://en.wikipedia.org/wiki/Papillary_carcinomas_of_the_breast

... androgen receptor modulator N-Terminal domain antiandrogen Discovery and development of antiandrogens Nonsteroidal estrogen ... They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... Cimetidine (Tagamet): An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR ... Gao W, Kim J, Dalton JT (2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharm. Res. ...

https://en.wikipedia.org/wiki/Nonsteroidal_antiandrogen

Stress can also result in inheritable changes DNA methylation in the promoter regions of the estrogen receptor alpha (ERα), ... Epigenetic modifications as a result of absent maternal care lead to decreased estrogen receptor alpha expression, due to ... glucocorticoid receptor (GR), and mineralocorticoid receptor (MR). These changes lead to altered expression of these genes in ... Such HPA axis modifications lead to decreased anxiety-like behavior in adulthood and increased glucocorticoid receptor levels ...

https://en.wikipedia.org/wiki/Transgenerational_stress_inheritance

Estrogen can cause an increase of cortisol-binding globulin and thereby cause the total cortisol level to be elevated. However ... This atrophy is associated with areas of high glucocorticoid receptor concentrations such as the hippocampus and correlates ... Elevated levels of total cortisol can also be due to estrogen found in oral contraceptive pills that contain a mixture of ... can act on the melanocortin 1 receptor. A variant of Cushing's disease can be caused by ectopic, i.e. extra pituitary, ACTH ...

https://en.wikipedia.org/wiki/Cushing's_syndrome

Reduced estrogen levels in the endometrium are responsible for the efficacy of elagolix in the treatment of endometriosis. ... Elagolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor (GnRHR), the biological target ... An efficacy and safety study of elagolix in combination with add-back estradiol, an estrogen, and norethisterone acetate, a ... Combined birth control is not contraindicated with elagolix, but because of the estrogen component, is expected to decrease the ...

https://en.wikipedia.org/wiki/Elagolix

Selective receptor modulator Selective estrogen receptor modulator Selective progesterone receptor modulator Selective ... There has been extensive research on selective estrogen receptor modulators (SERMs) such as tamoxifen, which is used to treat ... Selective Androgen Receptor Modulators or SARMs are a class of androgen receptor ligands that maintain some of the desirable ... Kearbey JD, Gao W, Narayanan R, Fisher SJ, Wu D, Miller DD, Dalton JT (February 2007). "Selective Androgen Receptor Modulator ( ...

https://en.wikipedia.org/wiki/Selective_androgen_receptor_modulator

These effects may be mediated by the defective functioning of estrogen via the estrogen receptor, which contains a zinc finger ...

https://en.wikipedia.org/wiki/Zinc_deficiency

October 2003). "Evaluation of an estrogen receptor-beta agonist in animal models of human disease". Endocrinology. 144 (10): ... Harris HA (2006). "Preclinical characterization of selective estrogen receptor beta agonists: new insights into their ... and highly selective agonist of the ERβ subtype of the estrogen receptor. It is used in scientific research to elucidate the ... "Reflections on the discovery and significance of estrogen receptor beta". Endocrine Reviews. 26 (3): 465-78. doi:10.1210/er. ...

https://en.wikipedia.org/wiki/Prinaberel

"Estrogen receptor-positive mammary tumorigenesis in TGFalpha transgenic mice progresses with progesterone receptor loss". ... Description of LDL receptor pathway at the Brown - Goldstein Laboratory webpage LDL+Receptor at the US National Library of ... This precludes the movement of the receptor from the ER to the Golgi, and leads to degradation of the receptor protein. Class 3 ... There are 5 broad classes of mutation of the LDL receptor: Class 1 mutations affect the synthesis of the receptor in the ...

https://en.wikipedia.org/wiki/LDL_receptor

Estrogens were discovered in 1929, and beginning in 1936, a variety of estradiol esters, such as estradiol benzoate and ... the "Gold Book") (1997). Online corrected version: (2006-) "esters". doi:10.1351/goldbook.E02219 Nuclear Receptor Coregulators ... Although esters of steroidal androgens and estrogens are generally inactive themselves and act as prodrugs, the same is not ... List of progestogen esters Steroid ester Estrogen ester Androgen ester List of steroid esters List of progestogens Fraser, Ian ...

https://en.wikipedia.org/wiki/Progestogen_ester

... of the affinity of estradiol for the estrogen receptor (ER), less than 0.2% of the affinity of dexamethasone for the ... The medication is used alone and is not formulated in combination with an estrogen. It is taken by mouth. Side effects of ... Allylestrenol is a progestogen, or an agonist of the progesterone receptor (PR). It is lacking the keto group at the C3 ... Allylestrenol is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological ...

https://en.wikipedia.org/wiki/Allylestrenol

"Skeletal muscle PGC-1α controls whole-body lactate homeostasis through estrogen-related receptor α-dependent activation of LDH ...

https://en.wikipedia.org/wiki/Chemical_peel

In this way, these modulators can block the body's conversion of testosterone into oestrogen, which is necessary for females.[ ... Meldonium has also been found to induce anticonvulsant and antihypnotic effects involving alpha 2-adrenergic receptors, as well ... oxide production via stimulation of the M3 muscarinic acetylcholine receptor or specific gamma-butyrobetaine ester receptors. ...

https://en.wikipedia.org/wiki/Meldonium

It was used in combination with the estrogen ethinylestradiol. It is taken by mouth. Norgesterone is a progestin, or a ... Norgesterone is a progestogen, and hence is an agonist of the progesterone receptor. Unlike related progestins, it is virtually ... Norgesterone was marketed in combination with ethinylestradiol, an estrogen, as a birth control pill under the brand name ... synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like ...

https://en.wikipedia.org/wiki/Norgesterone

Also, androgens, but not estrogens, increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which ... Again it was noted that AHN was not increase via activation of the estrogen receptors. Androgen regulation decreases the ... Moreover, estrogens had no effect. This research demonstrates how androgens can increase AHN. Researchers also examined how ... Also, androgens are the precursors to estrogens in both men and women. In addition to their role as natural hormones, androgens ...

https://en.wikipedia.org/wiki/Androgen

mu and kappa receptors are associated with aversion behaviors and Mu receptor density is greater in tethered sows than sows ... Estrogen deficiency in male mice Based on findings of changes in OCD symptoms in menstruating women and differences in the ... When compared to the 15 non-compulsive dogs used as a control group, the dogs with CCD were found to have lower receptor ... They used glutamate receptor blockers (memantine) and fluoxetine, commonly known as the antidepressant Prozac, to treat and ...

https://en.wikipedia.org/wiki/Animal_psychopathology

2013). "Assessment of cellular estrogenic activity based on estrogen receptor-mediated reduction of soluble-form catechol-O- ...

https://en.wikipedia.org/wiki/NE-tag

The first approach focuses on the inhibition of estrogen action by antiestrogens, which interact with the estrogen receptors. ... It has been proven that breast cancer in postmenopausal women can be treated or prevented by modulating the estrogen receptors ... A majority of breast cancers are hormone dependent and most of them express either estrogen receptor and/or progesterone ... In postmenopausal women the production of estrogen in the ovaries has ceased. The main source of estrogen is therefore ...

https://en.wikipedia.org/wiki/Steroidal_aromatase_inhibitor

TPE is the parent compound of a group of nonsteroidal estrogen receptor ligands. It includes the estrogens chlorotrianisene, ... Selective estrogen receptor modulators, Synthetic estrogens, Triphenylethylenes, All stub articles, Pharmacology stubs). ... The affinity of triphenylethylene for the rat estrogen receptor is about 0.002% relative to estradiol. For comparison, the ... Wittliff, J. L., Kerr II, D. A., & Andres, S. A. (2005). "Estrogens IV: Estrogen-Like Pharmaceuticals". In Wexler, P. (ed.). ...

https://en.wikipedia.org/wiki/Triphenylethylene

"Allelic variants of aromatase and the androgen and estrogen receptors: toward a multigenic model of prostate cancer risk". Clin ... This protein localizes to the endoplasmic reticulum and catalyzes the last steps of estrogen biosynthesis. Mutations in this ... "Evidence for association of polycystic ovary syndrome in caucasian women with a marker at the insulin receptor gene locus". J. ... gene can result in either increased or decreased aromatase activity; the associated phenotypes suggest that estrogen functions ...

https://en.wikipedia.org/wiki/Cytochrome_p450_family_19_subfamily_a_member_1

"DU-145 and PC-3 human prostate cancer cell lines express androgen receptor: implications for the androgen receptor functions ... Huggins CB, Hodges CV (1941). "Studies on prostate cancer: 1. The effects of castration, of estrogen and androgen injection on ... GnRH receptor agonists, such as leuprorelin and goserelin, were subsequently developed and used to treat prostate cancer. ... The androgen receptor helps cancer cells to survive. Prostate-specific membrane antigen (PSMA) stimulates cancer development by ...

https://en.wikipedia.org/wiki/Prostate_cancer

2009). "Protopanaxadiol and protopanaxatriol bind to glucocorticoid and oestrogen receptors in endothelial cells". British ... binding to the glucocorticoid and oestrogen beta receptors. The study also showed an increase of intracellular calcium ion ...

https://en.wikipedia.org/wiki/Protopanaxadiol

... erbB-2 receptor - erythropoietin - erythropoietin receptor - essential amino acid - ester - estradiol receptor - estrogen ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ... G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ... IgE receptor - IGF type 1 receptor - IGF type 2 receptor - IgG - IgM - immediate-early protein - immune cell - immune system - ...

https://en.wikipedia.org/wiki/Index_of_biochemistry_articles

95-. ISBN 978-3-527-62330-3. Cano A, Calaf i Alsina J, Duenas-Diez JL (22 September 2006). Selective Estrogen Receptor ... Pipendoxifene (INN) (developmental code name ERA-923) is a nonsteroidal selective estrogen receptor modulator (SERM) that was ... Selective estrogen receptor modulators, All stub articles, Antineoplastic and immunomodulating drug stubs). ... ISBN 978-1-60805-496-1. Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. ...

https://en.wikipedia.org/wiki/Pipendoxifene

... such as the androgen receptor, estrogen receptors, glucocorticoid receptor, and progesterone receptor. It has been noted that ... isolated the estrogen receptor 1980s - cloning of the estrogen, glucocorticoid, and thyroid hormone receptors by Pierre Chambon ... "Binding of type II nuclear receptors and estrogen receptor to full and half-site estrogen response elements in vitro". Nucleic ... Conversely, the estrogen receptor found in mollusks is constitutively active and did not bind estrogen-related hormones. Thus, ...

https://en.wikipedia.org/wiki/Nuclear_receptor

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 ...

https://en.wikipedia.org/wiki/Kent_Holtorf

Jiang M, Peng Q, Liu X, Jin J, Hou Z, Zhang J, Mori S, Ross CA, Ye K, Duan W (2013). "Small-molecule TrkB receptor agonists ... In addition, it has been found to inhibit aldehyde dehydrogenase and estrogen sulfotransferase in vitro (Ki = 35 μM and 1-3 μM ... Zeng Y, Wang X, Wang Q, Liu S, Hu X, McClintock SM (2013). "Small molecules activating TrkB receptor for treating a variety of ... It has been found to act as a potent and selective small-molecule agonist of the tropomyosin receptor kinase B (TrkB) (Kd ≈ 320 ...

https://en.wikipedia.org/wiki/Tropoflavin

... mismating shot in diestrus are at risk for more severe disease because estrogen increases the number of progesterone receptors ...

https://en.wikipedia.org/wiki/Pyometra

Incomplete studies on the cellular angiofibroma tentative variant find the presence of estrogen and progesterone receptors on ... Neoplastic cells in mammary and extramammary MMB commonly express the estrogen, progesterone and androgen receptors. ... It has been associated with taking estrogens and, in men, gynecomastia. MFB often develops in tissues derived from embryonic ...

https://en.wikipedia.org/wiki/Mammary-type_myofibroblastoma

Estrogen Receptor Alpha Ligand Binding Domain in Complex with Lasofoxifene ... Estrogen receptor. A, B, C, D. 249. Homo sapiens. Mutation(s): 3 Gene Names: ESR1, ESR, NR3A1. ... Estrogen Receptor Alpha Ligand Binding Domain in Complex with Lasofoxifene. *PDB DOI: 10.2210/pdb6VJD/pdb ...

https://www.rcsb.org/structure/6VJD

Estrogen receptor antagonists. Class Summary. These agents bind to estrogen receptors, preventing stimulating effects of ... Competitively binds to estrogen receptor, producing nuclear complex that decreases DNA synthesis and inhibits estrogen effects ...

https://www.medscape.com/answers/458501-161408/which-medications-in-the-drug-class-immunosuppressives-are-used-in-the-treatment-of-retroperitoneal-fibrosis

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. ...

https://medlineplus.gov/lab-tests/estrogen-receptor-progesterone-receptor-tests/

Estrogen receptor blockers. Class Summary. These agents cause increased hypothalamic secretion of GnRH owing to blockage of ... These agents are ergot derivatives and dopamine receptor agonists. They act on postsynaptic dopamine receptors while causing no ... Semisynthetic ergot alkaloid derivative with strong dopamine D2-receptor agonist and partial dopamine D1-receptor effects. ... Male infertility and variation in CAG repeat length in the androgen receptor gene: a meta-analysis. J Clin Endocrinol Metab. ...

http://emedicine.medscape.com/article/436829-medication

Open access peer-reviewed chapter

https://www.intechopen.com/chapters/22058

Source Reference: Hsu LH, et al "Estrogen, estrogen receptor and lung cancer" Int J Mol Sci 2017;18; DOI:10.3390/ijms18081713. ... Estrogen receptors do play a role in lung cancer. We dont know the specifics yet; were still trying to figure out is it ER-α ... Estrogen Receptors in Lung Ca: Protective, Prognostic, Both?. - ER-alpha, ER-beta, HRT -- exploring the links between hormones ... One of the first papers that came out in 2001 looked at the incidence of the estrogen receptor on lung cancer cells. That led ...

https://www.medpagetoday.com/reading-room/asco/lung-cancer/73207

... α and androgen receptor (AR) degradations via the ubiquitin-proteasome system (UPS) were developed. The designated inducers ... Peptide-based inducers of estrogen receptor (ER) α and androgen receptor (AR) degradations via the ubiquitin-proteasome system ... Design and synthesis of peptide-based chimeric molecules to induce degradation of the estrogen and androgen receptors Bioorg ... to induce ubiquitylation of nuclear receptors that bind to SRC-1. All of the synthesized chimeric E3 ligand-containing ...

https://pubmed.ncbi.nlm.nih.gov/32631565/

A drug that acts like estrogen on some tissues but blocks the effect of estrogen on other tissues. Tamoxifen and raloxifene are ... Retrieved from "http://www.webref.org/wiki/index.php?title=Selective_estrogen_receptor_modulator&oldid=178393" ...

https://www.webref.org/wiki/index.php?title=Selective_estrogen_receptor_modulator

Estrogen-related receptor gamma (human). Find diseases associated with this biological target and compounds tested against it ...

https://pubchem.ncbi.nlm.nih.gov/protein/2GPP_A

A novel mechanism for bile acid induced activation of estrogen receptor β in colorectal cancer. ...

https://www.proquest.com/openview/86efea7aadf396f9120b49bcf4da988c/1?pq-origsite=gscholar&cbl=18750&diss=y

Binding of Estrogen (E) to the Estrogen Receptor-α (ER-α) leads to translocation of the ligand receptor complex to the nucleus ... Epidermal growth factor receptor / HER2 / insulin-like growth factor receptor signalling and oestrogen receptor activity in ... Allred DC, Brown P, Medina D. The origins of estrogen receptor alpha-positive and estrogen receptor alpha-negative human breast ... of breast cancers are Estrogen Receptor alpha (ER-α) positive and are dependent on estrogen for growth. Selective estrogen ...

http://carcinogenesis.com/article/2037/mouse-models-of-estrogen-receptor-positive-breast-cancer-2

31 Studies found for: FULVESTRANT AND Advanced AND Estrogen Receptor AND Exemestane AND Phase 2 AND Exemestane ... FULVESTRANT AND Advanced AND Estrogen Receptor AND Exemestane AND Phase 2 AND Exemestane (31 records) ... FULVESTRANT AND Advanced AND Estrogen Receptor AND Exemestane AND Phase 2 AND Exemestane ...

https://www.clinicaltrials.gov/ct2/results?term=FULVESTRANT+AND+Advanced+AND+Estrogen+Receptor+AND+Exemestane+AND+Phase+2+AND+Exemestane&map=SA

Holding, A. N., Cullen, A. E., & Markowetz, F. (2018). Genome-wide Estrogen Receptor-α activation is sustained, not cyclical.. ... Estrogen Receptor-alpha (ER) drives 75% of breast cancers. Stimulation of the ER by estra-2-diol forms a transcriptionally- ... Humans, Estradiol, Neoplasm Proteins, Estrogen Receptor alpha, Signal Transduction, Gene Expression Regulation, Neoplastic, ... Binding Sites, Base Sequence, Protein Binding, Genome, Human, Female, Receptors, CXCR, Promoter Regions, Genetic, Genome-Wide ...

https://www.repository.cam.ac.uk/handle/1810/287052

... for breast cancer that is sensitive to the female hormone oestrogen (oestrogen receptor ... for breast cancer that is sensitive to the female hormone oestrogen (oestrogen receptor positive breast cancer). It recruited ... A trial of exemestane with or without everolimus for breast cancer that is oestrogen receptor positive and has spread outside ... A trial of exemestane with or without everolimus for breast cancer that is oestrogen receptor positive and has spread outside ...

https://www.cancerresearchuk.org/about-cancer/find-a-clinical-trial/trial-exemestane-with-without-everolimus-breast-cancer-oestrogen-receptor-positive-spread-outside-the-breast

Emergence of Constitutively Active Estrogen Receptor-α Mutations in Pretreated Advanced Estrogen Receptor-Positive Breast ... The nuclear hormone receptor estrogen receptor alpha (ERα) is present in approximately 70% of both early and late stage human ... Zhou, K.; Sun, P.; Zhang, Y.; You, X.; Li, P.; Wang, T. Estrogen stimulated migration and invasion of estrogen receptor- ... More recently, ERα mutations that decrease sensitivity of the receptor to selective estrogen receptor modulators (SERMs) and ...

https://www.mdpi.com/2072-6694/11/4/479

Mouse Monoclonal Estrogen Receptor beta antibody [14C8]. Validated in WB, ICC/IF, IHC-P, IHC-Fr, FACS, Dot, ChIP assay, IHC, ... 644-50 Estrogen receptor beta--an independent prognostic marker in estrogen receptor alpha and progesterone receptor-positive ... Estrogen Receptor beta stained by Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:200.. Antigen Retrieval: ... Estrogen Receptor beta antibody [14C8] detects Estrogen Receptor beta protein at nucleus by immunohistochemical analysis. ...

https://www.genetex.com/Product/Detail/Estrogen-Receptor-beta-antibody-14C8/GTX70174

Oestrogen and progesterone receptor activity in breast cancer in Malaysia. / Yahya, O.; Yaakub, J. A.; Ali, S. A.M. et al. ... Oestrogen and progesterone receptor activity in breast cancer in Malaysia. In: Asian Journal of Surgery. 1991 ; Vol. 14, No. 1 ... Oestrogen and progesterone receptor activity in breast cancer in Malaysia. Asian Journal of Surgery. 1991;14(1):10-12. ... title = "Oestrogen and progesterone receptor activity in breast cancer in Malaysia",. author = "O. Yahya and Yaakub, {J. A.} ...

https://research.monash.edu/en/publications/oestrogen-and-progesterone-receptor-activity-in-breast-cancer-in-

... raloxifene and tamoxifen improve ANP levels and decrease nuclear translocation of NF-kB in estrogen-deficient rats. Download ... Selective estrogen receptor modulator effects in the rat brain.. *Raloxifene and estradiol benzoate both fully restore ... The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and ... The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen improve ANP levels and decrease nuclear ...

https://www.unboundmedicine.com/medline/citation/28591668/The_selective_estrogen_receptor_modulators__SERMs__raloxifene_and_tamoxifen_improve_ANP_levels_and_decrease_nuclear_translocation_of_NF_kB_in_estrogen_deficient_rats_

Estrogen receptor β, there are two different estrogen receptors in man, estrogen receptor α and estrogen receptor β, which are ... Deroo, B.J. and Korach, K.S. (2006) Estrogen Receptors and Human Disease. The Journal of Clinical Investigation, 116, 561-570. ... The two estrogen receptors are expressed in different patterns throughout the human body [69]. ... with the Epstein Bar Virus and Human Cytomegalovirus Frequency and the Expression of Estrogen Receptor-Beta and IL-6 Receptor ...

https://scirp.org/journal/paperinformation.aspx?paperid=84633

"Selective Estrogen Receptor Modulators" by people in this website by year, and whether "Selective Estrogen Receptor Modulators ... A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS ... Bisphenol A Does Not Mimic Estrogen in the Promotion of the In Vitro Response of Murine Dendritic Cells to Toll-Like Receptor ... "Selective Estrogen Receptor Modulators" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, ...

https://profiles.umassmed.edu/display/118540

Overall, Gouania longipetala aqueous extract activates estrogen receptors to induce estrogen activities and exhibit ... Overall, longipetala aqueous extract activates estrogen receptors to induce estrogen activities and exhibit antiestrogenic ... the-arts/psychology/43840/gouania-longipetala-aqueous-extract-exhibits-antiestrogen-activities-and-activate-estrogen-receptors- ... "Gouania Longipetala Aqueous Extract Exhibits Antiestrogen Activities and Activate Estrogen Receptors in Ovariectomized Wistar ...

https://www.edocr.com/v/mebbvq9p/ijtsrdinfo/gouania-longipetala-aqueous-extract-exhibits-antie

Estrogen-triggered nuclear transcription factor, estrogen receptor (ER) is expressed in about 70% of breast cancer. ER mediates ... Discovery at the interface: novel anti-cancer agents targeting human estrogen receptor/S100 interactions. ... Calmodulin antagonists (w7 and melatonin) have been shown to significantly inhibit human estrogen receptor alpha (hERalpha) ... can activate transcription of target genes by directly binding to ER in lieu of estrogen. ...

https://dspace.sunyconnect.suny.edu/handle/1951/72399

... and the estrogen receptors esr1 and esr2 in Atlantic halibut (Hippoglossus hippoglossus). ... and the estrogen receptors esr1 and esr2 in Atlantic halibut (Hippoglossus hippoglossus). ... and the estrogen receptors esr1 and esr2 in Atlantic halibut (Hippoglossus hippoglossus) ...

https://nofima.no/publikasjon/758646/

keywords = "Benzodiazepine receptors, Dopamine receptors, Estrogen, Kainic acid, Striatum",. author = "Hruska, {Robert E.} and ... Abstract: Administration of estrogen to adult male rats increases the density of striatal dopamine receptors. The densities of ... Hruska, Robert E. ; Pitman, Karen T. / Distribution and Localization of Estrogen‐Sensitive Dopamine Receptors in the Rat Brain ... Hruska, R. E., & Pitman, K. T. (1982). Distribution and Localization of Estrogen‐Sensitive Dopamine Receptors in the Rat Brain ...

https://jhu.pure.elsevier.com/en/publications/distribution-and-localization-of-estrogensensitive-dopamine-recep

All phthalates activated the estrogen receptor in vitro.. Figure 3. ER transcription factor assay. Activation of estrogen ... mediated by nuclear receptors such as the estrogen receptor (ER) (17,18). ERs exist in 2 isoforms: ERα (ESR1) and ERβ (ESR2), ... In general, FKBP4 is associated with steroid receptors, altering receptor activity (39). One steroid receptor was downregulated ... Stanniocalcin 2 is an estrogen-responsive gene coexpressed with the estrogen receptor in human breast cancer. Cancer Res. 62: ...

https://www.spandidos-publications.com/10.3892/wasj.2021.92?text=fulltext

Estrogen-like activity of perfluoroalkyl acids in vivo and interaction with human and rainbow trout estrogen receptors in vitro ... Estrogen-like activity of perfluoroalkyl acids in vivo and interaction with human and rainbow trout estrogen receptors in vitro ... Estrogen-like activity of perfluoroalkyl acids in vivo and interaction with human and rainbow trout estrogen receptors in vitro ... Estrogen-like activity of perfluoroalkyl acids in vivo and interaction with human and rainbow trout estrogen receptors in vitro ...

https://agsci.oregonstate.edu/biblio/estrogen-activity-perfluoroalkyl-acids-vivo-and-interaction-human-and-rainbow-trout-estrogen

... of the estrogen receptor is found in the nuclear fraction in the absence of estrogen, and the Kd of the receptor for estradiol ... using the monoclonal antibodies D75P3γ and H222Spγ prepared against the MCF-7 estrogen receptor. The estrogen receptor shows ... We have examined the properties of the estrogen receptor and progesterone receptor in MDA-MB-134 human breast cells and have ... Characterization of Estrogen and Progesterone Receptors and the Dissociated Regulation of Growth and Progesterone Receptor ...

https://aacrjournals.org/cancerres/article/46/3/1124/490554/Characterization-of-Estrogen-and-Progesterone

Estrogen Alfa (ERα) is a receptor used as the main marker to identify the presence of tumors in the breast.compounds Gendarusin ... Cancer receptor protein used in Estrogen Alfa with PDB code 2JF9. Toxicity prediction using the Protox II Online tool. The ... Cytotoxic activity and physicochemical properties of Gendarusin A-E compounds on estrogen alfa receptors (2jf9). Authors: ... Gendarusin A-E compounds had activity against receptors Estrogen Alpha which is shown by the results of RMSD ,2 and Gendarusin ...

https://www.simulations-plus.com/resource/cytotoxic-activity-and-physicochemical-properties-of-gendarusin-a-e-compounds-on-estrogen-alfa-receptors-2jf9/

These data suggest aclivated estrogen receptor specifically modulates Ah receptor-mediated induction of (YP1A1 and may have ... These data suggest aclivated estrogen receptor specifically modulates Ah receptor-mediated induction of (YP1A1 and may have ... These data suggest aclivated estrogen receptor specifically modulates Ah receptor-mediated induction of (YP1A1 and may have ... These data suggest aclivated estrogen receptor specifically modulates Ah receptor-mediated induction of (YP1A1 and may have ...

https://experts.umn.edu/en/publications/estrogen-receptor-specifically-decreases-dioxin-induced-cypia1-in

Selective mutations in estrogen receptor alpha D-domain alters nuclear translocation and non-estrogen response element gene ... Estrogen receptor-alpha mediates the protective effects of estrogen against vascular injury. Circulation research. 2002;90:1087 ... Estrogen exerts their effects through banding and activating estrogen receptors (ERs), and ESR1 is a main mediator effect of ... Association of estrogen receptor α gene Pvu II and Xba I polymorphisms with coronary artery disease. Chinese Journal of ...

https://www.medsci.org/v10p0457.htm

A selective estrogen receptor modulator (SERM) is defined as a substance with dissimilar effects on different tissues: agonist in some and antagonists in others. (bgu.ac.il)
Tamoxifen is a selective estrogen receptor modulator (SERM). (stopbreastcancer.org)
27-OHC is an endogenous selective estrogen receptor modulator. (cdc.gov)
Evidences for antiosteoporotic and selective estrogen receptor modulator activity of silymarin compared with ethinylestradiol in ovariectomized rats. (osteoporosis-studies.com)

The selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen are used for the treatment of osteoporosis and cancer, respectively, in women. (unboundmedicine.com)
Our study demonstrates, for the first time, the additional benefits of raloxifene and tamoxifen in an estrogen-deficient state. (unboundmedicine.com)
Predictors of tamoxifen discontinuation among older women with estrogen receptor-positive breast cancer. (umassmed.edu)
tamoxifen (3%), as expected for estrogen receptor. (aacrjournals.org)
ER beta was shown to enhance MMP-13 expression somewhat more strongly than ER alpha, and the impact of a number of selective ER modulators (tamoxifen, raloxifene, and ICI 182,780) on ER beta enhancement of promoter activity was found to be significantly less than that of estrogen. (eurekamag.com)
Several studies have observed a possible modulatory effect of vitamin D or its analogues on the expression of different hormone receptors in breast cancer and increased sensitivity to tamoxifen. (qualitycounts.com)
As reported in the Journal of Clinical Oncology by Olivia Pagani, MD , and colleagues, 13-year follow-up in a combined analysis of the phase III TEXT and SOFT trials has shown continued disease-free survival and distant recurrence-free interval benefit-but no overall survival benefit-with exemestane plus ovarian function suppression (OFS) vs tamoxifen plus OFS in premenopausal patients with estrogen/progesterone receptor-positive breast cancer. (ascopost.com)
Researchers at the National Eye Institute (NEI) have discovered a novel therapeutic strategy of using one or more selective estrogen-receptor modulators (SERMs), which may include the FDA-approved drug, Tamoxifen, for treating retinal degenerative diseases, like retinitis pigmentosa (RP) and age-related degeneration (AMD). (cancer.gov)
Without those receptors, breast cancer treatments that involve tamoxifen and trastuzumab don't have anything to attach to. (sciencealert.com)

Abstract: Administration of estrogen to adult male rats increases the density of striatal dopamine receptors. (elsevier.com)
abstract = "\Vo oxamined whether [igand-bound estrogen receptor exerted regulalory contro] over dioxin-nmdiated cytochrome P450 1AI (CYP1A1) trans(:ription in cultured human endometrial epithelial (:ells (ECC 1). (umn.edu)
abstract = "Background: We postulate that the androgen dehydroepiandrosterone sulfate (DHEAS) may represent an innovative hormonal treatment for estrogen (ER), progesterone (PR) receptor-negative, but androgen receptor (AR)-positive breast cancers by inhibiting breast cancer cell growth through AR stimulation. (elsevier.com)
abstract = "Diethylstilbestrol (DES) is a synthetic estrogen and proven human teratogen and carcinogen reported to act via the estrogen receptor α (ERα). (wur.nl)

They act on postsynaptic dopamine receptors while causing no effect on other anterior pituitary functions. (medscape.com)
The densities of the dopamine receptors in the nucleus accumbens and cortex are not altered, while the density of those in the hippocampus is decreased. (elsevier.com)
The increased density of striatal dopamine receptors normally observed after estrogen treatment is prevented by prior injection into the striatum of kainic acid, which destroys the intrinsic neurons in the striatum. (elsevier.com)
Hruska, RE & Pitman, KT 1982, ' Distribution and Localization of Estrogen‐Sensitive Dopamine Receptors in the Rat Brain ', Journal of Neurochemistry , vol. 39, no. 5, pp. 1418-1423. (elsevier.com)
Cabergoline interacts with dopamine receptors that are located in the pituitary lactotrophic cells. (steroidsforsale.click)

The EMERALD trial is examining the use of a new investigational oral selective estrogen receptor degrader (SERD), elacestrant, for the treatment of women with estrogen receptor-positive/HER2-negative (ER+/HER2-) metastatic breast tumors that have progressed on prior endocrine and targeted therapies. (stopbreastcancer.org)

Calmodulin antagonists (w7 and melatonin) have been shown to significantly inhibit human estrogen receptor alpha (hERalpha) transcriptional activity. (suny.edu)
Addition of estrogen receptor antagonists, 4-hydroxytamoxifen or ICI lg2. (umn.edu)

These agents bind to estrogen receptors, preventing stimulating effects of estrogen on nucleic acid synthesis. (medscape.com)
In addition, the benzodiazepine receptors in the striatum, cortex, hippocampus, and cerebellum are not altered by estrogen treatment, showing the specificity of the estrogen treatment and suggesting that the effects of estrogen are not mediated through benzodiazepine receptors. (elsevier.com)
We have examined the properties of the estrogen receptor and progesterone receptor in MDA-MB-134 human breast cells and have evaluated the effects of estrogen on cell proliferation and progesterone receptor levels in these cells as indices of hormonal sensitivity. (aacrjournals.org)
G-protein coupled estrogen receptor (GPER) is a transmembrane receptor that mediates non-genomic effects of estrogen. (techscience.com)

Bisphenol A Does Not Mimic Estrogen in the Promotion of the In Vitro Response of Murine Dendritic Cells to Toll-Like Receptor Ligands. (umassmed.edu)
To that end, an in vivo test system in yeast has been used that allowed assessment of the transactivation properties of the artificial ligands in WT and mutated receptors. (uni-goettingen.de)

like all sarms, ostarine works by binding to proteins in the body, called androgen receptors (ars). (prodigymotorsports.net)

Selective estrogen receptor modulators (SERMs) have therefore provided an effective targeted therapy to treat ER-α positive breast cancer patients. (carcinogenesis.com)
The effects of SERMs on these parameters in the cardiac tissue of estrogen-deficient rats has not been reported. (unboundmedicine.com)
Both 17-β-estradiol and SERMs were able to reverse these alterations, which were induced by the estrogen deficient state. (unboundmedicine.com)
agonists and selective oestrogen receptor modulators (SERMs) is provided. (chemwatch.net)

There are multiple ways in which resistance can occur, but one common way in ER+/HER2- breast cancer is the development of mutations in a gene that codes for the estrogen receptor (ESR1). (stopbreastcancer.org)
If the presence of tumor is confirmed, estrogen receptor, progesterone receptor, and human epidermal growth factor type 2 (HER2) expression/amplification should be evaluated. (cancer.gov)
In a male breast cancer series, 99% of the tumors were estrogen receptor positive, 82% were progesterone receptor positive, 9% were HER2 positive, and 0.3% were triple negative. (cancer.gov)
Tumor size, lymph node involvement, and grade are anatomical prognostic factors, while estrogen receptor, progesterone receptor, and HER2 status are predictive of response to therapy. (cancer.gov)
They are called "triple negative" because about 90% lack both estrogen and progesterone receptors on their cell surfaces and they don't overproduce the Her2 oncogene. (breastlink.com)
One particularly nasty type of tumour that has been seen to use this tactic is triple-negative breast cancer , a disease that makes up 15 percent of breast cancers and is distinguished by a lack of receptors for estrogen, progesterone, and HER2/neu. (sciencealert.com)
Adding Kisqali to Femara as a first treatment for advanced-stage hormone-receptor-positive HER2-negative breast cancer in postmenopausal women improved overall survival by more than 1 year. (vsyl.net)
Adding the targeted therapy Kisqali (chemical name: ribociclib) to the hormonal therapy Femara (chemical name: letrozole) as a first treatment for advanced-stage hormone-receptor-positive HER2-negative breast cancer in postmenopausal women improved overall survival by more than 1 year, according to the latest results from the MONALEESA-2 study. (vsyl.net)
Kisqali is used in combination with an aromatase inhibitor, a type of hormonal therapy, to treat advanced-stage or metastatic hormone-receptor-positive HER2-negative breast cancer that hasn't been treated with hormonal therapy yet in premenopausal, perimenopausal, and postmenopausal women. (vsyl.net)
Kisqali also is used in combination with the hormonal therapy Faslodex (chemical name: fulvestrant) to treat advanced-stage or metastatic hormone-receptor-positive HER2-negative breast cancer that hasn't been treated with hormonal therapy yet or has grown while being treated with a different hormonal therapy in postmenopausal women. (vsyl.net)
The MONALEESA-2 study included 668 postmenopausal women diagnosed with advanced-stage hormone-receptor-positive HER2-negative breast cancer. (vsyl.net)

[4] , [5] The biological effects of estrogens are mediated by estrogen receptor alpha (ER-α), a member of the superfamily of nuclear receptors that function as ligand-inducible transcription factors. (carcinogenesis.com)
This gene encodes a member of the family of estrogen receptors and superfamily of nuclear receptor transcription factors. (genetex.com)

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. (umassmed.edu)

The receptor binds its natural ligand 17-β-estradiol (E2) in the ligand binding domain (LBD) ( 20 ). (spandidos-publications.com)
Upon exposure to estradiol, the receptors become occupied, but there is no processing or apparent decrease in either nuclear or total cellular estrogen receptor content, as can be seen in MCF-7 human breast cancer cells. (aacrjournals.org)
Control cells contain low levels of progesterone receptor that display high affinity (K d = 6 × 10 -9 m ) for the synthetic progestin R5020, but exposure to estradiol (10 -11 -10 -7 m ) fails to increase cellular progesterone receptor levels. (aacrjournals.org)
Hence, our data show that these cells, which contain substantial levels of estrogen receptor, respond to estrogen with enhanced cell proliferation but fail to have their progesterone receptor level modulated by estradiol. (aacrjournals.org)
To gain insights into the molecular consequences of the ESR2 defect, whole exome sequencing and extensive functional transactivation studies in ovarian, bone, and breast cells were conducted, with or without the natural activator of estrogen receptors, 17β-estradiol. (uzh.ch)
The aim of this dissertation was the development of an inducible gene switch based on a modified human estrogen receptor and non-steroidal estradiol analogs. (uni-goettingen.de)
DT56a, similarly to estradiol-17β (E 2 ), stimulated the specific activity of creatine kinase (CK) in skeletal and vascular tissues of female rats, as a marker of estrogen receptor (ER) activation. (bgu.ac.il)
PET imaging with 16α-18F-fluoro-17ß-fluoroestradiol (18F-FES), a radiolabeled form of estradiol , allows whole-body, noninvasive evaluation of estrogen receptor (ER). (bvsalud.org)

Estrogen Receptor beta antibody [14C8] detects Estrogen Receptor beta protein at nucleus by immunohistochemical analysis. (genetex.com)
The subsequent 3-dimensional change of the protein induces the dimerization of the receptor and translocation to the nucleus, where ERα binds to the DNA and functions as transcription factor ( 20 ). (spandidos-publications.com)
Cancer receptor protein used in Estrogen Alfa with PDB code 2JF9. (simulations-plus.com)
The protein also interacts with the estrogen receptor 1 transcription factor and regulates estrogen receptor 1 transcriptional activity. (innov-research.com)
Therefore, we tested for agonist-induced changes in AT1R mRNA expression by RT-PCR and protein expression by analyzing receptor binding to test the hypothesis that the divergent effects of these ER subtypes are mediated by region-specific changes in AT 1 R expression. (uky.edu)

[6] A related ER, termed ER-β, encoded by a distinct gene, has been identified and may mediate estrogen signaling in some tissues. (carcinogenesis.com)
Wei CD, Zheng HY, Wu W, Dai W, Tong YQ, Wang M, Li Y. Meta-Analysis of the Association of the Rs2234693 and Rs9340799 Polymorphisms of Estrogen Receptor Alpha Gene with Coronary Heart Disease Risk in Chinese Han Population. (medsci.org)
Estrogen resistance due to mutations in the estrogen receptor α gene (ESR1) has been described in men and women and is characterized by osteoporosis, delayed bone age and continuous growth in adulthood, and delayed puberty and multiple ovarian cysts in women. (uzh.ch)
Although mutations in the estrogen receptor β gene ESR2 were found in 46, XY patients with differences of sex development, no genetic variants of ESR2 were linked to gonadal defects in women. (uzh.ch)
Androgen receptor gene expression levels were determined using quantitative real-time polymerase chain reaction (q-RT-PCR). (elsevier.com)
IMSEAR at SEARO: PvuII polymorphism of estrogen receptor-α gene in breast cancer. (who.int)
Surekha D, Vishnupriya S, Rao D Nageswara, Sailaja K, Raghunadharao D. PvuII polymorphism of estrogen receptor-α gene in breast cancer. (who.int)
Several common polymorphisms of the ERα gene have been reported to be associated with alterations in receptor expression in breast cancer. (who.int)
Association of CYP1B1 gene polymorphisms and the positive expression of estrogen alpha and estrogen beta with endometrial cancer risk. (cdc.gov)

The natural compound DT56a (Femarelle) was shown to activate estrogen receptors in human cultured female derived osteoblasts. (bgu.ac.il)

In most mouse models of breast cancer, the tumors that form are typically ER-negative and independent of estrogen for their growth. (carcinogenesis.com)
Estrogen Alfa (ERα) is a receptor used as the main marker to identify the presence of tumors in the breast.compounds Gendarusin A-E have anticancer activity by inhibiting the poliferation of cancer cells and inducing apoptosis. (simulations-plus.com)
To test this hypothesis, we used real-time quantitative RT-PCR to quantify the mRNA expression of a large panel of genes coding for the major xenobiotic-metabolizing enzymes (12 phase I enzymes, 12 phase II enzymes and three members of the ABC transporter family) in a small series of normal breast (and liver) tissues, and in estrogen receptor alpha (ERα)-negative and ERα-positive breast tumors. (biomedcentral.com)
Due to reduced availability of estrogen, estrogen -dependent tumors regress. (gpatindia.com)
I. Regress in estrogen receptor positive tumors. (gpatindia.com)

Predicts risk for postmenopausal women of distant recurrence of early-stage hormone receptor positive breast cancer with up to three positive lymph nodes within 10 years of diagnosis and after five years of hormone therapy. (rgare.com)
Aromatase inhibitors stop the production of estrogen in postmenopausal women. (vsyl.net)
Estrogen therapy is the most effective option and is the current standard of care for vulvovaginal atrophy-related sexual dysfunction in postmenopausal women. (bvsalud.org)

Competitively binds to estrogen receptor, producing nuclear complex that decreases DNA synthesis and inhibits estrogen effects. (medscape.com)
Ligand-binding assays with recombinant sbERbetaa and sbERalpha revealed that sbERbetaa binds E(2) with 6.5-fold higher affinity than sbERalpha, confirming the selection of a high sensitive receptor for the yeast assay. (ualg.pt)
It binds the estrogen receptor and blocks estrogen from attaching. (stopbreastcancer.org)

Some isoforms dominantly inhibit the activity of other estrogen receptor family members. (genetex.com)
Inhibit estrogen effects by competitively binding to the estrogen receptor. (medscape.com)
and progesterone receptor in prostate adenocarcinoma, does it inhibit neoplastic proliferation and invasion? (who.int)

In a 2010 review article , Ganti's group noted that "the proliferative effect of estrogen in lung cancer cells is mediated through two main pathways -- the genomic or 'classical' pathway involving primarily ER-beta and possibly ER-alpha, and the non-genomic pathway involving both the ERs (ER-alpha and beta). (medpagetoday.com)
About 60 - 70% of breast cancers are Estrogen Receptor alpha (ER-α) positive and are dependent on estrogen for growth. (carcinogenesis.com)
Estrogen Receptor-alpha (ER) drives 75% of breast cancers. (cam.ac.uk)
The oestrogen receptor alpha (ERα) is expressed in prostate cancers, independent of AR status. (fry-it.com)
Breast cancer growth is regulated by estrogen, which acts by binding to its estrogen receptor alpha (ERα). (biomedcentral.com)

Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)

Lupinalbin A as the most potent estrogen receptor α- and aryl hydrocarbon receptor agonist in Eriosema laurentii de Wild. (biomedcentral.com)

Doctors often use hormone therapy to treat hormone receptor positive breast cancer . (cancerresearchuk.org)
The aim of this trial was to see if everolimus and exemestane together worked better than exemestane alone for hormone receptor positive breast cancer that had come back or continued to grow after treatment with letrozole or anastrozole. (cancerresearchuk.org)
This means that less estrogen is available to stimulate the growth of hormone-receptor-positive breast cancer cells. (vsyl.net)

Scientists at the National Cancer Institute (NCI) developed a potent chimeric antigen receptor (CAR) targeting glypican-3 (GPC3). (cancer.gov)
In January 2021, Pfizer announced that the Phase 2 clinical trials for product candidates includes individualized and off-the-shelf mRNA-based therapies, innovative chimeric antigen receptor T cells, bi-specific checkpoint immuno-modulators, targeted cancer antibodies and small molecules. (micronus.xyz)

BBP, BCP and BOP bound in silico and in vitro to ERα and activated the receptor. (spandidos-publications.com)

This is a report of a loss-of-function mutation in the estrogen receptor β in a young woman with complete ovarian failure, suggesting that ESR2 is necessary for human ovarian determination and/or maintenance and that ESR1 is not sufficient to sustain ovarian function in humans. (uzh.ch)

Receptors are proteins that attach to certain substances. (medlineplus.gov)
In addition, calcium binding proteins such as, calmodulin (CaM) which are significantly overexpressed in cancer cells, can activate transcription of target genes by directly binding to ER in lieu of estrogen. (suny.edu)
Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. (bvsalud.org)

53 (4) : 1204-1212 Expression of Estrogen and Progesterone Receptors in Papillary Thyroid Carcinoma in Korea. (genetex.com)

A drug that acts like estrogen on some tissues but blocks the effect of estrogen on other tissues. (webref.org)
Estrogen receptors (ERs) are present in connective tissues, indicating these tissues' potential responsiveness to estrogen. (eurekamag.com)

To formulate clinical consensus recommendations on bone health assessment and management of women with oestrogen receptor-positive early breast cancer receiving endocrine therapy, representatives appointed by relevant Australian Medical Societies used a systematic approach for adaptation of guidelines (ADAPTE) to derive an evidence-informed position statement addressing 5 key questions. (garvan.org.au)

About 60 - 70% of human breast cancers are ER-positive and estrogen-dependent, [8] and ER and progesterone receptor (PR) expression is an important indicator of potential responses to hormonal therapy. (carcinogenesis.com)

This research suggests that estrogen receptor status may have prognostic implications for treating patients with lung cancer. (medpagetoday.com)
What is the lung cancer community's current take on the role of estrogen, and/or HRT, in female patients with lung adenocarcinoma? (medpagetoday.com)
Here we describe a 16-year-old female patient who came to our tertiary care hospital with complete lack of estrogen action, as demonstrated by absent breast development, primary amenorrhea, and osteoporosis, resembling patients with ESR1 mutation. (uzh.ch)
The frequency of the PP genotype was increased in patients positive for ER and HER-2/neu as compared to those with receptor-negative status. (who.int)
This week we highlight a couple of other findings from SABCS, regarding metastatic estrogen receptor-positive breast cancer, with a focus on patients who develop treatment resistance through an estrogen receptor (ESR1) mutation. (stopbreastcancer.org)
En conséquence, 47 % de ces patients présentaient un stade avancé (III et IV). (who.int)
Most patients had positive estrogen and progesterone receptors. (who.int)
Estrogen and progesterone receptors [‎ER and PR]‎ were immunocytochemically analysed in mammary tumour cells obtained by fine needle sampling from 73 patients. (who.int)
On their own, such trials are not sufficient to provide recurrence estimates at the population level because they lack diversity, represent fewer than 5% of all cancer patients, and the study period may not be long enough to capture recurrences for long-latency breast cancers, such as estrogen receptor-positive malignancies. (medscape.com)
In oestrogen receptor negative patients that are known to have a poor overall survival, a considerably worse prognosis was seen in cases that exhibited low expression of TxNIP (P¼0.000003), stratifying patients into more defined groups. (nottingham.ac.uk)
Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important. (bvsalud.org)

ER/PR tests will show whether there are ER and/or PR receptors on your breast cancer cells. (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)
More recently, several groups have identified different receptors related to estrogen on lung cancer cells. (medpagetoday.com)
As for ER-β, it is "the predominant receptor that appears to mediate the proliferative effects of E2 on lung cancer cells. (medpagetoday.com)
Epigenetic and transcriptome responsiveness to ER modulation by tissue selective estrogen complexes in breast epithelial and breast cancer cells. (umassmed.edu)
For this purpose, molecular docking and microscale thermophoresis were applied, and estrogen receptor α (ERα) activation was measured in ESR1 ‑overexpressing 293 cells. (spandidos-publications.com)
EDCs mimic hormones and induce hormonal effects in cells, mediated by nuclear receptors such as the estrogen receptor (ER) ( 17 , 18 ). (spandidos-publications.com)
These cells contain high levels of estrogen receptor (approximately 1.5 pmol/mg DNA) and low levels of progesterone receptor (0.15 pmol/mg DNA). (aacrjournals.org)
These cells represent an interesting and unusual situation in which estrogenic regulation of proliferation and the stimulation of progesterone receptor are dissociated. (aacrjournals.org)
human endornetria] cells contain functional Ah receptors. (umn.edu)
Additionally, researchers subdivide human being NK cells into two main subsets with specific maturation and practical properties based on the manifestation of Compact disc56 as well as the antibody binding-Fc receptor Compact disc16 (13). (healthweblognews.info)
This prevents estrogen from stimulating the cells to grow. (stopbreastcancer.org)
ER positive breast cancer means good prognosis, as this cancerous cells are estrogen-dependent and can be treated with anti-estrogen therapy. (usmle-forums.com)
Both receptors had been present in Computer3 cells in handles (Cnt) and ZEA with or without ERs inhibitors treated cells. (cancerhugs.com)

BACKGROUND: Estrogen receptor (ER) is a ligand-inducible transcription factor that mediates estrogen action in target tissue. (who.int)

The nuclear estrogen receptor sediments as a 4.6 S species on high salt sucrose gradients, and it can be detected on sodium dodecyl sulfate-polyacrylamide gel immunoblot analysis as a species of molecular weight 65,000, identical to that of the MCF-7 estrogen receptor, using the monoclonal antibodies D75P3γ and H222Spγ prepared against the MCF-7 estrogen receptor. (aacrjournals.org)
Prediction of cytotoxic activity using Molegro Virtual Docker (MVD) by validating receptors and molecular docking. (simulations-plus.com)
Molecular docking analysis performed for 27b showed its possible interactions with estrogen receptor-α and -β (ER-α and ER-β) as well as the vitamin-D receptor (VDR). (rsc.org)
In addition, the binding property of SIL to the two estrogen receptors (ER) subtypes was tested by molecular docking. (osteoporosis-studies.com)
Molecular insight into the diverse oestrogen mechanism of action among PAEs with regard to hER? (chemwatch.net)

Kadhim A. L. Shadood, H. , Abdul-Aziz Atiya, S. and Ali Kardar, G. (2018) Correlation of Breast Cancer with the Epstein Bar Virus and Human Cytomegalovirus Frequency and the Expression of Estrogen Receptor-Beta and IL-6 Receptor in Iraqi Women. (scirp.org)

The pp and p allele frequencies were increased in progesterone-receptor-negative status. (who.int)

Estrogen sulfation genes, hormone replacement therapy, and endometrial cancer risk. (cdc.gov)
INTRODUCCIÓN: La causa más común de cáncer de seno hereditario es una mutación hereditaria en los genes BRCA1 y 2. (bvsalud.org)

Selective estrogen receptor degraders (SERD) attach to and break down the estrogen receptor. (stopbreastcancer.org)

Researchers at the National Cancer Institute's Experimental Transplantation and Immunology Branch (NCI ETIB) developed a T Cell receptor that specifically targets the Kita-Kyushu Lung Cancer Antigen 1 (KK-LC-1) 52-60 epitope that is highly expressed by several common and aggressive epithelial tumor types. (cancer.gov)

Selective Estrogen Receptor Modulators" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)
This graph shows the total number of publications written about "Selective Estrogen Receptor Modulators" by people in this website by year, and whether "Selective Estrogen Receptor Modulators" was a major or minor topic of these publications. (umassmed.edu)
Below are the most recent publications written about "Selective Estrogen Receptor Modulators" by people in Profiles. (umassmed.edu)
21. Diez-perez A. Selective Estrogen Receptor Modulators. (bvsalud.org)
Selective estrogen receptor modulators in reproductive medicine and biology. (bvsalud.org)

3 (1) : vdab099 Histone deacetylase inhibitors enhance estrogen receptor beta expression and augment agonist-mediated tumor suppression in glioblastoma. (genetex.com)
One unexpected consequence of having breast cancer is that Kathy has stopped eating Tofu and soy products that are estrogenic, given that her tumor is Estrogen Receptor positive and is "fueled" by estrogen. (blogspot.com)
INTRODUCCIÓN: Prostatectomía por laparoscopia es una técnica quirúrgica que se utiliza para extirpar un tumor de próstata localizado en el interior de la glándula o para extirpar la próstata por completo. (bvsalud.org)

The induction of beta-galactosidase activity was strictly dependent on the presence of seabream (Sparus aurata) betaa estrogen receptor (sbERbetaa) and substances known to have estrogenic activity. (ualg.pt)

Ganti et al went on to look at epigenetic changes in ER, the interaction of estrogen and testosterone, and the roles of progesterone and aromatase. (medpagetoday.com)
These results reveal the usefulness of using the yeast-based receptor assay for detecting chemical interaction with steroid receptors from contaminated samples. (ualg.pt)
Interaction of organochlorine compounds with thyroid receptor, transthyretin, and thyroid-binding globulin. (cdc.gov)

Estrogen receptor-α immunoreactivity predicts symptom severity and pain recurrence in deep endometriosis To determine the relationship between steroid receptor expression and pain symptoms in endometriosis. (embies.com)

These therapies can be combined with ovarian suppression in premenopausal women which reduces the production of estrogen. (stopbreastcancer.org)

Estrogen-triggered nuclear transcription factor, estrogen receptor (ER) is expressed in about 70% of breast cancer. (suny.edu)

E 2 decreases expression of the angiotensin II type 1 receptor (AT 1 R), a receptor with known relevance to water and salt intakes, in multiple areas of the brain where ERα and ERβ are differentially expressed. (uky.edu)

About 70 percent of all breast cancers in women have receptors that attach to estrogen and/or progesterone. (medlineplus.gov)
1995. Organochlorine compounds and estrogen-related cancers in women. (cdc.gov)

Anatomy20

Organisms3

Diseases8

Chemicals and Drugs77

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes35

Disciplines and Occupations1

Information Science2

Health Care2

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

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

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

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

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)

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

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

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

Estrogens

Receptors, Estrogen

Estrogen Receptor alpha

Estrogen Receptor beta

Estrogens, Conjugated (USP)

Estradiol

Estrogens, Catechol

Ovariectomy

Selective Estrogen Receptor Modulators

Estrogens, Non-Steroidal

Breast Neoplasms

Tamoxifen

Estradiol Congeners

Aromatase

Receptors, Progesterone

Diethylstilbestrol

Uterus

Estrone

Postmenopause

Progesterone

Ethinyl Estradiol

Progestins

Phytoestrogens

Neoplasms, Hormone-Dependent

RNA, Messenger

Hydroxyestrones

Aromatase Inhibitors

Menopause

Vitellogenins

Cell Line, Tumor

Antineoplastic Agents, Hormonal

Nafoxidine

Castration

Gonadal Steroid Hormones

Testosterone

Immunohistochemistry

Medroxyprogesterone Acetate

Phenols

Benzhydryl Compounds

Isoflavones

Signal Transduction

Rats, Sprague-Dawley

Response Elements

Receptors, Estradiol

Gene Expression Regulation

Transcription, Genetic

Sex Characteristics

Endocrine Disruptors

Androgens

Gene Expression Regulation, Neoplastic

Endometrium

Reverse Transcriptase Polymerase Chain Reaction

Receptors, Androgen

Dose-Response Relationship, Drug

Tumor Cells, Cultured

Ovary

Breast

Estrous Cycle

Hormone Replacement Therapy

Oviducts

Premenopause

Equilenin

Drug Implants

Pregnancy

Cell Proliferation

Dihydrotestosterone

Promoter Regions, Genetic

Hexestrol

Endometrial Neoplasms

Menstrual Cycle

Medroxyprogesterone

Transcriptional Activation

Cells, Cultured

Mammary Neoplasms, Experimental

Receptor, erbB-2

Blotting, Western

Plant Preparations

Cell Division

Estradiol Dehydrogenases

MCF-7 Cells