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.
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 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.
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.
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.
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)
Tumors or cancer of the human BREAST.
Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.
Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.
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.
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.
The surgical removal of one or both ovaries.
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.
A cell line derived from cultured tumor cells.
Non-steroidal compounds with estrogenic activity.
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.
PLANT EXTRACTS and compounds, primarily ISOFLAVONES, that mimic or modulate endogenous estrogens, usually by binding to ESTROGEN RECEPTORS.
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.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
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.
Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.
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)
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.
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.
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.
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 second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in neoplastic tissue.
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.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
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)
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
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.
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.
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)
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 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.
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.
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.
An estrogen responsive cell line derived from a patient with metastatic human breast ADENOCARCINOMA (at the Michigan Cancer Foundation.)
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.
Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.
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.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
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.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A nuclear transcription factor. Heterodimerization with RETINOID X RECEPTOR GAMMA is important to metabolism of LIPIDS. It is the target of FIBRATES to control HYPERLIPIDEMIAS.
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.
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.
Intracellular receptors that can be found in the cytoplasm or in the nucleus. They bind to extracellular signaling molecules that migrate through or are transported across the CELL MEMBRANE. Many members of this class of receptors occur in the cytoplasm and are transported to the CELL NUCLEUS upon ligand-binding where they signal via DNA-binding and transcription regulation. Also included in this category are receptors found on INTRACELLULAR MEMBRANES that act via mechanisms similar to CELL SURFACE RECEPTORS.
The simultaneous or sequential binding of multiple cell surface receptors to different ligands resulting in coordinated stimulation or suppression of signal transduction.
An interleukin-13 receptor subunit that is closely-related to the INTERLEUKIN-13 RECEPTOR ALPHA1 SUBUNIT. The receptor is found as a monomeric protein and has been considered to be a decoy receptor for interleukin-13 due the fact that it lacks cytoplasmic signaling domains.
An insecticide. Methoxychlor has estrogenic effects in mammals, among other effects.
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.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
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.
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.
Proteins that enhance gene expression when associated with ligand bound activated NUCLEAR RECEPTORS. The coactivators may act through an enzymatic process that affects the rate of transcription or the structure of chromatin. Alternatively nuclear receptor coactivators can function as adaptor proteins that bring nuclear receptors into close proximity with transcriptional complexes.
A nuclear transcription factor. Heterodimerization with PPAR GAMMA is important in regulation of GLUCOSE metabolism and CELL GROWTH PROCESSES.
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.
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.
An interleukin receptor subunit with specificity for INTERLEUKIN-13. It dimerizes with the INTERLEUKIN-4 RECEPTOR ALPHA SUBUNIT to form the TYPE II INTERLEUKIN-4 RECEPTOR which has specificity for both INTERLEUKIN-4 and INTERLEUKIN-13. Signaling of this receptor subunit occurs through the interaction of its cytoplasmic domain with JANUS KINASES such as the TYK2 KINASE.
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)
The relationship between the dose of an administered drug and the response of the organism to the drug.
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.
A technique for identifying specific DNA sequences that are bound, in vivo, to proteins of interest. It involves formaldehyde fixation of CHROMATIN to crosslink the DNA-BINDING PROTEINS to the DNA. After shearing the DNA into small fragments, specific DNA-protein complexes are isolated by immunoprecipitation with protein-specific ANTIBODIES. Then, the DNA isolated from the complex can be identified by PCR amplification and sequencing.
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).
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
Established cell cultures that have the potential to propagate indefinitely.
Proteins in the nucleus or cytoplasm that specifically bind RETINOIC ACID or RETINOL and trigger changes in the behavior of cells. Retinoic acid receptors, like steroid receptors, are ligand-activated transcription regulators. Several types have been recognized.
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.
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.
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.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
High affinity receptors for THYROID HORMONES, especially TRIIODOTHYRONINE. These receptors are usually found in the nucleus where they regulate DNA transcription. They are encoded by the THRA gene (also known as NR1A1, THRA1, ERBA or ERBA1 gene) as several isoforms produced by alternative splicing.
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.
Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.
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.
Enzymes that catalyze acyl group transfer from ACETYL-CoA to HISTONES forming CoA and acetyl-histones.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
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.
Enzymes that oxidize certain LUMINESCENT AGENTS to emit light (PHYSICAL LUMINESCENCE). The luciferases from different organisms have evolved differently so have different structures and substrates.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases.
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.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones.
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.
A forkhead transcription factor that is an essential activator of GLUCAGON gene expression.
Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.
MAMMARY GLANDS in the non-human MAMMALS.
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.
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
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).
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.
Elements of limited time intervals, contributing to particular results or situations.
The determination of the pattern of genes expressed at the level of GENETIC TRANSCRIPTION, under specific circumstances or in a specific cell.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
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.
Resistance or diminished response of a neoplasm to an antineoplastic agent in humans, animals, or cell or tissue cultures.
A negative 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.
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 highly chlorinated polycyclic hydrocarbon insecticide whose large number of chlorine atoms makes it resistant to degradation. It has been shown to be toxic to mammals and causes abnormal cellular changes in laboratory animals.
The first continuously cultured human malignant CELL LINE, derived from the cervical carcinoma of Henrietta Lacks. These cells are used for VIRUS CULTIVATION and antitumor drug screening assays.
Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
Cytoplasmic proteins that bind estradiol, migrate to the nucleus, and regulate DNA transcription.
Proteins found in the nucleus of a cell. Do not confuse with NUCLEOPROTEINS which are proteins conjugated with nucleic acids, that are not necessarily present in the nucleus.
Experimentally induced mammary neoplasms in animals to provide a model for studying human BREAST NEOPLASMS.
Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.
Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.
Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.
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.
An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST.
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.
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.
One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.
Proteins whose abnormal expression (gain or loss) are associated with the development, growth, or progression of NEOPLASMS. Some neoplasm proteins are tumor antigens (ANTIGENS, NEOPLASM), i.e. they induce an immune reaction to their tumor. Many neoplasm proteins have been characterized and are used as tumor markers (BIOMARKERS, TUMOR) when they are detectable in cells and body fluids as monitors for the presence or growth of tumors. Abnormal expression of ONCOGENE PROTEINS is involved in neoplastic transformation, whereas the loss of expression of TUMOR SUPPRESSOR PROTEINS is involved with the loss of growth control and progression of the neoplasm.
Screening techniques first developed in yeast to identify genes encoding interacting proteins. Variations are used to evaluate interplay between proteins and other molecules. Two-hybrid techniques refer to analysis for protein-protein interactions, one-hybrid for DNA-protein interactions, three-hybrid interactions for RNA-protein interactions or ligand-based interactions. Reverse n-hybrid techniques refer to analysis for mutations or other small molecules that dissociate known interactions.
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.
In vitro method for producing large amounts of specific DNA or RNA fragments of defined length and sequence from small amounts of short oligonucleotide flanking sequences (primers). The essential steps include thermal denaturation of the double-stranded target molecules, annealing of the primers to their complementary sequences, and extension of the annealed primers by enzymatic synthesis with DNA polymerase. The reaction is efficient, specific, and extremely sensitive. Uses for the reaction include disease diagnosis, detection of difficult-to-isolate pathogens, mutation analysis, genetic testing, DNA sequencing, and analyzing evolutionary relationships.
A hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA. Isomers with inversion of the hydroxyl group or groups are called epiestriol.
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
A receptor subunit that is a component of the TYPE I INTERLEUKIN-4 RECEPTOR and the TYPE II INTERLEUKIN-4 RECEPTOR. It signals through interaction of its cytoplasmic domain with JANUS KINASES such as JANUS KINASE 1.
17 beta-Hydroxy-4-androsten-3-ones. Testosterone derivatives formed by the substitution of one or more hydroxyl groups in any position.
Immunologic techniques based on the use of: (1) enzyme-antibody conjugates; (2) enzyme-antigen conjugates; (3) antienzyme antibody followed by its homologous enzyme; or (4) enzyme-antienzyme complexes. These are used histologically for visualizing or labeling tissue specimens.
Diffusible gene products that act on homologous or heterologous molecules of viral or cellular DNA to regulate the expression of proteins.
A nuclear protein that regulates the expression of genes involved in a diverse array of processes related to metabolism and reproduction. The protein contains three nuclear receptor interaction domains and three repressor domains and is closely-related in structure to NUCLEAR RECEPTOR CO-REPRESSOR 2.
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.
Proteins prepared by recombinant DNA technology.
The measurement of an organ in volume, mass, or heaviness.
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.
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.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure.
Hybridization of a nucleic acid sample to a very large set of OLIGONUCLEOTIDE PROBES, which have been attached individually in columns and rows to a solid support, to determine a BASE SEQUENCE, or to detect variations in a gene sequence, GENE EXPRESSION, or for GENE MAPPING.
A CELL CYCLE and tumor growth marker which can be readily detected using IMMUNOCYTOCHEMISTRY methods. Ki-67 is a nuclear antigen present only in the nuclei of cycling cells.
Region of hypothalamus between the ANTERIOR COMMISSURE and OPTIC CHIASM.
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.
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.
The aglucon moiety of a saponin molecule. It may be triterpenoid or steroid, usually spirostan, in nature.
The genetic constitution of the individual, comprising the ALLELES present at each GENETIC LOCUS.
The process by which two molecules of the same chemical composition form a condensation product or polymer.
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.
A low affinity interleukin-5 receptor subunit that combines with the CYTOKINE RECEPTOR COMMON BETA SUBUNIT to form a high affinity receptor for INTERLEUKIN-5. Several isoforms of the interleukin-5 receptor alpha subunit exist due to multiple ALTERNATIVE SPLICING.
Proteins found usually in the cytoplasm or nucleus that specifically bind steroid hormones and trigger changes influencing the behavior of cells. The steroid receptor-steroid hormone complex regulates the transcription of specific genes.
The regular and simultaneous occurrence in a single interbreeding population of two or more discontinuous genotypes. The concept includes differences in genotypes ranging in size from a single nucleotide site (POLYMORPHISM, SINGLE NUCLEOTIDE) to large nucleotide sequences visible at a chromosomal level.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
A low affinity interleukin-11 receptor subunit that combines with the CYTOKINE RECEPTOR GP130 to form a high affinity receptor for INTERLEUKIN-11. Multiple isoforms of this protein exist due to ALTERNATIVE SPLICING of its MRNA.
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.
Proteins which maintain the transcriptional quiescence of specific GENES or OPERONS. Classical repressor proteins are DNA-binding proteins that are normally bound to the OPERATOR REGION of an operon, or the ENHANCER SEQUENCES of a gene until a signal occurs that causes their release.
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.
Proteins that are normally involved in holding cellular growth in check. Deficiencies or abnormalities in these proteins may lead to unregulated cell growth and tumor development.
An electrophoretic technique for assaying the binding of one compound to another. Typically one compound is labeled to follow its mobility during electrophoresis. If the labeled compound is bound by the other compound, then the mobility of the labeled compound through the electrophoretic medium will be retarded.
Material prepared from plants.
Luciferases from RENILLA that oxidizes certain LUMINESCENT AGENTS to cause emission of PHOTONS.
An estrogen antagonist that has been used in the treatment of breast cancer.
Paired ducts in the human male through which semen is ejaculated into the urethra.
Promoter-specific RNA polymerase II transcription factor that binds to the GC box, one of the upstream promoter elements, in mammalian cells. The binding of Sp1 is necessary for the initiation of transcription in the promoters of a variety of cellular and viral GENES.
The rate dynamics in chemical or physical systems.
A subtype of RETINOIC ACID RECEPTORS that are specific for 9-cis-retinoic acid which function as nuclear TRANSCRIPTION FACTORS that regulate multiple signaling pathways.
Commonly observed structural components of proteins formed by simple combinations of adjacent secondary structures. A commonly observed structure may be composed of a CONSERVED SEQUENCE which can be represented by a CONSENSUS SEQUENCE.
Intercellular signaling peptides that were originally characterized by their ability to suppress NEOPLASM METASTASIS. Kisspeptins have since been found to play an important role in the neuroendocrine regulation of REPRODUCTION.
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.
The aggregation of soluble ANTIGENS with ANTIBODIES, alone or with antibody binding factors such as ANTI-ANTIBODIES or STAPHYLOCOCCAL PROTEIN A, into complexes large enough to fall out of solution.
An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES).
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.
A birth defect due to malformation of the URETHRA in which the urethral opening is below its normal location. In the male, the malformed urethra generally opens on the ventral surface of the PENIS or on the PERINEUM. In the female, the malformed urethral opening is in the VAGINA.
A gene silencing phenomenon whereby specific dsRNAs (RNA, DOUBLE-STRANDED) trigger the degradation of homologous mRNA (RNA, MESSENGER). The specific dsRNAs are processed into SMALL INTERFERING RNA (siRNA) which serves as a guide for cleavage of the homologous mRNA in the RNA-INDUCED SILENCING COMPLEX. DNA METHYLATION may also be triggered during this process.
Transport proteins that carry specific substances in the blood or across cell membranes.
Mutant mice homozygous for the recessive gene "nude" which fail to develop a thymus. They are useful in tumor studies and studies on immune responses.
The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.
A small, unpaired gland situated in the SELLA TURCICA. It is connected to the HYPOTHALAMUS by a short stalk which is called the INFUNDIBULUM.
The material of CHROMOSOMES. It is a complex of DNA; HISTONES; and nonhistone proteins (CHROMOSOMAL PROTEINS, NON-HISTONE) found within the nucleus of a cell.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
The surgical removal of one or both testicles.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A mediator complex subunit that is believed to play a key role in the coactivation of nuclear receptor-activated transcription by the mediator complex. It interacts with a variety of nuclear receptors including RETINOIC ACID RECEPTORS; THYROID HORMONE RECEPTORS; VITAMIN D RECEPTORS; PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS; ESTROGEN RECEPTORS; and GLUCOCORTICOID RECEPTORS.
An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR.
Refers to animals in the period of time just after birth.
Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.
An integrin alpha subunit that primarily associates with INTEGRIN BETA1 or INTEGRIN BETA4 to form laminin-binding heterodimers. Integrin alpha6 has two alternatively spliced isoforms: integrin alpha6A and integrin alpha6B, which differ in their cytoplasmic domains and are regulated in a tissue-specific and developmental stage-specific manner.
Detection of RNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.
The network of channels formed at the termination of the straight SEMINIFEROUS TUBULES in the mediastinum testis. Rete testis channels drain into the efferent ductules that pass into the caput EPIDIDYMIS.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
A protein-serine-threonine kinase that is activated by PHOSPHORYLATION in response to GROWTH FACTORS or INSULIN. It plays a major role in cell metabolism, growth, and survival as a core component of SIGNAL TRANSDUCTION. Three isoforms have been described in mammalian cells.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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 MAMMARY GLAND in animals (MAMMARY GLANDS, ANIMAL).
Extrachromosomal, usually CIRCULAR DNA molecules that are self-replicating and transferable from one organism to another. They are found in a variety of bacterial, archaeal, fungal, algal, and plant species. They are used in GENETIC ENGINEERING as CLONING VECTORS.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
Chemical substances that are foreign to the biological system. They include naturally occurring compounds, drugs, environmental agents, carcinogens, insecticides, etc.
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.

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. (1/3532)

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)

Localization of curved DNA and its association with nucleosome phasing in the promoter region of the human estrogen receptor alpha gene. (2/3532)

We determined DNA bend sites in the promoter region of the human estrogen receptor (ER) gene by the circular permutation assay. A total of five sites (ERB-4 to -1, and ERB+1) mapped in the 3 kb region showed an average distance of 688 bp. Most of the sites were accompanied by short poly(dA) x poly(dT) tracts including the potential bend core sequence A2N8A2N8A2 (A/A/A). Fine mapping of the ERB-2 site indicated that this A/A/A and the 20 bp immediate flanking sequence containing one half of the estrogen response element were the sites of DNA curvature. All of the experimentally mapped bend sites corresponded to the positions of DNA curvature as well as to nucleosomes predicted by computer analysis. In vitro nucleosome mapping at ERB-2 revealed that the bend center was located 10-30 bp from the experimental and predicted nucleosome dyad axes.  (+info)

Expression of oestrogen receptor alpha and beta mRNA in corpus luteum of human subjects. (3/3532)

To investigate the role of oestrogen receptor beta (ERbeta) in the function of human ovarian corpus luteum, the levels of luteal ERalpha and ERbeta mRNA were determined using competitive reverse transcription-polymerase chain reaction-Southern blot analysis. The expression of ERalpha and ERbeta mRNA was detected in all luteal samples analysed. Luteal ERalpha and ERbeta mRNA levels were significantly lower (P<0.01 and P<0.05 respectively) at the late secretory phase than those at the early and mid-secretory phases of the endometrium. The ratio of ERalpha to ERbeta mRNA levels showed no change during the secretory phase of the endometrium. This study demonstrates that ERbeta is co-expressed with ERalpha in human corpus luteum and is likely to play a biological role in the regulation of steroidal action of the corpus luteum with ERalpha.  (+info)

Oestrogen receptor-alpha variant mRNA expression in primary human breast tumours and matched lymph node metastases. (4/3532)

We have shown previously that the relative expression of a truncated oestrogen receptor-alpha variant mRNA (ER clone 4) is significantly increased in axillary node-positive primary breast tumours compared with node-negative tumours. In this study, we have examined the relative expression of clone 4-truncated, exon 5-deleted and exon 7-deleted oestrogen receptor-alpha variant mRNAs in 15 primary breast tumour samples and in synchronous axillary lymph node metastases. Overall, there were no significant differences between the primary tumours and the matched metastases in the relative expression of these three specific variant mRNAs. Furthermore, the pattern of all deleted oestrogen receptor-alpha variant mRNAs appeared conserved between any primary and its matched secondary tumour.  (+info)

Disruption of estrogen signaling does not prevent progesterone action in the estrogen receptor alpha knockout mouse uterus. (5/3532)

Estrogen is known to increase progesterone receptor (PR) levels in the wild-type mouse uterus, and this estrogen induction was thought to be important for progesterone action through the PR. The estrogen receptor alpha knockout (ERKO) mouse uterus was observed to express PR mRNA that cannot be induced by estrogen. Progesterone action was characterized to determine whether it was diminished in ERKO mice. The PR protein is present in the ERKO uterus at 60% of the level measured in a wild-type uterus. The PR-A and PR-B isoforms are both detected on Western blot, and the ratio of isoforms is the same in both genotypes. Although the level of PR is reduced in the ERKO uterus, the receptor level is sufficient to induce genomic responses, since both calcitonin and amphiregulin mRNAs were increased after progesterone treatment. Finally, the ERKO uterus can be induced to undergo a progesterone-dependent decidual response. Surprisingly, the decidual response is estrogen independent in the ERKO, although it remains estrogen dependent in a wild type. These results indicate that estrogen receptor alpha modulation of PR levels is not necessary for expression of the PR or genomic and physiologic responses to progesterone in the ERKO uterus.  (+info)

Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha and ER beta. (6/3532)

Estrogen receptor (ER) modulators produce distinct tissue-specific biological effects, but within the confines of the established models of ER action it is difficult to understand why. Previous studies have suggested that there might be a relationship between ER structure and activity. Different ER modulators may induce conformational changes in the receptor that result in a specific biological activity. To investigate the possibility of modulator-specific conformational changes, we have applied affinity selection of peptides to identify binding surfaces that are exposed on the apo-ERs alpha and beta and on each receptor complexed with estradiol or 4-OH tamoxifen. These peptides are sensitive probes of receptor conformation. We show here that ER ligands, known to produce distinct biological effects, induce distinct conformational changes in the receptors, providing a strong correlation between ER conformation and biological activity. Furthermore, the ability of some of the peptides to discriminate between different ER alpha and ER beta ligand complexes suggests that the biological effects of ER agonists and antagonists acting through these receptors are likely to be different.  (+info)

A mouse mammary tumor virus-Wnt-1 transgene induces mammary gland hyperplasia and tumorigenesis in mice lacking estrogen receptor-alpha. (7/3532)

Estrogens have important functions in mammary gland development and carcinogenesis. To better define these roles, we have used two previously characterized lines of genetically altered mice: estrogen receptor-alpha (ER alpha) knockout (ERKO) mice, which lack the gene encoding ER alpha, and mouse mammary virus tumor (MMTV)-Wnt-1 transgenic mice (Wnt-1 TG), which develop mammary hyperplasia and neoplasia due to ectopic production of the Wnt-1 secretory glycoprotein. We have crossed these lines to ascertain the effects of ER alpha deficiency on mammary gland development and carcinogenesis in mice expressing the Wnt-1 transgene. Introduction of the Wnt-1 transgene into the ERKO background stimulates proliferation of alveolar-like epithelium, indicating that Wnt-1 protein can promote mitogenesis in the absence of an ER alpha-mediated response. The hyperplastic glandular tissue remains confined to the nipple region, implying that the requirement for ER alpha in ductal expansion is not overcome by ectopic Wnt-1. Tumors were detected in virgin ERKO females expressing the Wnt-1 transgene at an average age (48 weeks) that is twice that seen in virgin Wnt-1 TG mice (24 weeks) competent to produce ER alpha. Prepubertal ovariectomy of Wnt-1 TG mice also extended tumor latency to 42 weeks. However, pregnancy did not appear to accelerate the appearance of tumors in Wnt-1 TG mice, and tumor growth rates were not measurably affected by late ovariectomy. Small hyperplastic mammary glands were observed in Wnt-1 TG males, regardless of ER alpha gene status; the glands were similar in appearance to those found in ERKO/Wnt-1 TG females. Mammary tumors also occurred in Wnt-1 TG males; latency tended to be longer in the heterozygous ER alpha and ERKO males (86 to 100 weeks) than in wild-type ER alpha mice (ca. 75 weeks). We conclude that ectopic expression of the Wnt-1 proto-oncogene can induce mammary hyperplasia and tumorigenesis in the absence of ER alpha in female and male mice. The delayed time of tumor appearance may depend on the number of cells at risk of secondary events in the hyperplastic glands, on the carcinogenesis-promoting effects of ER alpha signaling, or on both.  (+info)

Expression of human estrogen receptor-alpha and -beta, progesterone receptor, and androgen receptor mRNA in normal and malignant ovarian epithelial cells. (8/3532)

Our understanding of the roles played by sex hormones in ovarian carcinogenesis has been limited by a lack of data concerning the mode of sex hormone action in human ovarian surface epithelial (HOSE) cells, the tissue of origin of >90% of ovarian cancers. We have compared the relative abundance of estrogen receptor (ER)alpha, ERbeta, progesterone receptor (PR), and androgen receptor (AR) mRNA in four primary cultures of HOSE cells obtained from postmenopausal women to those found in late serous adenocarcinoma primary cell cultures and established ovarian cancer cell lines. We observed coexpression of ERalpha and ERbeta mRNA along with AR and PR transcripts in normal HOSE cells and disruption of ERalpha mRNA expression as well as dramatic down-regulation of PR and AR transcript expression in most ovarian cancer cells. In contrast, levels of ERbeta mRNA were unaffected by the malignant state. Additionally, a novel mutation involving a 32-bp deletion in exon 1 of ERalpha transcripts was detected in the SKOV3 cell line. This mutation would explain why SKOV3 was reported to be ER-positive but estrogen-insensitive. Taken together, these findings suggest that estrogens, signaling via either or both ER subtypes, may play an indispensable role in regulating normal HOSE cell functions. Therefore, loss of ERalpha, PR, and AR mRNA expression in HOSE cells may be responsible for neoplastic transformation in this cell type. In contrast, the roles played by ERbeta in normal and malignant HOSE cells remain elusive. Finally, the coexistence of mutated ERalpha mRNA and normal ERbeta transcripts in SKOV3 argues in favor of a dependency of ERbeta action on functional ERalphas.  (+info)

The results presented here demonstrate that p53 upregulates estrogen receptor-alpha (ER alpha) expression in the human breast cancer cell line MCF-7. Two approaches were used to alter the activity of p53 in the cells. In the first approach, stable transfectants expressing an antisense p53 were established. In the stable clones, expression of antisense p53 resulted in a decrease in the expression of ER alpha protein. In the second approach, MCF-7 cells were transiently transfected with wild-type p53. Overexpression of p53 increased the amount of ER alpha. To determine whether the effects of p53 on the expression of ER alpha were due to changes in transcription, deletion mutants of the ER alpha promoter were used. This experimental approach demonstrated that p53 up-regulates ER alpha gene expression by increasing transcription of the gene through elements located upstream of promoter A. Transfection assays using p53 mutants further demonstrated that the p53-induced increase in ER alpha gene ...
Loss of estrogen receptor α (ERα) expression and gain of TWIST (TWIST1) expression in breast tumors correlate with increased disease recurrence and metastasis and poor disease-free s...
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TY - JOUR. T1 - The estrogen receptors alpha, beta, and beta cx. AU - Shaaban, Abeer M. AU - Speirs, Valerie. PY - 2005/11/15. Y1 - 2005/11/15. KW - Breast. KW - Breast Neoplasms. KW - Carcinoma in Situ. KW - Carcinoma, Ductal, Breast. KW - Estrogen Receptor alpha. KW - Estrogen Receptor beta. KW - Female. KW - Humans. KW - Immunohistochemistry. KW - Protein Isoforms. KW - Receptors, Estrogen. KW - Comment. KW - Comparative Study. KW - Letter. U2 - 10.1158/1078-0432.CCR-05-1446. DO - 10.1158/1078-0432.CCR-05-1446. M3 - Article. C2 - 16299256. VL - 11. SP - 8222; author reply 8222-3. JO - Clinical Cancer Research. JF - Clinical Cancer Research. SN - 1078-0432. IS - 22. ER - ...
BACKGROUND: Estrogen acutely activates endothelial nitric oxide synthase (eNOS). However, the identity of the receptors involved in this rapid response remains unclear. METHODS AND RESULTS: We detected an estrogen receptor alpha (ERalpha) transcript in human endothelial cells that encodes a truncated 46-kDa ERalpha (Delta1a-hERalpha-46). A corresponding 46-kDa ERalpha protein was identified in endothelial cell lysates. Transfection of cDNAs encoding the full-length ERalpha (ERalpha-66) and Delta1a-hERalpha-46 resulted in appropriately sized recombinant proteins identified by anti-ERalpha antibodies. Confocal microscopy revealed that a proportion of both ERalpha-66 and hERalpha-46 was localized outside the nucleus and mediated specific cell-surface binding of estrogen as assessed by FITC-conjugated, BSA-estrogen binding studies. Both ERalpha isoforms colocalized with eNOS and mediated acute activation of eNOS in response to estrogen stimulation. However, estrogen-stimulated transcriptional activation
BACKGROUND: Estrogen acutely activates endothelial nitric oxide synthase (eNOS). However, the identity of the receptors involved in this rapid response remains unclear. METHODS AND RESULTS: We detected an estrogen receptor alpha (ERalpha) transcript in human endothelial cells that encodes a truncated 46-kDa ERalpha (Delta1a-hERalpha-46). A corresponding 46-kDa ERalpha protein was identified in endothelial cell lysates. Transfection of cDNAs encoding the full-length ERalpha (ERalpha-66) and Delta1a-hERalpha-46 resulted in appropriately sized recombinant proteins identified by anti-ERalpha antibodies. Confocal microscopy revealed that a proportion of both ERalpha-66 and hERalpha-46 was localized outside the nucleus and mediated specific cell-surface binding of estrogen as assessed by FITC-conjugated, BSA-estrogen binding studies. Both ERalpha isoforms colocalized with eNOS and mediated acute activation of eNOS in response to estrogen stimulation. However, estrogen-stimulated transcriptional activation
A novel estrogen receptor (ER)alpha coactivator complex, the MLL2 complex, which consists of MLL2, ASH2, RBQ3, and WDR5, was identified. ERalpha directly binds to the MLL2 complex through two LXXLL motifs in a region of MLL2 near the C terminus in a ligand-dependent manner. Disrupting the interaction between ERalpha and the MLL2 complex with small interfering RNAs specific against MLL2 or an MLL2 fragment representing the interacting region with ERalpha significantly inhibited the ERalpha transcription activity. The MLL2 complex was recruited on promoters of ERalpha target genes along with ERalpha upon estrogen stimulation. Inhibition of MLL2 expression decreased the estrogen-induced expression of ERalpha target genes cathepsin D and to a lesser extent pS2. In addition, MCF-7 cell growth was also inhibited by the depletion of MLL2. These results demonstrate that the ERalpha signaling pathway is critically dependent on its direct interaction with the MLL2 complex and suggest a central
TY - JOUR. T1 - Estrogen receptor alpha signaling promotes Sle1-induced loss of tolerance and immune cell activation and is responsible for sex bias in B6.Sle1 congenic mice. AU - Yoachim, Shayla D. AU - Nuxoll, Jenny S.. AU - Bynoté, Kimberly K.. AU - Gould, Karen A. PY - 2015/6/1. Y1 - 2015/6/1. N2 - Sex bias in lupus incidence is thought to be due, in part, to the ability of estrogens to promote loss of tolerance. Previously, we showed that estrogens promote lupus via estrogen receptor α (ERα). C57BL/6 (B6) mice carrying the Sle1 lupus susceptibility locus (B6.Sle1) display loss of tolerance and develop anti-nuclear antibodies and immune cell hyperactivation. The incidence of loss of tolerance in B6.Sle1 females is greater than in males. Here, we show that a deficiency of either estrogens or ERα attenuates loss of tolerance and autoantibody development in B6.Sle1 females. Furthermore, we demonstrate that immune cell activation in B6.Sle1 mice shows sex bias and that ERα deficiency ...
Endocrine therapies focus on the service of the oestrogen receptor alpha dog (Emergency room) via distinct systems, but it all is not very clear whether breasts tumor cells may adapt to treatment using drug-specific systems. development. Finally, we demonstrate that a CB-based personal might become utilized to improve the stratification of Emergency room breast cancer individuals before adjuvant treatment. Outcomes Version to AI treatment qualified prospects to invasiveness ETs are designed to stop oestrogen-driven expansion by interfering with one particular TF (for example, Emergency room). Nevertheless, we hypothesized that the advancement of level of resistance may follow specific ways and generate alternate phenotypes through the different molecular systems particular to each agent2. To check this speculation, we utilized a series of isogenic cell lines resistant to solitary real estate agents or a mixture of real estate agents (endocrine therapy (ET)-resistant ETR cells, Fig. 1a)15. Our ...
Estrogen is essential for the development and maintenance of optimal bone mass in women and men, and acts through activation of estrogen receptors (ER). We have examined the pathways of estrogen action on the skeleton by seeking to localize the classical estrogen receptor, ER alpha, to particular cells to test the hypotheses that 1) estrogen directly influences growth plate chondrocytes; and 2) estrogen has a principal action on bone tissue via osteoblasts. ER alpha messenger ribonucleic acid (mRNA) was localized by in situ hybridization in human specimens from five males (11-15 yr old), two females (9 and 11 yr old), and three growing rabbits. In all of the human material examined, ER alpha mRNA was consistently identified in chondrocytes. In all of the rabbit tissue studied, ER alpha mRNA was localized in chondrocytes of the growth plate and the subarticular epiphyseal growth center. ER alpha mRNA signals were readily observed in both active osteoblasts and lining cells on trabecular surfaces of all
In mammalian cells, the level of estrogen receptor alpha (ER alpha) is rapidly decreased upon estrogen treatment, and this regulation involves proteasome degradation. Using different approaches, we showed that the Mdm2 oncogenic ubiquitin-ligase directly interacts with ER alpha in a ternary complex with p53 and is involved in the regulation of ER alpha turnover (both in the absence or presence of estrogens). Several lines of evidence indicated that this effect of Mdm2 required its ubiquitin-ligase activity and involved the ubiquitin/proteasome pathway. Moreover, in MCF-7 human breast cancer cells, various p53-inducing agents (such as UV irradiation) or treatment with RITA (which inhibits the interaction of p53 with Mdm2) stabilized ER alpha and abolished its 17 beta-estradiol-dependent turnover. Interestingly, our data indicated that ligand-dependent receptor turnover was not required for efficient transactivation. Altogether, our results indicate that the Mdm2 oncoprotein and stress-inducing ...
Jessop, H L and Sjoberg, M and Cheng, M Z and Zaman, G and Wheeler-Jones, C P D and Lanyon, L E (2001) Mechanical strain and estrogen activate estrogen receptor alpha in bone cells. JOURNAL OF BONE AND MINERAL RESEARCH, 16 (6). pp. 1045-1055. ...
TY - JOUR. T1 - aP2-Cre-mediated inactivation of estrogen receptor alpha causes hydrometra. AU - Antonson, Per. AU - Matic, Marko. AU - Portwood, Neil. AU - Kuiper, Raoul V.. AU - Bryzgalova, Galyna. AU - Gao, Hui. AU - Windahl, Sara H.. AU - Humire, Patricia. AU - Ohlsson, Claes. AU - Berggren, Per Olof. AU - Gustafsson, Jan Åke. AU - Dahlman-Wright, Karin. PY - 2014/1/8. Y1 - 2014/1/8. N2 - In this study we describe the reproductive phenotypes of a novel mouse model in which Cre-mediated deletion of ERα is regulated by the aP2 (fatty acid binding protein 4) promoter. ERα-floxed mice were crossed with transgenic mice expressing Cre-recombinase under the control of the aP2 promoter to generate aP2-Cre/ERαflox/flox mice. As expected, ERα mRNA levels were reduced in adipose tissue, but in addition we also detected an 80% reduction of ERα levels in the hypothalamus of aP2-Cre/ ERαflox/flox mice. Phenotypic analysis revealed that aP2-Cre/ERαflox/flox female mice were infertile. In line with ...
6HHP: Ternary complex of Estrogen Receptor alpha peptide and 14-3-3 sigma C42 mutant bound to disulfide fragment PPI stabilizer 1
Human estrogen receptor alpha (hERα) is a hormone-responsive nuclear receptor (NR) involved in cell growth and survival that contains both a DNA-binding domain (DBD) and a ligand-binding domain (LBD). Functionally relevant inter-domain interactions between the DBD and LBD have been observed in sever …
Estrogen receptor-alpha (ER alpha) is downregulated in the presence of its cognate ligand, estradiol (E2), through the ubiquitin proteasome pathway. Here, we show that ubiquitin proteasome function is required for ER alpha to serve as a transcriptional activator. Deletion of the last 61 amino acids …
Background Breast cancer is currently classified in 3 groups based on estrogen receptor alpha (ER) and human epidermal growth factor receptor 2 (HER2/ERBB2) gene expression: one basal-like (ER-ERBB2-), one HER2−enriched (ERBB2+) and one luminal (ER+). Yet, in transcriptome-based classifications, ER-ERBB2+ group partially overlaps with more recently defined ER-AR+ (androgen receptor positive) group. This type was named molecular apocrine, in reference to the histopathologically characterized apocrine carcinomas (H-Apo), in which a marked activation of AR signaling was demonstrated with a distinct proteomic signature. H-Apo tumors correspond to 1% of invasive breast carcinomas and are clearly morphological distinct from other AR+ tumors. However, no specific H-Apo transcriptome signature has been reported for this sub-group. In an effort to better characterize those tumors, we have performed a meta-analysis of genomic data, focusing on the ER- AR+ breast subset.. Samples and Methods: Chips were ...
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Alternative splicing is critical for generating complex proteomes in response to extracellular signals. Nuclear receptors including estrogen receptor alpha (ERα) and their ligands promote alternative splicing. The endogenous targets of ERα:estradiol (E2)-mediated alternative splicing and the influence of extracellular kinases that phosphorylate ERα on E2-induced splicing are unknown. MCF-7 and its anti-estrogen derivatives were used for the majority of the assays. CD44 mini gene was used to measure the effect of E2 and AKT on alternative splicing. ExonHit array analysis was performed to identify E2 and AKT-regulated endogenous alternatively spliced apoptosis-related genes. Quantitative reverse transcription polymerase chain reaction was performed to verify alternative splicing. ERα binding to alternatively spliced genes was verified by chromatin immunoprecipitation assay. Bromodeoxyuridine incorporation-ELISA and Annexin V labeling assays were done to measure cell proliferation and apoptosis,
Comprehensive evaluation of the estrogen receptor alpha gene reveals further evidence for association with type 2 diabetes enriched for nephropathy in an African American population. ...
Phase 1 of the study will be conducted to determine the maximum tolerated dose (MTD) and/or the recommended Phase 2 dose (RP2D) of H3B-6545 in women with
Commander Estrogen Receptor alpha anticorps monoclonal et polyclonal pour beaucoup dapplications. Selection de fournisseur de qualité pour anti-Estrogen Receptor alpha anticorps.
Approximately 75% of breast cancers are estrogen receptor (ERα) positive, underscoring the dependence of cancer cells on estrogen for growth and survival. Patients treated with endocrine therapy often develop resistance, either de novo or acquired, which is caused by aberrations within the growth factor signaling pathways. The mechanistic target of rapamycin complex 1 (mTORC1) has emerged as a critical node in estrogenic signaling. We have previously shown that mTORC1 can phosphorylate and activate ERα on S167 via its effector the 40S ribosomal S6 kinase 1 (S6K1). Presently, we have uncovered a direct link between mTORC1 and ERα. We found that ERα binds to regulatory-associated protein of mTOR (Raptor) and causes it to translocate to the nucleus upon estrogen stimulation. Additionally, we identified mTOR as the kinase that directly phosphorylates ERα and activates transcription of ER target genes. Our findings show a direct link between mTORC1 and ERα, which further implicates mTORC1 ...
Rabbit polyclonal Estrogen Receptor alpha antibody validated for WB, IHC and tested in Human and Mouse. Immunogen corresponding to synthetic peptide
Rabbit recombinant monoclonal Estrogen Receptor alpha antibody [EPR703(2)] validated for WB, IHC and tested in Human and Bb. With 7 independent reviews.
Estrogen Receptor alpha兔多克隆抗体可与小鼠, 人样本反应并经WB, ELISA, IHC实验严格验证,被4篇文献引用并得到1个独立的用户反馈。
AS05 065 Aquaculture antibodies, antibodies to fish stress proteins, estrogen receptor, antibodies to estrogen receptor alpha and beta,PO3372, Q92731, nuclear receptor subfamily 3 group A member 2 antibody
Endocrine therapy is an effective option for the treatment of estrogen receptor alpha (ERα)-positive breast cancers. Unfortunately, a large fraction of women ...
Alonso A, Fernandez R, Ordanyonez P, Moreno M, Patterson buy cardarone safely online AM, et al. (2006) Regulation of estrogen receptor alpha past estradiol in buy generic cardarone pregnant and estradiol treated rats. Steroids. However, our information showed no interchange in buy generic cardarone GSK3 phosphorylation associated with decreased apartment viability induced at Akt2 and Akt3 disruption. Figure 1 Photochemistry parameters circumspect using the DualPAM. Immediately after the lay unrestricted pressed a button, the corresponding discs on the screen were switched to green (if dominates chose the right button, a hit) or to red (if fields chose a ended of the average button, an error). There was also a nonsignificant gain in amount survival (OS). For example, the examine showed that barely 83% of hospitals utilize automated dispensing cabinets as into a receive of their distribution model; 10% utilize robotic dispensing. The opportunity regions directorial conducive to largeness ...
Abstract: Alnustone-like compounds are promising inhibitors for estrogen receptor \alpha (ER-\alpha), which is a novel cancer therapeutic target. Therefore, 10 alnustone-like compounds with substituents at the phenyl rings ...
Summary Two polymorphisms of the aromatase and estrogen receptor genes appeared to interact to influence the risk of hip fractures in women. Introduction Allelic variants of the aromatase gene have been associated with bone mineral density and vertebral fractures. Our objective was to analyze the relationship between two polymorphisms of the aromatase and estrogen receptor genes and hip ...
The transition to the postmenopausal stage is associated with an increased risk for vascular diseases, including myocardial infarction and stroke. This has been linked to a decrease in estrogen production. Estrogens mediate their effects on the brain to a major extent through binding to nuclear receptors, estrogen receptor alpha and beta. It is possible that positive and adverse effects of estrogens are related to interactions between receptor genotypes and hormones. Notably, the estrogen receptor alpha polymorphism c 454-397T/T is associated with increased risk of hemorrhagic stroke, with a synergistic relationship between this genotype and hypertension. In experimental stroke settings estrogens influence recovery of cognitive functions, possibly via induction of neurotrophic factors and specific transcription factors including NGFI-A. This may be related to increased neuroplasticity in the hippocampal formation, a key area for memory processing. Individualized treatment with estrogen receptor ...
TY - JOUR. T1 - Expression of estrogen receptor gene in mouse oocyte and during embryogenesis. AU - Wu, T. C J. AU - Wang, L.. AU - Wan, Yu-Jui Yvonne. PY - 1992. Y1 - 1992. N2 - Estrogen is required for oocyte maturation and embryonic development in vivo; however, the mechanism involved is not clear. Since the effect of estrogen is mediated through the estrogen receptor (ER), we examined the ontogeny and expression of the ER gene in mouse oocytes and embryos of various gestational stages using the highly sensitive reverse transcriptase- polymerase chain reaction (RT-PCR) technique. Total RNA, extracted from 40 ovulated oocytes, 2-cell embryos, morulae, and blastocysts, was reverse transcribed into cDNA. A pair of primers flanking the 453-bp region encoding the hormone-binding domain of ER was used for 30 cycles of PCR. The identity of the amplified product was confirmed by sizing and Southern blot hybridization. The results indicated that ER gene is expressed in unfertilized oocytes and ...
We have previously demonstrated that endoxifen is the most important tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). However, the relevance of ERβ in mediating endoxifen action has yet to be explored. Here, we characterize the molecular actions of endoxifen in breast cancer cells expressing ERβ and examine its effectiveness as an anti-estrogenic agent in these cell lines. MCF7, Hs578T and U2OS cells were stably transfected with full-length ERβ. ERβ protein stability, dimer formation with ERα and expression of known ER target genes were characterized following endoxifen exposure. The ability of various endoxifen concentrations to block estrogen-induced proliferation of MCF7 parental and ERβ-expressing cells was determined. The global gene expression profiles of these two cell lines was monitored following estrogen and endoxifen exposure and biological pathway analysis of these data sets was
TY - JOUR. T1 - Novel estrogen receptor ligands based on an anthranylaldoxime structure. T2 - Role of the phenol-type pseudocycle in the binding process. AU - Minutolo, Filippo. AU - Antonello, Michela. AU - Bertini, Simone. AU - Ortore, Gabriella. AU - Placanica, Giorgio. AU - Rapposelli, Simona. AU - Sheng, Shubin. AU - Carlson, Kathryn E.. AU - Katzenellenbogen, Benita S. AU - Katzenellenbogen, John A.. AU - Macchia, Marco. PY - 2003/9/11. Y1 - 2003/9/11. N2 - The 3,4-diphenylsalicylaldoxime system 1 is an estrogen receptor (ER) ligand of unusual structure, having a hydrogen-bonded pseudocyclic A′-ring in place of the paradigmatic phenolic A-ring that is characteristic of most estrogens. We have investigated the role played by the pseudocycle A′ in binding to the ER by preparing 3,4-diphenylbenzaldoxime (4), a compound that completely lacks this ring but still preserves all of the other features of the original molecule 1, as well as a series of 3,4-diphenylanthranylaldoximes (5a-c) in ...
TY - JOUR. T1 - Synthesis and estrogen receptor affinity of a 4-hydroxytamoxifen-labeled ligand for diagnostic imaging. AU - Lashley, Matthew R.. AU - Niedzinski, Edmund J.. AU - Rogers, Jane M.. AU - Denison, Michael S.. AU - Nantz, Michael H.. PY - 2002/12/1. Y1 - 2002/12/1. N2 - A 10-step synthesis of a novel 4-hydroxytamoxifen-DTPA ligand (HOTam-DTPA) is reported. Tamoxifen and its primary metabolite 4-hydroxytamoxifen are common estrogen receptor ligands. Consequently, tamoxifen has found utility as the targeting component of various diagnostic agents for selective imaging of estrogen receptor-rich tissue, specifically breast cancer. An L-aspartic acid-derived DTPA analogue was attached to the ethyl side chain of 4-hydroxy-tamoxifen using N,N′-dimethylethylenediamine as a hydrophilic linker. A competitve estrogen receptor binding assay using [3H]-17β-estradiol was performed to determine the effect of the ethyl side chain modification on estrogen receptor affinity. The results show that ...
TY - JOUR. T1 - The changes of estrogen receptor-β variants expression in breast carcinogenesis. T2 - Decrease of estrogen receptor-β2 expression is the key event in breast cancer development. AU - Park, Byeongwoo. AU - Kim, Ki Suk. AU - Heo, Min Kyu. AU - Yang, Woo Ick. AU - Kim, Seung Il. AU - Kim, Joo Hang. AU - Kim, Gwi Eon. AU - Lee, Kyong Sik. PY - 2006/5/1. Y1 - 2006/5/1. N2 - Backgound and Objectives: Although more than five variant forms of estrogen receptor-β (ERβ) have been identilied, their role has not been identified. This study was carried out to investigate the changes of ERβ variants in breast cancer development. Methods: Using reverse transcription polymerase chain reaction (RT-PCR) and triple primer PCR (TP-PCR), the expression levels of ERβ variants mRNA were measured in 66 paired normal and cancer tissues. The relative expression level of ERβ variants were compared between normal and cancer tissues, and also compared according to various clinicopathological ...
TY - JOUR. T1 - Estrogen receptor β protects against in vivo injury in RPE cells. AU - Elliot, Sharon J.. AU - Catanuto, Paola. AU - Espinosa-Heidmann, Diego G.. AU - Fernandez, Pedro. AU - Hernandez, Eleut. AU - Saloupis, Peter. AU - Korach, Kenneth. AU - Karl, Michael. AU - Cousins, Scott W.. N1 - Funding Information: This work was supported in part by National Institutes of Health, National Eye Institute Grant RO1 EY1447-04 (SJE, MK, and SWC). PY - 2010/1. Y1 - 2010/1. N2 - Epidemiological data suggest that estrogen deficiency in postmenopausal women may contribute to the severity of AMD. We discovered that 17β-estradiol (E2) was a crucial regulator of the severity of extracellular matrix turnover (ECM) dysregulation both in vivo and in vitro. We also found in vitro that the presence of estrogen receptor (ER)β regulates MMP-2 activity. Therefore in an attempt to delineate the role of the ER subtypes, female estrogen receptor knockout (ERKO) mice were fed a high-fat diet, and the eyes were ...
Background Assess the relation between the presence of PVUII and XBAI polymorphisms in the estrogen receptor alpha gene and mammographic density in postmenopausal women.. Methods For the present analysis, 189 postmenopausal women who had never used hormonal therapy and who did not have clinical or mammographic features were selected. Based on the ACR-BIRADSâ 2003 classification, the mammographic density was determined by three independent readers (two subjective ratings and one computerized - Adobe Photoshop â 7.0 software). Blood samples were available to extract DNA according to KIT GFX â protocol. PCR-RFLP (Polymerase Chain Reaction - Restriction Fragment Length Polymorphism) was then used to identify the polymorphisms.. Results There was a high degree of agreement among the three readers to determine the mammographic density (Kappa,0.75). Sixty women (32%) had dense breasts and 129 (68%) had non-dense breasts. The PVUII polymorphism was found in 132 (69.8%) of 189 women, while the XBAI ...
TY - JOUR. T1 - Abnormal vascular function and hypertension in mice deficient in estrogen receptor β. AU - Zhu, Yan. AU - Bian, Zhao. AU - Lu, Ping. AU - Karas, Richard H.. AU - Bao, Lin. AU - Cox, Daniel. AU - Hodgin, Jeffrey. AU - Shaul, Philip W.. AU - Thorén, Peter. AU - Smithies, Oliver. AU - Gustafsson, Jan Åke. AU - Mendelsohn, Michael E.. PY - 2002/1/18. Y1 - 2002/1/18. N2 - Blood vessels express estrogen receptors, but their role in cardiovascular physiology is not well understood. We show that vascular smooth muscle cells and blood vessels from estrogen receptor β (ERβ) - deficient mice exhibit multiple functional abnormalities. In wild-type mouse blood vessels, estrogen attenuates vasoconstriction by an ERβ-mediated increase in inducible nitric oxide synthase expression. In contrast, estrogen augments vasoconstriction in blood vessels from ERβ-deficient mice. Vascular smooth muscle cells isolated from ERβ-deficient mice show multiple abnormalities of ion channel function. ...
In Silico Prediction of Estrogen Receptor Subtype Binding Affinity and Selectivity Using Statistical Methods and Molecular Docking with 2-Arylnaphthalenes and 2-Arylquinolines. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
There are several potential explanations for the failure of acute hormone replacement therapy to reduce ambulatory ECG ischemia in our study. Although human endothelial cells and smooth muscle cells express estrogen receptors (12,26), Losordo et al. (27)reported that atherosclerotic coronary arteries expressed fewer estrogen receptors than coronary arteries without significant atherosclerosis. Furthermore, Post et al. (28)reported increased rates of estrogen receptor gene promoter methylation with increasing age, both in nondiseased vessels and even more so in areas with atherosclerotic plaque. Increased promoter methylation inactivates estrogen receptor gene transcription. Since women with UA are usually elderly with significant atherosclerosis, they may be unresponsive to hormone therapy due to lack of the estrogen receptor. It also is possible that the concurrent use of nitroglycerin in three-quarters of our patients resulted in maximal endothelial-independent coronary vasodilation, thus ...
Dyslexia, or specific reading disability, is the unexpected failure in learning to read and write when intelligence and senses are normal. One of the susceptibility genes, DYX1C1, has been implicated in neuronal migration, but little is known about its interactions and functions. As DYX1C1 was suggested to interact with the U-box protein CHIP (carboxy terminus of Hsc70-interacting protein), which also participates in the degradation of estrogen receptors alpha (ERalpha) and beta (ERbeta), we hypothesized that the effects of DYX1C1 might be at least in part mediated through the regulation of ERs. ERs have shown to be important in brain development and cognitive functions. Indeed, we show that DYX1C1 interacts with both ERs in the presence of 17beta-estradiol, as determined by co-localization, co-immunoprecipitation and proximity ligation assays. Protein levels of endogenous ERalpha or exogenous ERbeta were reduced upon over-expression of DYX1C1, resulting in decreased transcriptional responses to ...
Estrogen Receptors Inhibitors on signaling pathway are available at Adooq Bioscience. Check Estrogen Receptors pathway , inhibitors reviews and assay information.
TY - JOUR. T1 - Membrane estrogen receptors in GH3/B6 cells are associated with rapid estrogen-induced release of prolactin. AU - Pappas, T. C.. AU - Gametchu, B.. AU - Yannariello-Brown, J.. AU - Collins, T. J.. AU - Watson, C. S.. PY - 1994. Y1 - 1994. UR - http://www.scopus.com/inward/record.url?scp=0028008304&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0028008304&partnerID=8YFLogxK. M3 - Article. AN - SCOPUS:0028008304. VL - 2. SP - 813. EP - 822. JO - Endocrine. JF - Endocrine. SN - 0969-711X. IS - 9. ER - ...
Epidemiological, clinical and animal studies revealed that sex differences exist in the manifestation and outcome of cardiovascular disease (CVD). The underlying molecular mechanisms implicated in these sex differences are not fully understood. The reasons for sex differences in CVD are definitely multifactorial, but major evidence points to the contribution of sex steroid hormone, 17β-estradiol (E2), and its receptors, estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). In this review, we summarize past and present studies that implicate E2 and ER as important determinants of sexual dimorphism in the physiology and pathophysiology of the heart. In particular, we give an overview of studies aimed to reveal the role of E2 and ER in the physiology of the observed sex differences in CVD using ER knock-out mice. Finally, we discuss recent findings from novel transgenic mouse models, which have provided new information on the sexual dimorphic roles of ER specifically in cardiomyocytes ...
Phosphorylation of estrogen receptor alpha at serine 305 (ER alpha S305-P) by protein kinase A (PKA) or p21-activated kinase 1 (PAK1) has experimentally been associated with tamoxifen sensitivity. Here, we investigated the clinical application of this knowledge to predict tamoxifen resistance in ER-positive breast cancer patients. Using immunohistochemistry, a score including PAK1 and co-expression of PKA and ER alpha S305-P (PKA/ER alpha S305-P) was developed on a training set consisting of 103 patients treated with tamoxifen for metastatic disease, and validated on 231 patients randomized between adjuvant tamoxifen or no treatment. In the training set, PAK1 levels were associated with tumor progression after tamoxifen (HR 1.57, 95% CI 0.99-2.48), as was co-expression of PKA and ER alpha S305-P (HR 2.00, 95% CI 1.14-3.52). In the validation set, a significant tamoxifen benefit was found among the 73% patients negative for PAK1 and PKA/ER alpha S305-P (HR 0.54, 95% CI 0.34-0.87), while others ...
Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects. - Mechanism of Action & Protocol.
Previous microarray studies on breast cancer identified multiple tumour classes, of which the most prominent, named luminal and basal, differ in expression of the oestrogen receptor alpha gene (ER). We report here the identification of a group of breast tumours with increased androgen signalling and a molecular apocrine gene expression profile. Tumour samples from 49 patients with large operable or locally advanced breast cancers were tested on Affymetrix U133A gene expression microarrays. Principal components analysis and hierarchical clustering split the tumours into three groups: basal, luminal and a group we call molecular apocrine. All of the molecular apocrine tumours have strong apocrine features on histological examination (P=0.0002). The molecular apocrine group is androgen receptor (AR) positive and contains all of the ER-negative tumours outside the basal group. Kolmogorov-Smirnov testing indicates that oestrogen signalling is most active in the luminal group, and androgen ...
Aretrospective study comparing the estrogen receptor (ER) alpha subtype and progesterone receptor (PR) profile of breast carcinomas amongst 1625 cases over 2.5 years was carried out. Strictly speaking it is generally believed that breast carcinomas can biochemically express PR only if they are ER-positive. However, a few ERalpha-PR+ cases do exist paradoxically. This class of tumors was the focus of our study in which we looked at the possible reasons for such an immunophenotype and compared it with a group of ERalpha+PR+ breast carcinomas. An internationally recognized immunohistochemical method employing monoclonal antibodies against estrogen and progesterone receptors was used. Correlations with established risk factors i.e. menopausal status, grade, tumor size and lymph node status were analyzed for our study group (ERalpha-PR+) and compared with a control (ERalpha+PR+). Out of the total 1625 cases, 29.91% (486) were ERalpha+PR+, 5.11% (83) were ERalpha+PR-, 56.86% (924) were ERalpha-PR- and 8.12%
The estrogen receptor alpha (ERα) is the central transcriptional regulator of ductal mammary epithelial lineage specification and is an important p...
The vascular consequences of estrogen treatment may be driven by its initiation timing. We tested the hypothesis that the duration of ovarian hormone deprivation before estrogen reintroduction affects the role of estrogen as mediator of endothelial f
SUMMARY, EXPLANATION AND LIMITATIONS:. Recognizes a protein of 67kDa, which is identified as estrogen receptor (ER) alpha. The ER gene consists of more than 140kb of genomic DNA divided into 8 exons, being translated into a protein with six functionally discrete domains, labeled A through F. This antibody strongly stains the nucleus of epithelial cells in breast carcinomas. The ER is an important regulator of growth and differentiation in the mammary gland. Presence of ER in breast tumors indicates an increased likelihood of response to anti-estrogen (e.g. tamoxifen) therapy.. Clone: SP1. Isotype: IgG. Immunogen: Synthetic peptide derived from C-terminal of human estrogen receptor.. Staining pattern: Nuclear.. Positive control: Tissue sample breast carcinoma.. APPLICATIONS:. This antibody is designed for the specific localization of human ER using IHC techniques in formalin-fixed, paraffin-embedded tissue sections.. The antibody identify ER in normal or neoplastic cells and reacts positively ...
Estrogen (E2) is a major risk factor for the initiation and progression of malignancy in estrogen receptor (ER) positive breast cancers, whereas sirtuin 3 (Sirt3), a major mitochondrial NAD+-dependent deacetylase, has the inhibitory effect on the tumorigenic properties of ER positive MCF-7 breast cancer cells. Since it is unclear if this effect is mediated through the estrogen receptor alpha (ERα) signaling pathway, in this study, we aimed to determine if the tumor-suppressive function of Sirt3 in MCF-7 cells interferes with their response to E2. Although we found that Sirt3 improves the antioxidative response and mitochondrial fitness of the MCF-7 cells, it also increases DNA damage along with p53, AIF, and ERα expression. Moreover, Sirt3 desensitizes cells to the proliferative effect of E2, affects p53 by disruption of the ERα–p53 interaction, and decreases proliferation, colony formation, and migration of the cells. Our observations indicate that these tumor-suppressive
in Trabajos del Instituto Cajal (2009), LXXXII. Steroid receptors such as estrogen receptors alpha and beta and androgen receptors are transcription factors involved in the transcriptional regulation of a large number of target genes. Steroid-dependent ... [more ▼]. Steroid receptors such as estrogen receptors alpha and beta and androgen receptors are transcription factors involved in the transcriptional regulation of a large number of target genes. Steroid-dependent expression in the brain controls a large array of biological processes including spatial cognition, copulatory behavior and neuroprotection. The discovery of a competition, or squelching, between two different nuclear receptors introduced the notion that common cofactors might be involved in the modulation of transcriptional activity of nuclear receptors. These cofactors, which are now known as coactivators, are involved in chromatin remodeling and stabilization of the general transcription machinery. Since the characterization of ...
MICHAEL PHELPS: PET molecular imaging probes can rapidly search for cancer throughout all tissues of the body, as well as characterize each cancer lesion it detects within an individual patient. Tumors can change their biological properties as they metastasize, so there is a need to characterize the initial tumor and each metastasis. For example, a patient with breast cancer can first present a tumor in the breast tissue with estrogen receptors, but then develop metastases that may or may not have estrogen receptors. Those metastases with estrogen receptors will likely respond to hormonal therapy, while those without estrogen receptors will not respond. About 40 percent of metastases have a different estrogen receptor status than the primary tumor from which they spread. Whole body PET imaging reveals the estrogen receptors in patients, lesion by lesion, to better determine whether response to hormonal therapy will be effective for all lesions. All cancer treatments are in need of better ...
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ER-alpha and ER-beta function as transcription factors to modulate expression of target genes. Both interact with nuclear regulatory proteins to enhance or inhibit transcription. We hypothesized that these co-regulators are expressed in breast cancer tissue and may be differentially regulated by estrogen and tamoxifen.. ER-alpha, ER-beta, the co-activator SRC-1, and the co-repressor SMRT were localized within breast tissue by immunohistochemistry, and the spatial co-expression assessed by immunofluoresence. The ability of beta-estradiol and 4-hydroxytamoxifen (4-HOT) to modulate the protein of ER-alpha, ER-beta, SRC-1, and SMRT in primary cell cultures, and MCF-7 and T47-D cell lines was assessed by western blotting.. ER-alpha and ER-beta were found to be co-expressed with the co-regulators SRC-1 and SMRT in the nuclei of breast cancer epithelial cells. Partial and complete response elements for the ER were identified on the promotor region of ER-alpha, ER-beta, SRC-1 and SMRT. Beta-estradiol ...
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of
To address globally the issue of tissue specificity of ER ligands, Duke scientists have developed a transgenic mouse that functions as a reporter of ER activity, termed ERIN (estrogen receptor action indicator). ERIN provides a model system that can be used to identify tissues and cells that contain functionally active ER and to define their ability to respond to different ER-ligands. This model system integrates the upstream requirements in ER action (including ER itself, ligand, and accessory comodulators) and results in expression of the enzyme P-galactosidase b-gal) that allows for enzymatic amplification of the signal and histological localization. After a systematic evaluation of seven different estrogen responsive reporters, (3XERE-tk-ZacZ) with the highest absolute level of induction was selected.. ...
This study investigates the molecular mechanisms by which critical genes are differentially regulated in the male and female brain. The hormone, estrogen, is cr...
To develop novel estrogen receptor (ER) ligands, ring-fused derivatives of the hormonally active (1R,2S)/(1S,2R)-1-(2-chloro-4-hydroxyphenyl)-2-(2,6-dichloro-4-hydroxyphenyl)ethylenediamine 4b were synthesized. (2R,3S)/(2S,3R)-2-(2-Chloro-4-hydroxyphenyl)-3-(2,6-dichloro-4-hydroxyphenyl)piperazine 4 induced ligand-dependent gene expression in MCF-7-2a cells, stably transfected with the plasmid ERE(wtc)luc and was therefore used as a lead structure. The influence of the substitution pattern in the aromatic rings (4-OH (1), 2-F,4-OH (2), 2-Cl,4-OH (3), 2,6-Cl2,3-OH (5), and 2,6-Cl2,4-OH (6)) and the effect of N-ethyl chains on the ER binding and activation of gene expression were studied. The synthesis started from the respective methoxy-substituted (1R,2S)/(1S,2R)-configurated 1,2-diarylethylenediamines 6b to 4b, which were reacted with dimethyl oxalate in order to get 5,6-diarylpiperazine-2,3-diones. Reduction with BH3*tetrahydrofuran and ether cleavage with BBr3 yielded the piperazines 1-6. The N
Figure 3 Thermogenic program and β3-adrenergic receptor signaling is mediated by membrane-initiated ERα signaling. A: Immunoblot analysis of UCP1 levels in BAT and pWAT of ERα+/+, ERα−/−, WT, and KRRki/ki mice. Representative immunoblots and quantification are shown (n = 5-8 per group). #P , 0.01. B: qRT-PCR analysis of genes consistent with beige adipocytes in adipose tissues of ERα+/+, ERα−/−, WT, and KRRki/ki mice (n = 6-8). Relative mRNA expression levels are normalized to gapdh. *P , 0.05, #P , 0.01. C: Hematoxylin and eosin staining of pWAT of ERα+/+, ERα−/−, WT, and KRRki/ki mice. Scale bar indicates 100 µm. The graph depicts the quantification of mean cell area (n = 4). #P , 0.01. D: qRT-PCR analysis of genes consistent with beige adipocytes in NIH 3T3-L1 preadipocytes treated with vehicle (control), 100 nmol/L E2, or 2 µmol/L rosiglitazone for 72 h. Relative mRNA expression levels are normalized to gapdh. Data depict the results from three independent experiments. ...
Berkeley Lab researchers have developed the first clinically-relevant mouse model of human breast cancer to successfully express functional estrogen receptor positive adenocarcinomas. This model should be a powerful tool for testing therapies for aggressive ER+ breast cancers and for studying luminal cancers -- the most prevalent and deadliest forms of breast cancer.
Trial finds estrogen receptor degrader significantly increases progression-free survival in patients with advanced breast cancer.
Communications DOI: 10.1002/anie.201101655 DNA Complexes DNA-Controlled Bivalent Presentation of Ligands for the Estrogen Receptor** Frank Abendroth, Alexander Bujotzek, Min Shan, Rainer Haag, Marcus Weber, and Oliver Seitz* The assembly of DNA complexes proceeds according to known rules. Thus, the mutual recognition of DNA conjugates can be used for the precise positioning of functional groups. For example, chromophores,[1] metals,[2] catalytic units,[3] nanoparticles,[4] fluorophores[5] and even proteins[6] have been arranged at well-defined distances by means of DNA hybridization. Until recently, the main interest was focused on issues within materials science as well as on the immobilization of biomolecules. We and others assumed that the ability to position functional units at defined distances could also be used to address biological problems.[7] According to this, DNA may serve as a molecular ruler to determine the distance between binding pockets in biological receptors. Due to ...
mouse anti-estrogen receptor alpha, ligand binding domain (aa 304-554) hybridoma (ERalpha BZ1) is an eagle-i resource of type Hybridoma cell line at eagle-i Network Shared Resource Repository.
First estrogen eeceptor-α mutation identified in a young woman. A receptor mutation that essentially blocks estrogens action has been identified in a female.
Researchers then monitored the response of estrogen receptor-alpha (ERa) - the bodys main bone-related mediator of the hormone - to the estradiol. In particular, the group wanted to know whether the inhibition of one of the ERas two activation functions, known as AF-1 and AF-2, would redirect estrogen to specific tissues ...
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Hormones are vital to our health and vitality. One hormone that is vitally important for many reasons is estrogen. Physical functions and other biochemical parameters are affected with the amount of estrogen found in the body.. In women, estrogen is important during the time frame of puberty. It decelerates height increase, accelerates body fat burning, and reduces muscle bulk. It assists in regulating the menstrual cycle and developing breasts. It helps reduce bone re-absorption and increase bone formation. Good cholesterol (HDL) and triglycerides are increased through estrogen. LDL (bad cholesterol) is lowered and increased fat deposition is a result of having a good level of estrogen. Collagen content and quality is admired through the assistance of estrogen. It helps increase skin thickness and improves blood supply to the skin.. Fluctuating estrogen levels during the transition to menopause can take a toll on your health. There can be: ...
"Antagonists selective for estrogen receptor alpha". Endocrinology. 143 (3): 941-7. doi:10.1210/endo.143.3.8704. PMID 11861516. ... antiestrogens with estrogen receptor alpha selective activity". Bioorganic & Medicinal Chemistry Letters. 19 (1): 108-10. doi: ... Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50-. ISBN 978-3-527-62330-3. ... and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor. It has 200- ...
Yamamoto Y, Moore R, Hess H, Guo G, Gonzalez F, Korach K, Maronpot R, Negishi M (2006). "Estrogen receptor alpha mediates ...
LXA4 binds to and activates estrogen receptor alpha. In this capacity, it mimics an estrogenic molecule to stimulate human ... Russell R, Gori I, Pellegrini C, Kumar R, Achtari C, Canny GO (Dec 2011). "Lipoxin A4 is a novel estrogen receptor modulator". ... FPR2, which is now termed the ALX, ALX/FPR, or ALX/FPR2 receptor, is a G protein coupled receptor initially identified as a ... LXA4 and 15-epi-LXA4 are high affinity receptor ligands for and activators of the FPR2 receptor. ...
"ADA3-containing complexes associate with estrogen receptor alpha". Nucleic Acids Research. 30 (11): 2508-14. doi:10.1093/nar/ ... TADA3L has been shown to interact with: Retinoic acid receptor alpha, Retinoid X receptor alpha, TADA2L, TAF9, Transcription ... "Human ADA3 binds to estrogen receptor (ER) and functions as a coactivator for ER-mediated transactivation". The Journal of ... "Human papilloma virus 16 E6 oncoprotein inhibits retinoic X receptor-mediated transactivation by targeting human ADA3 ...
"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". ... However, in contrast to androstenediol, its affinity for the estrogen receptors is very low, with less than 0.01% of the ... Thus, theca cells and granulosa cells work together to form estrogens. Androstanedione is a 5α-reduced metabolite of 4- ...
Yamamoto Y, Moore R, Hess H, Guo G, Gonzalez F, Korach K, Maronpot R, Negishi M (2006). "Estrogen receptor alpha mediates ... Marcus R, Korenman S (1976). "Estrogens and the human male". Annu Rev Med. 27: 357-70. doi:10.1146/annurev.me.27.020176.002041 ... which is usually caused by high levels of circulating estrogen), may arise because of increased conversion of testosterone to ... estrogen by the enzyme aromatase. Reduced sexual function and temporary infertility can also occur in males. Another male- ...
ERalpha Estrogen receptor alpha GRCh38: Ensembl release 89: ENSG00000118046 - Ensembl, May 2017 GRCm38: Ensembl release 89: ... In contrast, 17β-estradiol treatment increased LKB1 mRNA, an effect mediated by oestrogen receptor alpha. However, in ER- ... Nath-Sain S, Marignani PA (June 2009). "LKB1 catalytic activity contributes to estrogen receptor alpha signaling". Molecular ... murine 3T3-L1 or human SGBS adipocytes for 24 h significantly decreased the mRNA expression of LKB1 via the androgen receptor ...
Gburcik V, Bot N, Maggiolini M, Picard D (May 2005). "SPBP is a phosphoserine-specific repressor of estrogen receptor alpha". ...
... has been shown to interact with Estrogen receptor alpha. ISL1 is a marker for cardiac progenitors of the secondary heart ... Gay F, Anglade I, Gong Z, Salbert G (2001). "The LIM/homeodomain protein islet-1 modulates estrogen receptor functions". Mol. ... "The LIM/homeodomain protein islet-1 modulates estrogen receptor functions". Mol. Endocrinol. 14 (10): 1627-48. doi:10.1210/me. ...
... has been shown to interact with Estrogen receptor alpha. GRCh38: Ensembl release 89: ENSG00000131263 - Ensembl, May 2017 ... "Regulation of estrogen-dependent transcription by the LIM cofactors CLIM and RLIM in breast cancer". Cancer Res. 69 (1): 128-36 ...
... has been shown to interact with Estrogen receptor alpha. GRCh38: Ensembl release 89: ENSG00000067334 - Ensembl, May ... a novel estrogen receptor binding protein enhancing the activity of estrogen receptor". Biochem Biophys Res Commun. 317 (1): 54 ...
"Cyclin D1 antagonizes BRCA1 repression of estrogen receptor alpha activity". Cancer Research. 65 (15): 6557-67. doi:10.1158/ ... Independent of CDK, cyclin D1 binds to nuclear receptors (including estrogen receptor α, thyroid hormone receptor, PPARγ and AR ... "Ligand-independent recruitment of steroid receptor coactivators to estrogen receptor by cyclin D1". Genes & Development. 12 (22 ... "P/CAF associates with cyclin D1 and potentiates its activation of the estrogen receptor". Proceedings of the National Academy ...
... has been shown to interact with estrogen receptor alpha. Unfolded protein response GRCh38: Ensembl release 89: ... "Ligand-independent activation of estrogen receptor alpha by XBP-1". Nucleic Acids Research. 31 (18): 5266-74. doi:10.1093/nar/ ... DR alpha. The expression of this protein is required for the transcription of a subset of class II major histocompatibility ... "An HLA-DR alpha promoter DNA-binding protein is expressed ubiquitously and maps to human chromosomes 22 and 5". Immunogenetics ...
Gururaj AE, Peng S, Vadlamudi RK, Kumar R (August 2007). "Estrogen induces expression of BCAS3, a novel estrogen receptor-alpha ... Gururaj AE, Peng S, Vadlamudi RK, Kumar R (2007). "Estrogen induces expression of BCAS3, a novel estrogen receptor-alpha ... The BCAS3 gene is regulated by estrogen receptor alpha (ER-α). The PELP1 protein acts as a transcriptional coactivator of ... estrogen receptor induced BCAS3 gene expression. In addition BCAS3 possesses histone acetyltransferase activity and itself ...
"Formononetin promotes angiogenesis through the estrogen receptor alpha-enhanced ROCK pathway". Scientific Reports. 5: 16815. ... "Red Clover Isoflavones Biochanin A and Formononetin are Potent Ligands of the Human Aryl Hydrocarbon Receptor". The Journal of ...
In a particular study, patients with end-stage dilated cardiomyopathy showed almost doubled estrogen receptor alpha (ER-alpha) ... "Estrogen receptor alpha up-regulation and redistribution in human heart failure". FASEB Journal. 20 (7): 926-34. doi:10.1096/fj ... This way receptor-bound axin will abolish mediating the phosphorylation of β-catenin. Since beta-catenin is no longer marked ... Although the precise details are much less clear, it appears that the same site is used by alpha-catenin when beta-catenin is ...
November 2009). "An oestrogen-receptor-alpha-bound human chromatin interactome". Nature. 462 (7269): 58-64. Bibcode:2009Natur. ... This assay was used to show that estrogen induces an interaction between the prolactin gene promoter and a nearby enhancer. In ...
"DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ... 7α-OH-DHEA has weak estrogenic activity, selectively activating the estrogen receptor ERβ. In addition, 7α-OH-DHEA may be ... "Increased total 7 alpha-hydroxy-dehydroepiandrosterone in serum of patients with Alzheimer's disease". J. Gerontol. A Biol. Sci ...
"DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ... 7β-OH-DHEA has weak antiestrogenic activity, selectively antagonizing the estrogen receptor ERβ. 7β-OH-DHEA is on the World ...
"DHEA metabolites activate estrogen receptors alpha and beta". Steroids. 78 (1): 15-25. doi:10.1016/j.steroids.2012.10.002. PMC ...
Estrogen (alpha and beta) and androgen receptor-mediated responses in yeast assays.. ...
2003). "Transcriptional suppression of the estrogen receptor by truncated estrogen receptor-alpha". Horm. Metab. Res. 34 (8): ... and 4 differentially regulate signaling via the Galphaq/11-linked muscarinic M3 receptor". Mol. Pharmacol. 66 (6): 1453-64. doi ...
miR-26a also directly suppresses expression of estrogen receptor alpha (Erα). Overexpression of miR-26a brings about negative ... and peroxisome proliferator-activated receptor δ. Depletion of β-catenin partially prevents miR-26a-induced tumor cell ...
Mo R, Rao SM, Zhu YJ (June 2006). "Identification of the MLL2 complex as a coactivator for estrogen receptor alpha". The ... Increased KMT2D was shown to facilitate chromatin opening and recruitment of transcription factors, including estrogen receptor ... The protein also contains six N-terminal PHDs, a high mobility group (HMG-I), and nine nuclear receptor interacting motifs ( ... of the hepatic circadian clock and are co-activators of the circadian transcription factors retinoid-related orphan receptor ( ...
... has been shown to interact with Estrogen receptor alpha and SAFB. GRCh38: Ensembl release 89: ENSG00000130254 - Ensembl, ... a new scaffold attachment factor homolog and estrogen receptor corepressor". J. Biol. Chem. 278 (22): 20059-68. doi:10.1074/jbc ...
"An acetylation switch modulates the transcriptional activity of estrogen-related receptor alpha". Mol. Endocrinol. 24 (7): 1349 ... Histone deacetylase 8 is involved in skull morphogenesis and metabolic control of the ERR-alpha / PGC1-alpha transcriptional ... ERR-alpha. Histone deacetylase GRCh38: Ensembl release 89: ENSG00000147099 - Ensembl, May 2017 GRCm38: Ensembl release 89: ... 2006). "Histone deacetylase HDAC8 associates with smooth muscle alpha-actin and is essential for smooth muscle cell ...
Sentis S, Le Romancer M, Bianchin C, Rostan MC, Corbo L (2005). "Sumoylation of the estrogen receptor alpha hinge region ... Wang LH, Yang XY, Mihalic K, Xiao W, Li D, Farrar WL (Aug 2001). "Activation of estrogen receptor blocks interleukin-6- ... SMAD and estrogen receptor. PIAS3 protein also functions as a SUMO (small ubiquitin-like modifier)-E3 ligase which catalyzes ... inducible cell growth of human multiple myeloma involving molecular cross-talk between estrogen receptor and STAT3 mediated by ...
... has been shown to interact with Estrogen receptor alpha and HNRPUL1. GRCh38: Ensembl release 89: ENSG00000160310 - ... 2002). "Identification of protein arginine methyltransferase 2 as a coactivator for estrogen receptor alpha". J. Biol. Chem. ... "Identification of protein arginine methyltransferase 2 as a coactivator for estrogen receptor alpha". J. Biol. Chem. United ...
Estrogen-related receptor alpha 1 up-regulates endothelial nitric oxide synthase expression. Proc. Natl. Acad. Sci. USA 100: ... Rapid nitric oxidemediated S-nitrosylation of estrogen receptor: Regulation of estrogen-dependent gene transcription. Proc. ... 1987, 1988, 1989, 1990, 1991, 1992, 1993, 1994, 1995, 1996, 1997, 1999 Alpha Omega Alpha - Honorary Member. 1990 UCLA School of ...
In mammals, miR-206 is a crucial regulator of estrogen-receptor-alpha. Non-coding RNAs are crucial in the development of ... miR-206 targets the human estrogen receptor-alpha (ERalpha) and represses ERalpha messenger RNA and protein expression in ... However, a handful of other bifunctional RNAs are known to exist (e.g., steroid receptor activator/SRA, VegT RNA, Oskar RNA, ... Kishore S, Stamm S (January 2006). "The snoRNA HBII-52 regulates alternative splicing of the serotonin receptor 2C". Science. ...
Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... These gene candidates include certain variations in tumor necrosis factor-alpha (TNF-alpha), IL-1 alpha, and CYP1A1 genes, ... C. acnes' ability to bind and activate a class of immune system receptors known as toll-like receptors (TLRs), especially TLR2 ... LTB4 promotes skin inflammation by acting on the peroxisome proliferator-activated receptor alpha (PPARα) protein.[45] PPARα ...
T4 and T3 bind to thyroid receptor proteins in the cell nucleus and cause metabolic effects through the control of DNA ...
Elliott J (1997). "Alpha-adrenoceptors in equine digital veins: evidence for the presence of both α1 and α2-receptors mediating ... Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ... Alfa-2 (α2) adrenergički receptor (ili adrenoceptor) je G protein-spregnuti receptor koji vezuje Gi heterotrimerni G protein. ...
... but not estrogens, increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... Again it was noted that AHN was not increase via activation of the estrogen receptors.[13] ...
... activities by activating estrogen receptors. Quercetin activates both estrogen receptor alpha (ERα) and beta (ERβ)[23] with ... "Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).[26][27] ... "The stimulation of cell proliferation by quercetin is mediated by the estrogen receptor". (primary). Molecular Nutrition & Food ...
... and are analogous to selective estrogen receptor degraders (SERDs) like fulvestrant (a drug used to treat estrogen receptor- ... R 1881 binding to the prostatic androgen receptor and [3H]5 alpha-dihydrotestosterone and [3H]cortisol binding to plasma ... Androgen receptor degradersEdit. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... and estrogens like estradiol, estradiol esters, ethinylestradiol, conjugated estrogens, diethylstilbestrol, and bifluranol.[2][ ...
"Estrogen receptor alpha interacts with mitochondrial protein HADHB and affects beta-oxidation activity". Molecular & Cellular ... The genes of the alpha and beta subunits of the mitochondrial trifunctional protein are located adjacent to each other in the ... 2004). "General mitochondrial trifunctional protein (TFP) deficiency as a result of either alpha- or beta-subunit mutations ... and the interaction may play an important role in the estrogen-mediated lipid metabolism in animals and humans.[14] ...
第三亚族(甾类激素(英语:Steroid hormone receptor)(雄激素、雌激素(α、β)、糖皮质激素、盐皮质激素、孕酮)、雌激素相关(英语:Estrogen related receptor)(α、β、γ)). 第四亚族NUR(英语:Nur ... 第一亚族:甲状腺激素受体(英语:Thyroid hormone receptor)(α、β)、CAR、FXR
It may also modulate the activity of various neurotransmitter receptors, including the Alpha-7 nicotinic receptor.[27] BDNF has ... The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... receptor binding. • neurotrophin TRKB receptor binding. • growth factor activity. • GO:0001948 protein binding. ... regulation of receptor activity. • activation of phospholipase C activity. • neurotrophin TRK receptor signaling pathway. • ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... 1999). „Cloning and characterization of a rabbit ortholog of human Galpha16 and mouse G(alpha)15.". FEBS Lett. 460 (1): 53-6. ... Nociceptinski receptor (NOP, orfaninski FQ receptor, kapa tip 3 opioidni receptor) je protein koji je kod čoveka kodiran OPRL1 ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Firstly, oestrogen is used in tablet or gel form in order to maximise breast development, then a combination of oestrogen and ... Kisspeptin and its associated receptor KISS1R are known to be involved in the regulation of puberty. Studies have shown there ... Alpha-thalassemia mental retardation syndrome. *Siderius X-linked mental retardation syndrome. *Eye disorders: Color blindness ... Oestrogen (females) or testosterone (males) is essential for maintaining bone density.[18] Deficiency in either testosterone or ...
2005). „Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids". Mol. ... Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... G protein spregnuti receptor familija C group 6 član A je protein koji je kod ljudi kodiran GPRC6A genom.[1] Ovaj receptor ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Ribociclib are US FDA approved CDK4 and CDK6 inhibitors for the treatment of estrogen receptor positive/ HER2 negative advanced ... Receptor protein serine/threonine kinase (EC 2.7.11.30). *Bone morphogenetic protein receptors *BMPR1 ... regulation of insulin receptor signaling pathway. • regulation of lipid biosynthetic process. • regulation of lipid catabolic ...
σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... Women starting an estrogen-containing oral contraceptive may need to increase the dosage of lamotrigine to maintain its level ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
... which is caused by a defective estrogen receptor (ER) - specifically, the estrogen receptor alpha (ERα) - that results in an ... EIS results when the function of the estrogen receptor alpha (ERα) is impaired. The ERα protein (pictured) mediates most of the ... Estrogen insensitivity syndrome (EIS), or estrogen resistance, is a form of congenital estrogen deficiency or hypoestrogenism[2 ... "Estrogen resistance caused by a mutation in the estrogen-receptor gene in a man". N. Engl. J. Med. 331 (16): 1056-61. doi: ...
Premarin (conjugated estrogens, introduced in 1942) and Prempro (a combination estrogen-progestin pill, introduced in 1995) ... General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... antifungal, alkalinizing agents, quinolones, antibiotics, cholinergics, anticholinergics, antispasmodics, 5-alpha reductase ... Doctors prescribe estrogen for their older female patients both to treat short-term menopausal symptoms and to prevent long- ...
receptor ligand activity. Cellular component. • extracellular region. • platelet alpha granule lumen. • extracellular. ... IGF-2 exerts its effects by binding to the IGF-1 receptor and to the short isoform of the insulin receptor (IR-A or exon 11-).[ ... 8] IGF2 may also bind to the IGF-2 receptor (also called the cation-independent mannose 6-phosphate receptor), which acts as a ... insulin receptor binding. • hormone activity. • GO:0001948 protein binding. • growth factor activity. • insulin-like growth ...
The ACTH receptor is a seven-membrane-spanning G protein-coupled receptor.[7] Upon ligand binding, the receptor undergoes ... melanotropin alpha. melanocyte-stimulating hormone. α-MSH. 138-150 corticotropin-like intermediate peptide. CLIP. 156-176 ... A family of related receptors mediates the actions of these hormones, the MCR, or melanocortin receptor family. These are ... ACTH receptors outside the adrenal gland[edit]. As indicated above, ACTH is a cleavage product of the pro-hormone, ...
... the androgen receptor, and the vitamin D receptor.[26] TMPRSS2-ETS gene family fusion, specifically TMPRSS2-ERG or TMPRSS2-ETV1 ... Alpharadin uses bone targeted Radium-223 isotopes to kill cancer cells by alpha radiation.[183][unreliable medical source?] It ... In 1941, Charles B. Huggins published studies in which he used estrogen to oppose testosterone production in men with ... GnRH receptor agonists, such as leuprolide and goserelin, were subsequently developed and used to treat prostate cancer.[171][ ...
... of exogenous epidermal-like growth factors on mammary gland development and differentiation in the estrogen receptor-alpha ... and not exogenous human prolactin induces estrogen receptor α and prolactin receptor expression and increases estrogen ... "Delayed Puberty and Estrogen Resistance in a Woman with Estrogen Receptor α Variant". New England Journal of Medicine. 369 (2 ... "Testosterone inhibits estrogen-induced mammary epithelial proliferation and suppresses estrogen receptor expression". FASEB J. ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat • ... "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.". Proc. Natl. Acad ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... 1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ...
2003). "Transcriptional regulation of human CYP3A4 basal expression by CCAAT enhancer-binding protein alpha and hepatocyte ... Testicular receptor *2. *4. *TLX. subfamily 3. *Steroid hormone *Androgen. *Estrogen *α ... "Assignment of the human genes for hepatocyte nuclear factor 3-alpha, -beta, and -gamma (HNF3A, HNF3B, HNF3G) to 14q12-q13, ...
Desai MA, Burnett JP, Mayne NG, Schoepp DD (1995). „Cloning and expression of a human metabotropic glutamate receptor 1 alpha: ... Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... Metabotropni glutamatni receptor. Spoljašnje veze[уреди]. *. „Metabotropic Glutamate Receptors: mGlu1". IUPHAR Database of ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
... an alpha chain and a beta chain. LH and FSH share nearly identical alpha chains (about 100 amino acids long), whereas the beta ... Gonadotropin receptors are embedded in the surface of the target cell membranes and coupled to the G-protein system. Signals ... where constantly high and progressively-increasing levels of hCG circulate and mediate production of estrogen and progesterone ... The alpha subunit is common to each protein dimer (well conserved within species, but differing between them[5]), and a unique ...
... predicts site-specific relapse in oestrogen receptor-positive primary breast carcinomas". British Journal of Cancer. 107 (2): ... "Entrez Gene: Calcium channel, voltage-dependent, alpha 2/delta subunit 3". مؤرشف من الأصل في 3 نوفمبر 2016. الوسيط ,تاريخ ... "Molecular cloning and characterization of the human voltage-gated calcium channel alpha(2)delta-4 subunit". Molecular ...
podfamilija 3 (Steroidni hormon (Androgen, Estrogen (α, β), Glukokortikoid, Mineralokortikoid, Progesteron), Estrogen-vezani (α ... 1994). "Isoform-specific amino-terminal domains dictate DNA-binding properties of ROR alpha, a novel family of orphan hormone ... RAR-srodni orfan receptor beta (ROR-beta), ili NR1F2 (nuklearni receptor potfamilije 1, grupe F, član 2), je nuklearni receptor ... 1996). "Functional analysis of retinoid Z receptor beta, a brain-specific nuclear orphan receptor.". Proc. Natl. Acad. Sci. U.S ...
The first targeted therapies blocked the estrogen receptor molecule, inhibiting the growth of breast cancer. Another common ... "Five-alpha-reductase Inhibitors for prostate cancer prevention". The Cochrane Database of Systematic Reviews (2): CD007091. doi ... the daughters of women who have breast cancer have significantly higher levels of estrogen and progesterone than the daughters ... The benefit versus harm for 5-alpha-reductase inhibitor such as finasteride is not clear.[115] ...
Peroxisome proliferation-activated receptor alpha (PPARα) agonists enhance the activity of the SREBP-1c promoter via a DR1 ... "Human SREBP1c expression in liver is directly regulated by peroxisome proliferator-activated receptor alpha (PPARalpha)". The ... "ADD1/SREBP1c activates the PGC1-alpha promoter in brown adipocytes". Biochimica et Biophysica Acta. 1801 (4): 421-9. doi: ... "SREBP-1, a basic-helix-loop-helix-leucine zipper protein that controls transcription of the low density lipoprotein receptor ...
"Skeletal muscle PGC-1α controls whole-body lactate homeostasis through estrogen-related receptor α-dependent activation of LDH ... The N-terminus is a Rossmann NAD-binding fold and the C-terminus is an unusual alpha+beta fold.[5][6] ... "Skeletal muscle PGC-1α controls whole-body lactate homeostasis through estrogen-related receptor α-dependent activation of LDH ... This consists of a large seven-stranded antiparallel beta-sheet flanked on both sides by alpha-helices. It allows for membrane ...
... is a G protein-coupled receptor that links to and when bound to its CysLT ligands activates the Gq alpha subunit and/or Ga ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes# ...
InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites. We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their individual strengths to produce a powerful integrated database and diagnostic tool.
The human estrogen receptor (hER) exists as two subtypes, hER alpha and hER beta, that differ in the C-terminal ligand-binding ... Interaction of phytoestrogens with estrogen receptors alpha and beta.. Morito K1, Hirose T, Kinjo J, Hirakawa T, Okawa M, ... Isoflavone glycoside binds weakly to both receptors and estrogen receptor-dependent transcriptional expression is poor. The ... Equol induces transcription most strongly with hER alpha and hER beta. The concentration required for maximal gene expression ...
"The aryl hydrocarbon receptor interacts with estrogen receptor alpha and orphan receptors COUP-TFI and ERRalpha1". Arch. ... Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types ... Surmacz E, Bartucci M (2005). "Role of estrogen receptor alpha in modulating IGF-I receptor signaling and function in breast ... Gururaj AE, Peng S, Vadlamudi RK, Kumar R (August 2007). "Estrogen induces expression of BCAS3, a novel estrogen receptor-alpha ...
Substances : Alpha-naphthoflavone, Vitamin C. Diseases : Breast Cancer: Estrogen, Breast Cancer: estrogen receptor alpha- ... estrogen receptor alpha-positive, Breast Cancer: Triple Negative Pharmacological Actions : Apoptotic, Estrogen Receptor ... estrogen receptor alpha-positive. Pharmacological Actions : Antiproliferative , Chemopreventive, Estrogen Receptor Modulators, ... Breast Cancer: estrogen receptor alpha-positive is a Sub of the following Topic. *Breast Cancer: Estrogen ...
Rabbit polyclonal Estrogen Receptor alpha antibody validated for WB, IHC and tested in Human and Mouse. Immunogen corresponding ... Anti-Estrogen Receptor alpha antibody. See all Estrogen Receptor alpha primary antibodies. ... Synthetic peptide within Human Estrogen Receptor alpha conjugated to keyhole limpet haemocyanin. The exact sequence is ... Immunohistochemical analysis of formalin-fixed, paraffin-embedded human breast tissue, staining Estrogen Receptor alpha with ...
Rabbit polyclonal Estrogen Receptor alpha antibody validated for WB, IHC, ICC, Flow Cyt, ICC/IF and tested in Human, Mouse and ... Anti-Estrogen Receptor alpha antibody. See all Estrogen Receptor alpha primary antibodies. ... Anti-Estrogen Receptor alpha antibody (ab3575) at 1/1000 dilution. Lane 1 : Recombinant full-length human Estrogen Receptor ... Recombinant full-length human Estrogen Receptor alpha protein, 125 ng. Lane 3 : Recombinant full-length human Estrogen Receptor ...
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 targets shared by estrogen receptor- related receptors (ERRs) and estrogen receptor (ER) alpha, but not by ... "Transcriptional activities of the orphan nuclear receptor ERR alpha (estrogen receptor-related receptor-alpha)". Molecular ...
The estrogen receptor-alpha-induced microRNA signature regulates itself and its transcriptional response.. Castellano L1, ... Following estrogenic activation, the estrogen receptor-alpha (ERalpha) directly regulates the transcription of target genes via ... The estrogen receptor-α-induced microRNA signature regulates itself and its transcriptional response ... The estrogen receptor-α-induced microRNA signature regulates itself and its transcriptional response ...
Thermal unfolding of estrogen receptors alpha and beta. Sandhya Y. K. Nair, T. J. Thomas, Norma Greenfield, Alex Chen, Huixin ... Thermal unfolding of estrogen receptors alpha and beta. Sandhya Y. K. Nair, T. J. Thomas, Norma Greenfield, Alex Chen, Huixin ... Thermal unfolding of estrogen receptors alpha and beta. Sandhya Y. K. Nair, T. J. Thomas, Norma Greenfield, Alex Chen, Huixin ... Thermal unfolding of estrogen receptors alpha and beta Message Subject (Your Name) has forwarded a page to you from Cancer ...
We hypothesized that alpha isoform of estrogen receptor (ERα) could be involved in the transduction of the vascular benefits of ... Meanwhile evidences in the literature have enlightened, not only structural similarities between estrogens and polyphenols ...
Invitrogen Anti-Estrogen Receptor alpha Monoclonal (33), Catalog # MA1-310. Tested in Western Blot (WB), Immunofluorescence (IF ... estrogen nuclear receptor alpha; Estrogen receptor; estrogen receptor 1 (alpha); estrogen receptor alpha; estrogen receptor ... estrogen receptor alpha E1-E2-1-2; estrogen receptor alpha E1-N2-E2-1-2; estrogen receptor alpha splice variant, CTERP-1; ... estrogen receptor alpha splice variant, ERalphai56; estrogen receptor alpha splice variant, ERalphai67; estrogen receptor alpha ...
Invitrogen Anti-Estrogen Receptor alpha Monoclonal (1D5), Catalog # MA5-13191. Tested in Western Blot (WB), Immunofluorescence ... estrogen nuclear receptor alpha; Estrogen receptor; estrogen receptor alpha E1-E2-1-2; estrogen receptor alpha E1-N2-E2-1-2; ... estrogen receptor alpha splice variant, CTERP-1; estrogen receptor alpha splice variant, ERalphaDup5; estrogen receptor alpha ... estrogen receptor alpha splice variant, ERalphai45bL; estrogen receptor alpha splice variant, ERalphai45bS; estrogen receptor ...
Estrogen receptor-alpha (ESR1) is highly expressed in the efferent ductules of all species studied as well as in the epididymal ... Epididymal Hypo-Osmolality Induces Abnormal Sperm Morphology and Function in the Estrogen Receptor Alpha Knockout Mouse. ... "Epididymal Hypo-Osmolality Induces Abnormal Sperm Morphology and Function in the Estrogen Receptor Alpha Knockout Mouse," ... "Epididymal Hypo-Osmolality Induces Abnormal Sperm Morphology and Function in the Estrogen Receptor Alpha Knockout Mouse," ...
... were investigated for an estrogen receptor alpha, and found that demethylated metabolites had stronger binding affinities than ... Phytoestrogens are defined as plant-derived compounds with estrogen-like activities according to their chemical structures and ... Keywords: arctigenin; estrogen receptor alpha; demethylation; ligand binding affinity arctigenin; estrogen receptor alpha; ... Ligand Binding Affinities of Arctigenin and Its Demethylated Metabolites to Estrogen Receptor Alpha Jong-Sik Jin 1, Jong-Hyun ...
Regulation of estrogen receptor alpha (ERalpha) plays an important role in hormone responsiveness and growth of ER-positive ... Regulation of estrogen receptor alpha (ERalpha) plays an important role in hormone responsiveness and growth of ER-positive ... Hypoxia induces proteasome-dependent degradation of estrogen receptor alpha in ZR-75 breast cancer cells Mol Endocrinol. 2002 ... and estrogen response element-dependent reporter gene activity in ZR-75 cells. Although 17beta-estradiol and hypoxia induce ...
Estrogen receptor alpha gene 1 encodes Estrogen Receptor-alpha, which is activated by estrogen. Polymorphisms. ... searching for Estrogen receptor alpha 114 found (219 total). alternate case: estrogen receptor alpha. Mir-22 (787 words) [view ... Maternal care associated with methylation of the estrogen receptor alpha 1b promoter and estrogen receptor alpha expression in ... Lin D, Liang Z (2010). An estrogen receptor alpha suppressor, microRNA-22, is downregulated in estrogen receptor alpha- ...
Estrogen related receptor alpha (ERRalpha) is a family member of the steroid/thyroid nuclear receptor superfamily. Estrogen ... Estrogen-related Receptor (ERR) and Proliferator-activated Receptor Gamma Coactivator (PGC)/ERR Reporter Stable Cell Lines ... For example, the inventors previously cloned the human estrogen receptor-related orphan receptor alpha1 cDNA and demonstrated ... 4G10, a Monoclonal Antibody Against the Chemokine Receptor CXCR4, Raised Against a Synthetic Peptide of 38 Residues in Length ...
We tested the hypothesis that the duration of ovarian hormone deprivation before estrogen reintroduction affects the role of ... The vascular consequences of estrogen treatment may be driven by its initiation timing. ... Estrogen Receptor alpha / agonists*, genetics, metabolism. Estrogen Replacement Therapy. Estrogens / pharmacology*. Female. ... 0/Estrogen Receptor alpha; 0/Estrogens; 0/Nitriles; 0/Propionates; 0/RNA, Messenger; 0/Vasodilator Agents; 0/ ...
Here, we show that ubiquitin proteasome function is required for ER alpha to serve as a transcriptional activator. Deletion of ... ER alpha) is downregulated in the presence of its cognate ligand, estradiol (E2), through the ubiquitin proteasome pathway. ... The 26S proteasome is required for estrogen receptor-alpha and coactivator turnover and for efficient estrogen receptor-alpha ... Estrogen receptor-alpha (ER alpha) is downregulated in the presence of its cognate ligand, estradiol (E2), through the ...
Crystal structure of human estrogen receptor alpha LBD in complex with GRIP peptide and two isomers of Ethoxy triphenylethylene ... Crystal structure of human estrogen receptor alpha LBD in complex with GRIP peptide and two isomers of Ethoxy triphenylethylene ...
Human Estrogen Receptor Alpha Ligand-Binding Domain In Complex With OBCP-2M and A Glucocorticoid Receptor Interacting Protein 1 ... Human Estrogen Receptor Alpha Ligand-Binding Domain In Complex With OBCP-2M and A Glucocorticoid Receptor Interacting Protein 1 ...
A. Cavallini, M. Notarnicola, R. Giannini et al., "Oestrogen receptor-related receptor alpha (ERRα) and oestrogen receptors (ER ... E. Bonnelye and J. E. Aubin, "Estrogen receptor-related receptor α: a mediator of estrogen response in bone," The Journal of ... R. Sladek, J.-A. Bader, and V. Giguere, "The orphan nuclear receptor estrogen-related receptor alpha is a transcriptional ... H. Wang and J. Wang, "Estrogen-related receptor alpha interacts cooperatively with peroxisome proliferator-activated receptor- ...
The human estrogen receptor comes in two forms, alpha and beta. This work focuses on the alpha form of the estrogen receptor. ... The 3ERT PDB crystal structure has the estrogen receptor bound to the cancer drug 4-hydroxytamoxifen. The 4-hydroxytamoxifen ... However the estrogen receptor also has additional functions independent of DNA binding. ... and other pesticides causes conformational changes in the estrogen receptor. Before examining these factors, this work examines ...
... estrogen receptor 1) for ICC/IF, IHC, WB, ChIP assay. Anti-Estrogen Receptor alpha mAb (GTX60809) is tested in Human samples. ... estrogen receptor 1. Background. This gene encodes an estrogen receptor, a ligand-activated transcription factor composed of ... Storage Conditions: Estrogen Receptor alpha antibody [GT9077]. Storage Buffer. PBS containing 0.05% azide; purified by ammonium ... Monoclonal antibody raised in mouse against the NH2 terminus of the human ERα (estrogen receptor alpha), using a KLH-conjugated ...
Methods of using these genes in identifying candidate agents that exert at least some of the biological effects of estrogen and ... with and without exposure to estrogen and/or other hormone compositions. ... A plurality of genes modulated by estrogen or other agents, such as hormones or combinations of hormones, in various types of ... The distribution of estrogen receptor-beta mRNA in forebrain regions of the estrogen receptor-alpha knockout mouse. ...
Estrogen receptor alpha delta 3*,4,5,6,7*/775 hypothalamic isoformImported. Automatic assertion inferred from database entriesi ... tr,B6DU67,B6DU67_HUMAN Estrogen receptor alpha delta 3*,4,5,6,7*/775 hypothalamic isoform (Fragment) OS=Homo sapiens OX=9606 GN ... ReceptorImported. ,p>Information which has been imported from another database using automatic procedures.,/p> ,p>,a href="/ ... Nuclear receptorInterPro annotation. ,p>Information which has been generated by the UniProtKB automatic annotation system, ...
"Estrogen Receptor alpha" by people in this website by year, and whether "Estrogen Receptor alpha" was a major or minor topic of ... "Estrogen Receptor alpha" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... Below are the most recent publications written about "Estrogen Receptor alpha" by people in Profiles. ... Estrogen receptor a mediates proliferation of osteoblastic cells stimulated by estrogen and mechanical strain, but their acute ...
Abstract 2106: Estrogen receptor alpha drives proliferation of prostate cancer through PI3K and MAPK signaling. Itsuhiro ... Estrogen receptor alpha drives proliferation of prostate cancer through PI3K and MAPK signaling. [abstract]. In: Proceedings of ... Abstract 2106: Estrogen receptor alpha drives proliferation of prostate cancer through PI3K and MAPK signaling ... Abstract 2106: Estrogen receptor alpha drives proliferation of prostate cancer through PI3K and MAPK signaling ...
... fulvestrant is more effective than tamoxifen in blocking estrogen receptor-alpha action. Estrogen receptor-alpha H-score is ... estrogen receptor-alpha has been understudied as a target in this disease. We sought to identify hormone-responsive, estrogen ... Active estrogen receptor-alpha signaling in ovarian cancer models and clinical specimens. Courtney L Andersen, Matthew J Sikora ... Results: Proliferation is estrogen receptor-alpha-regulated in HGSOC cells in vitro and in vivo, and is partly dependent on 3-D ...
Agonist activity at estrogen receptor alpha in human MCF7:WS8 cells after 18 hrs by dual luciferase reporter assay. ...
  • In humans, ERα is encoded by the gene ESR1 (EStrogen Receptor 1). (wikipedia.org)
  • There are two different forms of the estrogen receptor, alpha and beta, encoded by separate genes (ESR1 and ESR2, respectively). (thermofisher.com)
  • Estrogen receptor-alpha (ESR1) is highly expressed in the efferent ductules of all species studied as well as in the epididymal epithelium in mice and other select species. (bioone.org)
  • Several polymorphisms of the estrogen receptor (ER) alpha (ESR1) gene exist that may influence the impact of estrogen, leading to clinically relevant phenotypes. (rti.org)
  • The association between two common estrogen receptor alpha (ESR1) polymorphisms with lifetime MDD was examined using adjusted logistic regression models, taking into account the age at first depressive episode and the recurrence of depression. (inserm.fr)
  • To confirm the generality of the latter approach, we show that the dimeric human estrogen receptor alpha (hERalpha, ESR1, NR3A1), which binds in the major groove of the ERE, can be inhibited by a polyamide bound in the opposing minor groove of the ERE. (caltech.edu)
  • Estrogen Receptor (ER Alpha or Estradiol Receptor or Nuclear Receptor Subfamily 3 Group A Member 1 or NR3A1 or ESR1) pipeline Target constitutes close to 22 molecules. (reportsnreports.com)
  • The latest report Estrogen Receptor - Pipeline Review, H2 2017, outlays comprehensive information on the Estrogen Receptor (ER Alpha or Estradiol Receptor or Nuclear Receptor Subfamily 3 Group A Member 1 or NR3A1 or ESR1) targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA) and molecule type. (reportsnreports.com)
  • Furthermore, this report also reviews key players involved in Estrogen Receptor (ER Alpha or Estradiol Receptor or Nuclear Receptor Subfamily 3 Group A Member 1 or NR3A1 or ESR1) targeted therapeutics development with respective active and dormant or discontinued projects. (reportsnreports.com)
  • Furthermore, I found that this hormonal regulation is via the estrogen receptor alpha, encoded by the ESR1 gene. (dal.ca)
  • Thus by modulating levels of PRP4K, estrogen may affect pre-mRNA splicing in tissues expressing ESR1. (dal.ca)
  • We examined estrogen receptor beta (ESR2) polymorphisms in interaction with estrogen receptor alpha (ESR1) and insulin-like growth factor I (IGF1) variants in relation to the risk of osteoporotic fracture, BMD, and bone geometry. (cdc.gov)
  • We investigated whether the effect of hormone therapy use is modified by polymorphisms in the estrogen receptor (ESR1) and progesterone receptor (PGR) genes in the Dutch Prospect-EPIC and the English EPIC-Norfolk cohorts. (cam.ac.uk)
  • Abstract B255: Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells. (aacrjournals.org)
  • ABSTRACT Growth factors are thought to activate estrogen receptor-alpha ERα by phosphorylating the serines in the N-terminus of the receptor. (georgetown.edu)
  • Estrogen receptors (ERα and ERβ) are ligand activated nuclear receptor proteins that mediate the action of estradiol and structurally related compounds. (aacrjournals.org)
  • however, hypoxic conditions decreased basal and 17beta-estradiol-induced pS2 gene expression (mRNA levels) and estrogen response element-dependent reporter gene activity in ZR-75 cells. (nih.gov)
  • One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. (umassmed.edu)
  • Measurement of the global proteomic effects of estradiol by stable isotope labeling by amino acids in cell culture (SILAC) resulted in identification of 103 estrogen-regulated proteins, with only 40 of the corresponding genes having estrogen response elements. (mcponline.org)
  • Four reference chemicals should be included in each experiment: a strong estrogen (17beta-estradiol), a weak estrogen (17alpha-estradiol), a very weak estrogen (17alpha-methyltestosterone) and a negative control (corticosterone). (oecd-ilibrary.org)
  • Global profiling of estradiol-stimulated ERα-positive cells by ChIP-sequencing and DNA microarrays revealed thousands of EREs ( 3 ⇓ ⇓ - 6 ) and hundreds of estrogen-regulated mRNA transcripts ( 7 , 8 ), respectively. (mcponline.org)
  • Estrogen receptors alpha (ER-a) and beta (ER-b) are thought to mediate the action of estradiol in target tissues. (mcmaster.ca)
  • Stimulation with estradiol (E2) leads to receptor binding to estrogen response elements (ERE) in target gene regulatory sequences in association with transcription cofactors, and results in altered gene expression, increased cell proliferation and accelerated tumour growth. (umontreal.ca)
  • Moreover, in MCF-7 human breast cancer cells, various p53-inducing agents (such as UV irradiation) or treatment with RITA (which inhibits the interaction of p53 with Mdm2) stabilized ER alpha and abolished its 17 beta-estradiol-dependent turnover. (cnrs.fr)
  • Estrogen receptor beta inhibits 17beta-estradiol-stimulated proliferation of the breast cancer cell line T47D. (semanticscholar.org)
  • Estradiol attenuates the adenosine triphosphate-induced increase of intracellular calcium through group II metabotropic glutamate receptors in rat dorsal root ganglion neurons. (semanticscholar.org)
  • Estrogen receptor-alpha (ERalpha) expression was strongly down-regulated by RANKL, whether or not estradiol was present. (pubfacts.com)
  • Effect of estradiol on estrogen receptor-alpha gene expression and activity can be modulated by the ErbB2/PI 3-K/Akt pathway. (koreascience.or.kr)
  • We then compared these expression changes after 17β-estradiol and a membrane receptor selective estrogen-BSA treatment using quantitative real-time PCR. (biomedcentral.com)
  • Our quantitative real-time PCR results confirmed that the selective membrane receptor agonist, estrogen-BSA induces similarly pronounced expression changes regarding these genes as 17β-estradiol. (biomedcentral.com)
  • The genomic effects of estradiol are traditionally mediated by nuclear estrogen receptors (ERs). (biomedcentral.com)
  • Following estrogenic activation, the estrogen receptor-alpha (ERalpha) directly regulates the transcription of target genes via DNA binding. (nih.gov)
  • MicroRNAs (miRNAs) modulated by ERalpha have the potential to fine tune these regulatory systems and also provide an alternate mechanism that could impact on estrogen-dependent developmental and pathological systems. (nih.gov)
  • Characterization of the mir-17-92 locus confirms that the ERalpha target protein c-MYC binds its promoter in an estrogen-dependent manner. (nih.gov)
  • We propose that ERalpha, c-MYC, and miRNA transcriptional programs invoke a sophisticated network of interactions able to provide the wide range of coordinated cellular responses to estrogen. (nih.gov)
  • 22, 233-236] reported a difference between Chinese dry eye and control groups in the frequency of a polymorphism in estrogen receptor alpha (ERalpha). (nih.gov)
  • Regulation of estrogen receptor alpha (ERalpha) plays an important role in hormone responsiveness and growth of ER-positive breast cancer cells and tumors. (nih.gov)
  • Whereas no rapid vasorelaxant responses were elicited by an estrogen receptor (ER) beta-selective agonist, responses to E(2) and an ERalpha selective agonist waned postovariectomy at any given time and were restored by E(2) treatment after 1 and 4 months but not 8 months postovariectomy. (biomedsearch.com)
  • Accordingly, endothelial ERalpha mRNA and protein expression declined approximately 6-fold after prolonged hypoestrogenicity and was restored by estrogen replacement starting 1 month but not 8 months postovariectomy. (biomedsearch.com)
  • The present findings document that the functional impairment of the ERalpha/endothelial NO synthase signaling network after an extended period of hypoestrogenicity was not restored by E(2) administration, providing experimental support to early initiation of estrogen replacement with preferential ERalpha targeting to improve cardiovascular outcomes. (biomedsearch.com)
  • Association studies between estrogen receptor alpha (ERalpha) gene polymorphisms and bone mineral density (BMD) have yielded inconsistent results. (unboundmedicine.com)
  • In the present study we evaluated the influence of XbaI and PvuII ERalpha gene polymorphisms on BMD, biochemical markers, rates of bone loss and the response to estrogen/hormone therapy (ET/HT) in elderly postmenopausal women. (unboundmedicine.com)
  • The functions of estrogen receptors (ERs) in mouse ovary and genital tracts were investigated by generating null mutants for ERalpha (ERalphaKO), ERbeta (ERbetaKO) and both ERs (ERalphabetaKO). (biologists.org)
  • These and other results reveal a functional redundancy between ERalpha and ERbeta for ovarian folliculogenesis, and strongly suggest that (1) ERbeta plays an important role in mediating the stimulatory effects of estrogens on granulosa cell proliferation, (2) ERalpha is not required for follicle growth under wild type conditions, while it is indispensable for ovulation, and (3) ERalpha is also necessary for interstitial glandular cell development. (biologists.org)
  • In the present study, the expression of estrogen receptors-alpha and -beta (ERalpha, ERbeta), androgen receptor (AR) and 5-HT was examined immunohistochemically in the rat and mouse DRN in both sexes. (researchmap.jp)
  • Altogether, our observations suggest that the enhancement of ERalpha activity by p160/SRCs and CBP can be regulated by phosphorylation and stress the importance of using full-length receptors to assess the role of the activation function-1 in cofactor recruitment. (thebiogrid.org)
  • The estrogen receptor alpha (ERalpha) is understood to play an important role in the progression of breast cancer. (uni-regensburg.de)
  • Mature human osteoclasts thus cannot respond to estrogen via ERalpha. (pubfacts.com)
  • However, ERalpha was present in CD14+ osteoclast progenitors, and a scaffolding protein, BCAR1, which binds ERalpha in the presence of estrogen, was abundant. (pubfacts.com)
  • Immunoprecipitation showed rapid (approximately 5 min) estrogen-dependent formation of ERalpha-BCAR1 complexes, which were increased by RANKL co-treatment. (pubfacts.com)
  • In the present study, we investigated the relationship between polymorphisms in the genes encoding the vitamin D receptor (VDR) (FokI, TaqI) and estrogen receptor-alpha (ERalpha) (PvuII, XbaI), and bone mineral density (BMD), bone mineral content (BMC), and markers of bone turnover in 224 Danish girls aged 11-12 years. (cdc.gov)
  • METHODS AND RESULTS: We detected an estrogen receptor alpha (ERalpha) transcript in human endothelial cells that encodes a truncated 46-kDa ERalpha (Delta1a-hERalpha-46). (ox.ac.uk)
  • Confocal microscopy revealed that a proportion of both ERalpha-66 and hERalpha-46 was localized outside the nucleus and mediated specific cell-surface binding of estrogen as assessed by FITC-conjugated, BSA-estrogen binding studies. (ox.ac.uk)
  • Both ERalpha isoforms colocalized with eNOS and mediated acute activation of eNOS in response to estrogen stimulation. (ox.ac.uk)
  • However, estrogen-stimulated transcriptional activation mediated by Delta1a-hERalpha-46 was much less than with ERalpha-66. (ox.ac.uk)
  • CONCLUSIONS: These findings suggest that expression of an alternatively spliced, truncated ERalpha isoform in human endothelial cells confers a unique ability to mediate acute but not transcriptional responses to estrogen. (ox.ac.uk)
  • Toll-like receptor 9 agonist inhibits ERalpha-mediated transactivation by activating NF-kappaB in breast cancer cell lines. (qxmd.com)
  • We studied the association between polymorphisms in the estrogen receptor alpha (ERalpha) gene and the prevalence of radiographic OA of the knee. (ox.ac.uk)
  • Breast cancer is a heterogeneous disease, and stratification of patients into cohorts based on the expression of the molecular markers estrogen receptor α (ERα), progesterone receptor (PR) and/or HER2 helps dictate choice of therapy and predict disease prognosis. (umontreal.ca)
  • It shows lesser enhancement of ERβ transcriptional activity and has no influence on the transcriptional activity of other nuclear hormone receptors (progesterone receptor, glucocorticoid receptor, thyroid hormone receptor, or retinoic acid receptor) or on the basal activity of ERs. (asm.org)
  • Estrogen-alpha and progesterone receptor expression in cystic endometrial hyperplasia and pyometra in the bitch. (ugent.be)
  • De Bosschere H, Ducatelle R, Vermeirsch H, Simoens P, Coryn M. Estrogen-alpha and progesterone receptor expression in cystic endometrial hyperplasia and pyometra in the bitch. (ugent.be)
  • Immunophenotyping revealed that the mammary tumors express luminal markers, are positive for estrogen and progesterone receptors, negative for HER2 and have a low proliferation index. (ovid.com)
  • Objective: We aimed to characterize the somatostatin, estrogen, and progesterone receptor distribution for NFPAs and compare it with factors of tumor aggressiveness. (diva-portal.org)
  • Design: Tumor samples for immunohistochemistry (n = 145) and quantitative reverse transcription polymerase chain reaction (n = 106) analyses of somatostatin receptor (SSTR) 1, SSTR2, SSTR3, SSTR5, estrogen receptor alpha (ER alpha), and progesterone receptor (PR) were measured by immunoreactive score (IRS) andmessenger RNA relative quantity and retrospectively compared with variables of aggressiveness. (diva-portal.org)
  • To assess oestrogen receptor (ER)α, ERβ, and progesterone receptor (PR) expression in stage I ovarian adult-type granulosa cell tumours (AGCTs) and correlate the findings with clinical outcome. (ovid.com)
  • The reason why hormone treatment alone cannot cure endometriosis could be that estrogen and progesterone receptors are not distributed homogeneously in different lesions and between women. (endonews.com)
  • There is high variability in the expression of estrogen receptor alpha and progesterone receptor among distinct glands in the same deep infiltrating endometriosis sample. (endonews.com)
  • So, in order to better understand the differences among the cells that make up endometrial lesions, Dr. Géraldine Brichant at the University of Liege in Belgium and colleagues looked at the expression of estrogen and progesterone receptors (receptors to which hormones bind to), in endometriosis samples obtained from women with deep infiltrating endometriosis. (endonews.com)
  • They found that the distribution of estrogen receptor alpha and progesterone receptor were not even in these lesions. (endonews.com)
  • In support of this hypothesis, treatment of MCF-7 cells with EGF (150 ng/ml) lead to an increase in intracellular calcium from 150 nM to 350 nM (+/-70 nM) and the induction of the ERα responsive genes, progesterone receptor (PgR) and pS2. (georgetown.edu)
  • Influence of estrogen receptor alpha and progesterone receptor polymorphisms on the effects of hormone therapy on mammographic density. (cam.ac.uk)
  • The following product was used in this experiment: Estrogen Receptor alpha Monoclonal Antibody (33) from Thermo Fisher Scientific, catalog # MA1-310, RRID AB_325422. (thermofisher.com)
  • By Western blot, this antibody detects an ~66 kDa protein representing ER alpha from MCF-7 cell extract. (thermofisher.com)
  • Monoclonal antibody raised in mouse against the NH2 terminus of the human ERα (estrogen receptor alpha), using a KLH-conjugated synthetic peptide (Q19-K32). (genetex.com)
  • WB analysis of 100 fmol ER alpha (ERa) and ER beta (ERb1) recombinant protein using ER alpha antibody at a concentration of 7 μg/ml. (genetex.com)
  • ICC analysis of COS-7 cells transiently overexpressing human ERα or ERs1 using ER alpha antibody at a concentration of 15 μg/ml, followed by a biotinylated secondary antibody and peroxidase-labeled avidin. (genetex.com)
  • Immunocytochemistry/Immunofluorescence: ERR alpha/NR3B1 Antibody [NBP1-47254] - ERR alpha antibody was tested in HeLa cells at a 1:100 dilution against Dylight 488 (Green). (antibodies-online.com)
  • Immunohistochemistry-Paraffin: ERR alpha/NR3B1 Antibody [NBP1-47254] - IHC-P detection of ERR alpha/ESRRA protein in a section of normal human kidney using 5 ug/ml concentration of Estrogen Related Receptor alpha antibody. (antibodies-online.com)
  • Using a comprehensive antibody-based proteomics approach, we interrogated PRDX1 protein as a putative biomarker in estrogen receptor (ER)-positive breast cancer. (lu.se)
  • Western blot analysis of extracts from MCF-7 cells untreated or treated with E2 and EGF using Rabbit anti estrogen receptor alpha (pSer104) antibody. (bio-rad-antibodies.com)
  • Rabbit anti estrogen receptor alpha (pSer104) antibody recognizes estrogen receptor alpha, also known as ER-alpha, when phosphorylated at serine 104. (bio-rad-antibodies.com)
  • In this study, we investigated the estrogenic activities of soy isoflavones after digestion with enteric bacteria in competition binding assays with hER alpha or hER beta protein, and in a gene expression assay using a yeast system. (nih.gov)
  • The protein encoded by this gene is a nuclear receptor that is closely related to the estrogen receptor. (wikipedia.org)
  • This protein acts as a site-specific (consensus TNAAGGTCA) transcription regulator and has been also shown to interact with estrogen and the transcription factor TFIIB by direct protein-protein contact. (wikipedia.org)
  • The binding and regulatory activities of this protein have been demonstrated in the regulation of a variety of genes including lactoferrin, osteopontin, medium-chain acyl coenzyme A dehydrogenase (MCAD) and thyroid hormone receptor genes. (wikipedia.org)
  • The protein localizes to the nucleus where it may form a homodimer or a heterodimer with estrogen receptor 2. (genetex.com)
  • Dynamics of protein expression unambiguously revealed early and delayed response proteins and well correlated with presence or absence of estrogen response elements in the corresponding genes. (mcponline.org)
  • ERα action is exerted through four distinct pathways: direct ligand-dependent transcription through binding to estrogen response elements (EREs), tethered mode through its binding to other transcription factors which interact with their DNA response elements, nongenomic pathway mediated through membrane or cytoplasmic ERα and rapid signaling by protein kinases, and finally, estrogen-independent pathway through growth factor signaling and ERα phosphorylation ( 2 ). (mcponline.org)
  • For example, ERD3, the variant protein encoded by exon 3 deleted ER-a mRNA, that is missing the second zinc finger of the DNA binding domain, has been shown to have a dominant negative activity on wild-type ER-a receptor action (3). (mcmaster.ca)
  • An alternative strategy to kill the estrogen signaling is to downregulate ERα protein. (aacrjournals.org)
  • The activation of ER-alpha produced a protein expression pattern similar to that observed in the control culture, with a moderate expression of Ki-67 being observed. (uni-muenchen.de)
  • This selectivity for ER is explained by PTα interaction not with ER, but with a 37-kDa protein denoted REA, for repressor of estrogen receptor activity, a protein that we have previously shown binds to ER, blocking coactivator binding to ER. (asm.org)
  • Our data support a model in which PTα, which does not interact with ER, selectively enhances the transcriptional activity of the ER but not that of other nuclear receptors by recruiting the repressive REA protein away from ER, thereby allowing effective coactivation of ER with SRC-1 or other coregulators. (asm.org)
  • These findings highlight a new role for PTα as a coregulator activity-modulating protein that confers receptor specificity. (asm.org)
  • The relationship of insulin-like growth factor-II, insulin-like growth factor binding protein-3, and estrogen receptor-alpha expression to disease progression in epithelial ovarian cancer. (aacrjournals.org)
  • Total RNA was extracted from the tumor and analyzed for IGF-II, IGF binding protein 3 (IGFBP-3), and estrogen receptor-alpha expressions using quantitative reverse transcription PCR. (aacrjournals.org)
  • Ligand-independent interactions of p160/steroid receptor coactivators and CREB-binding protein (CBP) with estrogen receptor-alpha: regulation by phosphorylation sites in the A/B region depends on other receptor domains. (thebiogrid.org)
  • RPPA screening of cancer signaling proteins showed that ER alpha protein was upregulated in PRDX1 high tumors. (lu.se)
  • Exogenous H2O2 treatment decreased ER alpha protein levels in ER-positive cells. (lu.se)
  • The role of the tumor necrosis factor receptor associated protein 1 (TRAP1) - supposed to be involved in protection of cells from apoptosis and oxidative stress - has just started to be investigated in ovarian cancer. (biomedcentral.com)
  • In this study I demonstrated that PRP4K is expressed in the normal mammary duct epithelial cells of the mouse, and that estrogen induces PRP4K gene and protein expression in ER+ human MCF7 breast cancer cells. (dal.ca)
  • Expression levels of ER alpha protein vary with sample type. (abcam.co.jp)
  • In the stable clones, expression of antisense p53 resulted in a decrease in the expression of ER alpha protein. (bioscientifica.com)
  • Equol induces transcription most strongly with hER alpha and hER beta. (nih.gov)
  • Although genistin binds more weakly to the receptors and induces transcription less than does genistein, it stimulates the growth of MCF-7 cells more strongly than does genistein. (nih.gov)
  • The estrogen receptor is a ligand-activated transcription factor, that when bound to estrogen hormone, induces a conformational change that allows dimerization and binding to estrogen response elements (ERE) in DNA. (thermofisher.com)
  • It is hypothesized that epidermal growth factor (EGF) activates ERα through the PLC--calcium-calmodulin pathway by increasing intracellular calcium which, upon binding to the LBD, induces a conformational change that activates the receptor. (georgetown.edu)
  • Estrogen-related receptor alpha induces the expression of vascular endothelial growth factor in breast cancer cells. (koreascience.or.kr)
  • Detects a band of approximately 64 kDa (predicted molecular weight: 68 kDa).Can be blocked with Human Estrogen Receptor alpha peptide (ab5847) . (abcam.com)
  • R. Sladek, J.-A. Bader, and V. Giguere, "The orphan nuclear receptor estrogen-related receptor alpha is a transcriptional regulator of the human medium-chain acyl coenzyme A dehydrogenase gene," Molecular and Cellular Biology , vol. 17, no. 9, pp. 5400-5409, 1997. (hindawi.com)
  • Expression of estrogen receptor-related receptors, a subfamily of orphan nuclear receptors, as new tumor biomarkers in ovarian cancer cells," Journal of Molecular Medicine , vol. 83, no. 6, pp. 457-467, 2005. (hindawi.com)
  • Result: Discussions on molecular transitions and drug therapies offer insights into cervical cancer and the functions of estrogen receptors. (eurekaselect.com)
  • We summarize here an in vivo molecular "dissection" that allows to delineate in mouse the role of the main "subfunctions" of the receptor. (inserm.fr)
  • A 3D animation illustrating the estrogen mechanism at cellular and molecular levels. (lookfordiagnosis.com)
  • Oestrogen-receptor-positive breast cancer: towards bridging histopathological and molecular classifications. (koreascience.or.kr)
  • Molecular subtype approximated by quantitative estrogne receptor, progestron receptor and Her2 can predict the prognosis of breast cancer. (koreascience.or.kr)
  • The present study, aims at prediction and analysis of ligands from the KEGG COMPOUND database (containing 10,739 entries) able to interact against estrogen receptor alpha using a similarity search and molecular docking approach. (koreascience.or.kr)
  • Nuclear factor-kappaB activation: a molecular therapeutic target for estrogen receptor-negative and epidermal growth factor receptor family receptor-positive human breast cancer. (qxmd.com)
  • Sep 15, 2010 (BUSINESS WIRE) -- GTx, Inc. (Nasdaq: GTXI) today announced that in a Phase II, open label, pharmacokinetic-pharmacodynamic clinical trial, GTx-758, an oral selective estrogen receptor alpha agonist being developed to treat advanced prostate cancer, suppressed serum total testosterone to castrate levels, increased serum SHBG (sex hormone binding globulin), and markedly reduced serum free testosterone in healthy male volunteers. (fiercebiotech.com)
  • As a selective estrogen receptor alpha agonist, GTx-758 has the potential to achieve medical castration by feedback inhibition of the pituitary and hypothalamus without bone loss and hot flashes. (fiercebiotech.com)
  • The principle application of this assay product is in the screening of test samples to quantify functional activities, either agonist or antagonist, that they may exert against the estrogen receptor alpha. (nrresource.org)
  • Phosphorylation at serine 104 contributes to agonist independent activation of estrogen receptor alpha. (bio-rad-antibodies.com)
  • Estrogen Receptors (ER) are members of the steroid/thyroid hormone receptor superfamily of nuclear receptors. (thermofisher.com)
  • Estrogen related receptor alpha (ERRalpha) is a family member of the steroid/thyroid nuclear receptor superfamily. (nih.gov)
  • These two receptors, which belong to the steroid/retinoic acid/thyroid receptor superfamily, contain several structural and functional domains encoded by two mRNAs containing 8 exons. (mcmaster.ca)
  • Nuclear hormone receptors encompass the steroid/thyroid/retinoid receptor superfamily and are ligand-inducible transcription factors. (asm.org)
  • Estrogen receptor alpha is a member of the nuclear receptor superfamily and also functions as a ligand-regulated transcription factor. (bio-rad-antibodies.com)
  • 产品介绍】Estrogen-related receptor alpha (ERR alpha) is an orphan member of the superfamily of nuclear hormone receptors. (klamar-reagent.com)
  • Upon ligand binding, ER-a and ER-b proteins recognize specific estrogen responsive elements (EREs) located in DNA in the proximity of target genes, and through interactions with several co-activators modulate the transcription of these genes. (mcmaster.ca)
  • The putative proteins encoded by these variant mRNAs would therefore be missing some functional domains of the wild-type receptors and might interfere with wild-type ER signaling pathways. (mcmaster.ca)
  • Indeed, in vitro functional studies have shown that some recombinant ER-a variant proteins can affect estrogen regulated gene transcription. (mcmaster.ca)
  • Proteins such as PTα represent an additional regulatory component that defines a novel paradigm enabling receptor-selective enhancement of transcriptional activity by coactivators. (asm.org)
  • These proteins exist as a part of large, multicomponent complexes that can be recruited by nuclear hormone receptors and function, in part, as chromatin-remodeling factors ( 2 , 29 , 44 ). (asm.org)
  • Caveolin proteins and estrogen signaling in the brain. (semanticscholar.org)
  • Caveolin proteins are essential for distinct effects of membrane estrogen receptors in neurons. (semanticscholar.org)
  • Recombinant Human Estrogen Receptor Alpha RECOMBINANT & NATURAL PROTEINS Human samples 80 % of the research is conducted on human samples. (antibody-antibodies.com)
  • GENTAUR suppliers human normal cells, cell lines, RNA extracts and lots of antibodies and ELISA kits to Human proteins as well as Recombinant Human Estrogen Receptor Alpha RECOMBINANT & NATURAL PROTEINS. (antibody-antibodies.com)
  • This experimental approach demonstrated that p53 up-regulates ER alpha gene expression by increasing transcription of the gene through elements located upstream of promoter A. Transfection assays using p53 mutants further demonstrated that the p53-induced increase in ER alpha gene transcription was not dependent on the ability of p53 to bind to DNA but on its ability to interact with other proteins. (bioscientifica.com)
  • Estrogen receptor alpha (ERα) and estrogen-related receptor alpha (ERRα) have been found to regulate many of the same genes. (wikipedia.org)
  • Estrogen related receptors are thought to regulate similar target genes in the absence of known ligands. (nih.gov)
  • Estrogen-regulated transcriptome data were overlapped with public datasets to develop a comprehensive panel of estrogen receptor-alpha target genes. (aacrjournals.org)
  • Transcriptomic studies identified genes shared by cell lines and PDX explants as estrogen receptor-alpha targets. (aacrjournals.org)
  • Estrogen receptor alpha (ERα)-mediated proliferation of breast cancer cells is facilitated through expression of multiple primary target genes, products of which induce a secondary response to stimulation. (mcponline.org)
  • Given the fundamental importance of estrogen signaling and its involvement in breast cancer progression, numerous approaches have been undertaken to discover primary ERα target genes and their secondary messengers. (mcponline.org)
  • These receptors modulate the transcription of specific genes by interacting with hormone response elements located near the target gene promoter ( 17 , 21 , 35 ). (asm.org)
  • Of 921 genes differentially regulated by estrogen in ERβ+ vs ERβ- cells, 424 showed one or more ERβ site within 10 kb. (biomedcentral.com)
  • ERβ binding in close proximity of several miRNA genes and in the mitochondrial genome, suggests the possible involvement of this receptor in small non-coding RNA biogenesis and mitochondrial genome functions. (biomedcentral.com)
  • Development of cDNA microarray for expression profiling of estrogen-responsive genes. (semanticscholar.org)
  • Strikingly, however, in contrast to p68, knockdown of endogenous p72 results in a marked inhibition of both baseline and estrogen stimulated-expression of these genes. (biomedcentral.com)
  • DNA demethylating agents such as genistein (GE) and histone deacetylase inhibitors (HDACIs) such as trichostatin A (TSA) may strongly reactivate silenced genes and exposure to these two agents in combination is reported to enhance estrogen receptor alpha (ERα) reactivation and induction of apoptosis. (waocp.org)
  • Mechanisms of estrogen receptor signaling: convergence of genomic and nongenomic actions on target genes. (koreascience.or.kr)
  • Re-analyzing expression data from multiple microarray experiments, we selected a set of key regulatory genes involved in proliferation regulation and estrogen signaling to monitor estrogen-induced transcription changes. (biomedcentral.com)
  • Nuclear hormone receptor. (abcam.com)
  • Belongs to the nuclear hormone receptor family. (abcam.com)
  • Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen. (wikipedia.org)
  • The estrogen receptor (ER) is a ligand-activated transcription factor composed of several domains important for hormone binding, DNA binding, and activation of transcription. (wikipedia.org)
  • Prolonged ovarian hormone deprivation impairs the protective vascular actions of estrogen receptor alpha agonists. (biomedsearch.com)
  • We tested the hypothesis that the duration of ovarian hormone deprivation before estrogen reintroduction affects the role of estrogen as mediator of endothelial function and vascular relaxation in nondiseased vessels. (biomedsearch.com)
  • This gene encodes an estrogen receptor, a ligand-activated transcription factor composed of several domains important for hormone binding, DNA binding, and activation of transcription. (genetex.com)
  • Prostate cancer, a hormone-dependent disease of aging men, occurs as the relative levels of estrogen compared to testosterone are increasing. (aacrjournals.org)
  • We sought to identify hormone-responsive, estrogen receptor-alpha-dependent HGSOC. (aacrjournals.org)
  • Steroid hormone receptors are ubiquitous nuclear receptors with key roles in control of reproduction, fetal development, metabolism, homeostasis, immune response and cognitive functions ( 1 ). (mcponline.org)
  • Although estrogen is primarily thought of as the hormone involved in female reproduction, it also plays a role in many additional physiological and pathological processes. (rti.org)
  • We find that prothymosin alpha (PTα) selectively enhances transcriptional activation by the estrogen receptor (ER) but not transcriptional activity of other nuclear hormone receptors. (asm.org)
  • The gene transcriptional activity by nuclear hormone receptors is enhanced or repressed by their interaction with regulatory factors which function positively (coactivator) or negatively (corepressor) as intermediates between the receptor and the RNA polymerase II transcription complex ( 2 , 25 , 33 , 44 ). (asm.org)
  • We recently reported on an ER-selective coregulator, denoted REA for repressor of estrogen receptor activity, that interacts only with ER among the nuclear hormone receptors and represses the activity of the estrogen-occupied ER and potentiates the inhibitory activity of antiestrogens ( 27 ). (asm.org)
  • 1995 ) Anti-mullerian hormone and anti-mullerian hormone type II receptor messenger ribonucleic acid expression in rat ovaries during postnatal development, the estrous cycle, and gonadotropin-induced follicle growth. (biologists.org)
  • Twelve cases (21%) recurred and hormone receptor staining was compared in the corresponding primary and metastatic tumours. (ovid.com)
  • Hormone receptor expression in AGCT may become increasingly relevant due to developments in selective therapy. (ovid.com)
  • Estrogen receptors alpha (ERα) and beta (ERβ) are transcription factors (TFs) that mediate estrogen signaling and define the hormone-responsive phenotype of breast cancer (BC). (biomedcentral.com)
  • The identification of the genomic targets of ERβ in hormone-responsive BC cells is thus a critical step to elucidate the roles of this receptor in estrogen signaling and tumor cell biology. (biomedcentral.com)
  • Expression of full-length ERβ in hormone-responsive, ERα-positive MCF-7 cells resulted in a marked reduction in cell proliferation in response to estrogen and marked effects on the cell transcriptome. (biomedcentral.com)
  • The hormone estrogen, when bound to its receptor (ER) triggers a cascade of signalling events that result in the proliferation of normal mammary glands. (dal.ca)
  • Hormone receptor status, tumor characterstics, and prognosis:a prospective cohort of breast cancer patients. (koreascience.or.kr)
  • This observation does not support an important role of estrogens in tumor growth and prompt us to study the expression of the estrogen receptor, necessary to the action of the hormone, in a large group of prolactinomas. (growkudos.com)
  • Researchers found great variability in hormone receptor distribution in the lesion of different women with endometriosis as well as in the different lesions of the same woman. (endonews.com)
  • There was no typical pattern of hormone receptor distribution in treated or untreated women. (endonews.com)
  • This unevenness was also seen in the lesions of women who were treated with the same hormone therapy, and no typical pattern of hormone receptor distribution could be identified in women how were not treated or those who were. (endonews.com)
  • Estrogen receptor (ER)-positive breast cancer cells have low levels of constitutive NF-kappaB activity while ER negative (-) cells and hormone-independent cells have relatively high constitutive levels of NF-kappaB activity. (qxmd.com)
  • Estrogen withdrawal-induced NF-kappaB activity and bcl-3 expression in breast cancer cells: roles in growth and hormone independence. (qxmd.com)
  • The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. (abcam.com)
  • Further analysis of the influence of the co-activators on the conformation of ERα/ERβ will define the regulation of receptor conformation in controlling estrogenic function in normal and cancer cells. (aacrjournals.org)
  • Estrogen receptor a mediates proliferation of osteoblastic cells stimulated by estrogen and mechanical strain, but their acute down-regulation of the Wnt antagonist Sost is mediated by estrogen receptor ß. (umassmed.edu)
  • 1997 ) Estrogen receptor-mRNA expression in rat ovary: down-regulation by gonadotropins. (biologists.org)
  • These results for the first time imply a close connection between biological activity of PRDX1 and regulation of estrogen-mediated signaling in breast cancer. (lu.se)
  • In mammalian cells, the level of estrogen receptor alpha (ER alpha) is rapidly decreased upon estrogen treatment, and this regulation involves proteasome degradation. (cnrs.fr)
  • Using different approaches, we showed that the Mdm2 oncogenic ubiquitin-ligase directly interacts with ER alpha in a ternary complex with p53 and is involved in the regulation of ER alpha turnover (both in the absence or presence of estrogens). (cnrs.fr)
  • Breast Neoplasms and 69 others ), proposed to participate in pathways (CARM1 and Regulation of the Estrogen Receptor, Downregulated of MTA-3 in ER-negative Breast Tumors, Pelp1 Modulation of Estrogen Receptor Activity) and processes (androgen metabolic process, antral ovarian follicle growth, epithelial cell development, epithelial cell proliferation involved in mammary gland duct elongation, male gonad development and 12 others ). (nrresource.org)
  • Dual action of neuro-estrogens in the regulation of male sexual behavior. (semanticscholar.org)
  • Polymorphism upstream of estrogen receptor alpha reverses negative regulation of transcription. (docphin.com)
  • Figtree GA, Robinson BG, Channon KM, Watkins H. Polymorphism upstream of estrogen receptor alpha reverses negative regulation of transcription. (docphin.com)
  • Estrogen acts primarily via its receptors, ERα and ERβ, nuclear transcription factors involved in the regulation of many complex physiological processes. (biomedcentral.com)
  • Ganoderma lucidum inhibits proliferation of human breast cancer cells by down-regulation of estrogen receptor and NF-kappaB signaling. (qxmd.com)
  • The breast cancer cells response to chronic hypoxia involves the opposite regulation of NF-kB and estrogen receptor signaling. (qxmd.com)
  • PTPrho is also upregulated in estrogen receptor alpha positive breast tumor samples versus estrogen receptor alpha negative tumor samples. (edwardbetts.com)
  • Altered Expression of Estrogen Receptor Alpha Variant mRNAs Between Adjacent Normal Breast And Breast Tumor Tissues. (mcmaster.ca)
  • Absence of ER alpha together with young age may predict tumor recurrence in groups of NFPAs. (diva-portal.org)
  • If ERβ can halt tumor growth, its introduction into cancers may be a novel therapeutic approach to the treatment of estrogen-responsive cancers. (semanticscholar.org)
  • The expression of the estrogen receptor was inversely correlated with tumor size which means that small tumors had a lot of receptors and large one very few. (growkudos.com)
  • Moreover, markers of proliferation of the cells within the tumor were mostly present when the receptor was absent. (growkudos.com)
  • Estrogen receptor status of breast cancer: a marker of different stages of tumor or different entities of the disease? (koreascience.or.kr)
  • Vitamin C and alpha-naphthoflavone prevent estrogen-induced mammary tumors and decrease oxidative stress in female rats. (greenmedinfo.com)
  • ERα is thought to be responsible for pubertal development of the adult phenotype, through mediation of mammary gland response to estrogens. (wikipedia.org)
  • Through its antioxidant function, PRDX1 may prevent oxidative stress-mediated ER alpha loss, thereby potentially contributing to maintenance of an ER-positive phenotype in mammary tumors. (lu.se)
  • These steroid hormones exert their effects in normal and transformed mammary epithelial cells by binding to specific receptors, ERα and ERβ, that mediate estrogen signaling by functioning as ligand-dependent transcription factors. (biomedcentral.com)
  • Mammary development and tumorigenesis are profoundly influenced by signaling pathways under the control of c-erbB2/c-neu and estrogen receptor α (ERα). (usu.edu)
  • Here, we demonstrate that a single biochemical assay is able to predict the tissue-selective pharmacology of an array of selective estrogen receptor modulators (SERMs). (rcsb.org)
  • We describe an approach to classify estrogen receptor (ER) modulators based on dynamics of the receptor-ligand complex as probed with hydrogen/deuterium exchange (HDX) mass spectrometry. (rcsb.org)
  • We demonstrate that analysis of dynamics of the receptor-ligand complex facilitates binning of ER modulators into distinct groups based on structural dynamics. (rcsb.org)
  • In summary, HDX provides a sensitive and rapid approach to classify modulators of the estrogen receptor that correlates with their pharmacological profile. (rcsb.org)
  • However, the use of these estrogens or selective estrogen receptors modulators (SERMs) have also induced undesired effects. (inserm.fr)
  • ERRα was originally cloned by DNA sequence homology to the estrogen receptor alpha (ERα, NR3A1), but subsequent ligand binding and reporter-gene transfection experiments demonstrated that estrogens did not regulate ERRα. (wikipedia.org)
  • ERα is a member of the nuclear receptor family, and its activity is implicated in the gene transcription linked to the proliferation of breast cancer cells, as well as in extranuclear signaling pathways related to the development of resistance to endocrine therapy. (unam.mx)
  • The two-pore domain potassium channel KCNK5: induction by estrogen receptor alpha and role in proliferation of breast cancer cells. (semanticscholar.org)
  • Although membrane-associated estrogen receptors (mERs) have been known to play important role in steroid-induced signal transmission, we still know little about their function in the estrogen-induced proliferation of breast cancer cells. (biomedcentral.com)
  • The uterus of female ERKO mice is hypoplastic, suggesting that ERα mediates mitosis and differentiation in the uterus in response to estrogen stimulation. (wikipedia.org)
  • Estrogen signaling pathway and its imaging in human breast cancer. (koreascience.or.kr)
  • Mechanism of estrogen-induced apoptosis in breast cancer cells: role of the NF-kappaB signaling pathway. (qxmd.com)
  • The presence of the estrogen receptor alpha was detected by a technique called immunohistochemistry, just like in breast cancer. (growkudos.com)
  • Androgens may regulate the male skeleton either directly by stimulation of the androgen receptor (AR) or indirectly by aromatization of androgens into estrogens and, thereafter, by stimulation of the estrogen receptors (ERs). (galileo-training.com)
  • The androgen receptor (AR) plays a central role in establishing an oncogenic cascade that drives prostate cancer progression. (gwu.edu)
  • Furthermore, studies in models of psychopathology and neurodegenerative disease states suggest that estrogen receptors mediate the neuroprotective role of estrogen in the brain. (wikipedia.org)
  • The role of estrogen on MUC1 isoform expression in human breast cancer cells, MCF-7 and T47D, was also analyzed. (biomedcentral.com)
  • ERR alpha was initially isolated based on its sequence homology to the estrogen receptor but is not activated by classic estrogens. (klamar-reagent.com)
  • Estrogen-related receptor alpha (ERRα), also known as NR3B1 (nuclear receptor subfamily 3, group B, member 1), is a nuclear receptor that in humans is encoded by the ESRRA (Estrogen Related Receptor Alpha) gene. (wikipedia.org)
  • On this basis, estrogens are considered to promote prolactinoma growth also in humans. (growkudos.com)
  • Estrogen receptor beta inhibits angiogenesis and growth of T47D breast cancer xenografts. (semanticscholar.org)
  • Estrogen inhibits RANKL-stimulated osteoclastic differentiation of human monocytes through estrogen and RANKL-regulated interaction of estrogen receptor-alpha with BCAR1 and Traf6. (pubfacts.com)
  • Estrogen inhibits renal cell carcinoma cell progression through estrogen receptorbeta activation. (koreascience.or.kr)
  • The human estrogen receptor (hER) exists as two subtypes, hER alpha and hER beta, that differ in the C-terminal ligand-binding domain and in the N-terminal transactivation domain. (nih.gov)
  • Synthetic peptide within Human Estrogen Receptor alpha conjugated to keyhole limpet haemocyanin. (abcam.com)
  • Synthetic peptide corresponding to Human Estrogen Receptor alpha aa 21-32. (abcam.com)
  • MA1-310 detects both the steroid occupied and unoccupied forms of the estrogen receptor (ER) alpha from human samples. (thermofisher.com)
  • For example, the inventors previously cloned the human estrogen receptor-related orphan receptor alpha1 cDNA and demonstrated that it enhances estrogen responsiveness of the lactoferrin gene promoter in transfected human endometrial carcinoma cells. (nih.gov)
  • Estrogen-related receptor α in human breast carcinoma as a potent prognostic factor," Cancer Research , vol. 64, no. 13, pp. 4670-4676, 2004. (hindawi.com)
  • Increased expression of estrogen-related receptor α (ERR α ) is a negative prognostic predictor in human prostate cancer," International Journal of Cancer , vol. 120, no. 11, pp. 2325-2330, 2007. (hindawi.com)
  • Oestrogen receptor-related receptor alpha (ERR α ) and oestrogen receptors (ER α and ER β ) exhibit different gene expression in human colorectal tumour progression," European Journal of Cancer , vol. 41, no. 10, pp. 1487-1494, 2005. (hindawi.com)
  • Methods: The present study focuses a library of fatty acid coumarin conjugates as ligands to the ligand-binding domain of the human estrogen receptor α (PDB ID 2IOG) and their binding affinities using GLIDE module of Schrodinger after ascertaining their drug-likeness with QIKPROP. (eurekaselect.com)
  • Human estrogen-related receptor 2 (hERR2, ESRRB, ERRbeta, NR3B2) belongs to a class of nuclear receptors that bind DNA through sequence-specific interactions with a 5'-AGGTCA-3' estrogen response element (ERE) half-site in the major groove and an upstream 5'-TNA-3' site in the minor groove. (caltech.edu)
  • Altogether, our results indicate that the Mdm2 oncoprotein and stress-inducing agents complexly and differentially regulate ER alpha stability and transcriptional activity in human cancer cells. (cnrs.fr)
  • Given this widespread role for estrogen in human physiology, it is not surprising that estrogen influence the pathophysiology of numerous diseases, including cancer (of the reproductive tract as breast, endometrial but also colorectal, prostate. (inserm.fr)
  • Profiling of estrogen up- and down-regulated gene expression in human breast cancer cells: insights into gene networks and pathways underlying estrogenic control of proliferation and cell phenotype. (semanticscholar.org)
  • The human estrogen receptor (ER) is a ligand-based gene transcription factor. (bu.edu)
  • We conclude that estrogen directly, but only partially, curtails human osteoclast formation. (pubfacts.com)
  • Full length Clone DNA of Human estrogen-related receptor alpha with N terminal HA tag. (sinobiological.com)
  • Synthetic peptide derived from C-terminal of human estrogen receptor alpha. (abcam.co.jp)
  • Probing the Human Estrogen Receptor-Alpha Binding Requirements for Phe" by Christopher McCullough, Terrence S. Neumann et al. (marquette.edu)
  • Various estrogen analogs were synthesized and tested for binding to human ERα using a fluorescence polarization displacement assay. (marquette.edu)
  • Estrogen-related receptor alpha in human breast carcinoma as a potent prognostic factor. (koreascience.or.kr)
  • Estrogen-related receptor alpha and estrogen-related receptor gamma associate with unfavorable and favorable biomarkers, respectively, in human breast cancer. (koreascience.or.kr)
  • Synthetic peptide within Human Estrogen Receptor alpha aa 50-150. (abcam.co.jp)
  • The results presented here demonstrate that p53 upregulates estrogen receptor-alpha (ER alpha) expression in the human breast cancer cell line MCF-7. (bioscientifica.com)
  • Truncated estrogen receptor alpha 46-kDa isoform in human endothelial cells: relationship to acute activation of nitric oxide synthase. (ox.ac.uk)
  • The estrogen receptor (ER), a member of the steroid receptor family, mediates the stimulatory effects of estrogens and the inhibitory effects of antiestrogens in breast cancer and other estrogen target cells. (asm.org)
  • The selective estrogen receptor-alpha down-regulator (SERD) fulvestrant is more effective than tamoxifen in blocking estrogen receptor-alpha action. (aacrjournals.org)
  • ER alpha deletion in T cells contributed to multiple aspects of T cell function, including reducing T cell activation and proliferation and increasing the expression of Foxp3, which encodes a critical transcription factor for the differentiation and function of regulatory T cells. (utu.fi)
  • Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen. (patentgenius.com)
  • Although my promoter studies indicated that estrogen does not regulate PRP4K directly at the transcriptional level, I identified several putative binding sites for miRNAs in the 3ʹ-UTR of PRP4K. (dal.ca)
  • To determine whether the effects of p53 on the expression of ER alpha were due to changes in transcription, deletion mutants of the ER alpha promoter were used. (bioscientifica.com)
  • Moreover, the estrogen receptor alpha, ERα, could bind in vitro estrogen responsive cis -elements, EREs, that are present in the MUC1 promoter. (biomedcentral.com)
  • ERRalpha and ERRbeta (formerly ERR1 and ERR2) form a subgroup of the steroid/thyroid/retinoid receptor family. (klamar-reagent.com)
  • Interaction of phytoestrogens with estrogen receptors alpha and beta. (nih.gov)
  • The gene regulatory effects of both ERα and ERβ are exerted after their interaction with a specific DNA sequence, the estrogen response element (ERE). (aacrjournals.org)
  • This minor groove interaction is mediated by a C-terminal extension (CTE) of the DNA binding domain and is unique to the estrogen-related receptors. (caltech.edu)
  • A search for TF binding matrices revealed that the majority of the binding sites identified comprise one or more Estrogen Response Element and the remaining show binding matrixes for other TFs known to mediate ER interaction with chromatin by tethering, including AP2, E2F and SP1. (biomedcentral.com)
  • Cooperative interaction between retinoic acid receptor-alpha and estrogen receptor in breast cancer. (koreascience.or.kr)
  • Direct interaction between estrogen receptor alpha and NF-kappaB in the nucleus of living cells. (qxmd.com)
  • These results identify a pivotal role for ERα in the hypothalamus, in addition to its role in the estrogen-driven maturation through theca and interstitial cells of the ovary. (wikipedia.org)
  • Estrogen receptor alpha -silenced MCF7 breast cancer cells. (edwardbetts.com)
  • Results: Proliferation is estrogen receptor-alpha-regulated in HGSOC cells in vitro and in vivo, and is partly dependent on 3-D context. (aacrjournals.org)
  • SNIPER(ER) induced degradation of ERα and inhibited estrogen-dependent expression of pS2 gene in an estrogen-dependent breast cancer MCF-7 cells. (aacrjournals.org)
  • Previous studies have indicated that malignant cervical cells tend to lose Estrogen Receptor alpha (ER-α) expression in the cervical epithelium while maintaining ER-α expression in the stromal cells. (eurekaselect.com)
  • Inhibition of PRDX1/2 antioxidant activity with adenanthin dramatically reduced ER alpha levels in breast cancer cells. (lu.se)
  • By ChIP-Seq we identified 9702 ERβ and 6024 ERα binding sites in estrogen-stimulated cells, comprising sites occupied by either ERβ, ERα or both ER subtypes. (biomedcentral.com)
  • We found that ER alpha deletion in T cells reduced their pathogenic potential in a mouse model of colitis and correlated with transcriptomic changes that affected T cell activation. (utu.fi)
  • Thus, these data demonstrate that ER alpha in T cells plays an important role in inflammation and suggest that ER alpha-targeted immunotherapies could be used to treat autoimmune disorders. (utu.fi)
  • Impact of estrogen receptor beta on gene networks regulated by estrogen receptor alpha in breast cancer cells. (semanticscholar.org)
  • Moreover, our preliminary data suggest that overexpression of p68 in cells may additionally coactivate ERα in an estrogen-independent manner, a finding that may have implications in the development of resistance to endocrine therapies. (biomedcentral.com)
  • TRAP1 has been shown to be estrogen up-regulated in estrogen receptor α (ERα) positive ovarian cancer cells. (biomedcentral.com)
  • Here, I have demonstrated that treatment with tamoxifen, an inhibitor of estrogen signalling, can decrease PRP4K levels in MCF7 breast cancer cells reducing cell sensitivity to the taxane paclitaxel. (dal.ca)
  • Thus, this study suggests that PRP4K is novel estrogen regulated kinase, whose expression can be inhibited by tamoxifen in ER+ breast cancer cells which in turn impact cell response to taxanes. (dal.ca)
  • Genistein and Trichostatin A Induction of Estrogen Receptor Alpha Gene Expression, Apoptosis and Cell Growth Inhibition in Hepatocellular Carcinoma HepG 2 Cells', Asian Pacific Journal of Cancer Prevention , 18(12), pp. 3445-3450. (waocp.org)
  • Sanaei, M., Kavoosi, F., Salehi, H. Genistein and Trichostatin A Induction of Estrogen Receptor Alpha Gene Expression, Apoptosis and Cell Growth Inhibition in Hepatocellular Carcinoma HepG 2 Cells. (waocp.org)
  • Treatment with calcium also resulted in dose dependent growth of MCF-7 cells suggesting that calcium has estrogen-like effects on cell proliferation. (georgetown.edu)
  • Epidermal growth factor-induced signaling in breast cancer cells results in selective target gene activation by orphan nuclear receptor estrogen-related receptor alpha. (koreascience.or.kr)
  • In our current work we tried to separate membrane-initiated estrogen receptor signaling from the overall estrogenic effect in MCF-7 breast carcinoma cells. (biomedcentral.com)
  • This study, involving 30 women with endometriosis and 28 controls without endometriosis, aimed to investigate relative levels of estrogen receptor alpha (ERα) splice variants in the endometrium of women with and without endometriosis and investigate potential links to the severity of pain. (oncotarget.com)
  • Estrogen stimulation of ERα is known to stimulate cell proliferation in breast tissue. (wikipedia.org)
  • Estrogen receptors are involved in pathological processes including breast cancer, endometrial cancer, and osteoporosis. (thermofisher.com)
  • It also decreases the expression of estrogen receptor alpha in ER-positive breast cancer. (edwardbetts.com)
  • Most of the primary breast cancers express estrogen receptor α (ERα) and they show estrogen-dependent proliferation. (aacrjournals.org)
  • Since tamoxifen antagonizes estrogen in breast cancers, it is widely used to treat the primary breast cancers. (aacrjournals.org)
  • More than 70% of all breast cancer cases are estrogen receptor alpha-positive (ERα). (unam.mx)
  • Background: In view of the estrogenic receptor inhibitory properties of coumarin nucleus, long chain nature of fatty acid and anti-breast cancer activity of fatty acids, it was proposed to attach long chain fatty acids at 3rd,4th and 7th position of coumarin nucleus and evaluate for their anti-breast cancer activity through suitable in-vitro methods. (eurekaselect.com)
  • Several of these miRNAs, including miR-21, are estrogen regulated and/or deregulated in breast cancer. (dal.ca)
  • Thus this study aimed to clarify the correlation of different IHC-based subtypes of breast tumors with $ER{\alpha}$ methylation in Iranian breast cancer patients. (koreascience.or.kr)
  • The prevalence of estrogen and progestron receptors in breast cancer in Shariati general hospital of Tehran. (koreascience.or.kr)
  • Our data indicate that loss of estrogen receptor expression is a likely indicator of poor prognosis in prolactinomas and that a routine assessment of the estrogen receptor expression status should be considered, like in breast cancer. (growkudos.com)
  • Loss of estrogen receptor α (ERα) expression and gain of TWIST (TWIST1) expression in breast tumors correlate with increased disease recurrence and metastasis and poor disease-free survival. (umm.ac.id)
  • Deregulation of estrogen pathway has been linked to the pathophysiology of breast cancer. (georgetown.edu)
  • Among the various hormonal types of breast cancer, those that are estrogen receptor (ER) positive account for the majority. (koreascience.or.kr)
  • Among the estrogen related receptors, estrogen related receptor ${\alpha}$ is known to have a potential role in breast cancer and is one of the therapeutic target. (koreascience.or.kr)
  • Estrogen-related receptor alpha is critical for the growth of estrogen receptornegative breast cancer. (koreascience.or.kr)
  • Estrogen receptor prevents p53-dependent apoptosis in breast cancer. (koreascience.or.kr)
  • In breast cancer FOXM1 expression is linked with estrogen receptor (ERα) activity and resistance to endocrine therapies, with high levels correlated with poor prognosis. (biomedcentral.com)
  • Approximately 70% of breast cancers are estrogen receptor (ERα)-positive and there is increasing evidence to suggest that ERα and FOXM1 act as co-regulators. (biomedcentral.com)
  • Various side chains with amino and/or sulfur functions were linked to C3 to convert the furans to estrogen antagonists without residual estrogenic activity. (uni-regensburg.de)
  • However, in the last two decades it became apparent that a subpopulation (10-15%) of ERs are membrane-bound and this receptor pool also contributes to the overall estrogenic effect. (biomedcentral.com)
  • Finally, ERα appears to mediate positive feedback effects of estrogen on the brain's secretion of GnRH and LH, by way increasing expression of kisspeptin in neurons of the arcuate nucleus and anteroventral periventricular nucleus. (wikipedia.org)
  • Although classical studies have suggested that negative feedback effects of estrogen also operate through ERα, female mice lacking ERα in kisspeptin-expressing neurons continue to demonstrate a degree of negative feedback response. (wikipedia.org)
  • The effects of estrogen on osteoclast survival and differentiation were studied using CD14-selected mononuclear osteoclast precursors from peripheral blood. (pubfacts.com)
  • Paisley, Jacquelyn Carrie, "Differential Effects of Estrogen Receptor alpha Suppression by Antisense Oligodeoxynucleotides in the Medial Preoptic Area and the Medial Amygdala on Male Rat Mating Behavior. (gsu.edu)
  • These differences render membrane estrogen receptors ideal pharmacological targets in cancer therapy. (biomedcentral.com)
  • It is hypothesized that estrogen stimulation of ERα may trigger the release of growth factors, such as epidermal growth factor or insulin-like growth factor-1, which in turn regulate bone development and maintenance. (wikipedia.org)
  • Our results revealed that the HaCaT keratinocytes expressed both ER-alpha and -beta, and thus are well-suited for studying the effects of ER agonists on epidermal regeneration. (uni-muenchen.de)
  • Betulinic acid and ursolic acid have potential use as therapeutic agents against estrogen-dependent tumors. (greenmedinfo.com)
  • Moreover, cell lines derived from such tumors are estrogen-responsive and, when transplanted into nude mice, form tumors that respond to the antiestrogen ICI 182780. (ovid.com)
  • $ER{\alpha}$ methylation was found in 25 of 28 (89.3%) basal tumors, 21 of 24 (87.5%) Her2+ tumors, 18 of 34 (52.9%) luminal A tumors and 7 of 14 (50%) luminal B tumors. (koreascience.or.kr)
  • Pituitary prolactin tumors are more frequently encountered in women than in men and estrogens are known to induce pituitary prolactin tumors in rodents. (growkudos.com)
  • Small tumors expressing large amount of receptors were mainly found in women and large proliferating receptor negative tumors in men. (growkudos.com)
  • Estrogens might in fact restrain the growth of well-differentiated tumors, whereas the growth of aggressive prolactinomas seems estrogen independent. (growkudos.com)
  • Isoflavone glycoside binds weakly to both receptors and estrogen receptor-dependent transcriptional expression is poor. (nih.gov)
  • Thus, EGF activates ERα by increasing intracellular calcium which binds to the LBD, thereby activating the receptor. (georgetown.edu)
  • Recent studies show that the anion nitrite binds to and activates estrogen receptor-alpha (ERα). (georgetown.edu)
  • Despite high expression of estrogen receptor-alpha in ~80% of HGSOC and some small but promising clinical trials of endocrine therapy, estrogen receptor-alpha has been understudied as a target in this disease. (aacrjournals.org)
  • The expression of estrogen receptor-alpha had no effect on survival. (aacrjournals.org)
  • In the present study, we provide information on the mechanisms through which estrogens affect the expression patterns of selected markers, thus modulating keratinocyte proliferation and differentiation;in addition, we demonstrate that the pharmacological activation of ER-alpha and -beta has a direct impact on wound healing. (uni-muenchen.de)
  • Membrane-localised oestrogen receptor alpha and beta influence neuronal activity through activation of metabotropic glutamate receptors. (semanticscholar.org)
  • Estrogen receptor alpha consists of several domains including the transcription activation function-1 domain (AF-1), the DNA-binding domain, the hinge domain and the ligand-binding domain (AF-2). (bio-rad-antibodies.com)
  • The two receptors can be found co-expressed and play specific, often opposite, roles, with ERβ being able to modulate the effects of ERα on gene transcription and cell proliferation. (biomedcentral.com)
  • Membrane estrogen receptor-alpha interactions with metabotropic glutamate receptor 1a modulate female sexual receptivity in rats. (semanticscholar.org)
  • This adult ovarian phenotype suggests that in the absence of ERα, estrogen is no longer able to perform negative feedback on the hypothalamus, resulting in chronically elevated LH levels and constant ovarian stimulation. (wikipedia.org)
  • Une stimulation par l'estradiol permet la liaison du récepteur aux éléments de réponse aux estrogènes (ERE) dans les séquences régulatrices de gènes cibles, en association avec des cofacteurs transcriptionnels, et modifie les profils d'expression des gènes, augmente la prolifération cellulaire et accélère la croissance tumorale. (umontreal.ca)
  • Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations with biological characterand distinct differences among SRC coactivator family members. (patentgenius.com)
  • In contrast, the steroid receptor coactivator SRC-1 increases transcriptional activity of all of these receptors. (asm.org)