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.
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.
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)
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.
Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.
The unspecified form of the steroid, normally a major metabolite of TESTOSTERONE with androgenic activity. It has been implicated as a regulator of gonadotropin secretion.
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.
Tumors or cancer of the human BREAST.
The surgical removal of one or both ovaries.
PLANT EXTRACTS and compounds, primarily ISOFLAVONES, that mimic or modulate endogenous estrogens, usually by binding to ESTROGEN RECEPTORS.
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.
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.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
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.
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.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
A cell line derived from cultured tumor cells.
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 THRB gene (also known as NR1A2, THRB1, or ERBA2 gene) as several isoforms produced by alternative splicing. Mutations in the THRB gene cause THYROID HORMONE RESISTANCE SYNDROME.
Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure.
Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.
The 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.
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 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.
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.
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)
Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.
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.
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.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
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.
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.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in neoplastic tissue.
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 phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
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.
Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.
Non-steroidal compounds with estrogenic activity.
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.
Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.
Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.
A group of FLAVONOIDS characterized with a 4-ketone.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A subunit of the interleukin-12 receptor. It plays a role in receptor signaling by associating with TYK2 KINASE 1.
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.
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.
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.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
Established cell cultures that have the potential to propagate indefinitely.
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 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.
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.
An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
The relationship between the dose of an administered drug and the response of the organism to the drug.
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)
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.
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.
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.
A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM.
Cell surface receptors for INTERLEUKIN-12. They exist as dimers of beta 1 and beta 2 subunits. Signaling from interleukin-12 receptors occurs through their interaction with JANUS KINASES.
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.
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)
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.
Tumors or cancer of the PROSTATE.
A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.
DNA sequences encoding the beta chain of the T-cell receptor. The genomic organization of the TcR beta genes is essentially the same in all species and is similar to the organization of Ig genes.
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.
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.
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.
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.
An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.
A subunit of the interleukin-12 receptor. It plays a role in receptor signaling by associating with JANUS KINASE 2.
One of the PPAR nuclear transcription factors.
A PDGF receptor that binds specifically to the PDGF-B chain. It contains a protein-tyrosine kinase activity that is involved in SIGNAL TRANSDUCTION.
An OOCYTE-containing structure in the cortex of the OVARY. The oocyte is enclosed by a layer of GRANULOSA CELLS providing a nourishing microenvironment (FOLLICULAR FLUID). The number and size of follicles vary depending on the age and reproductive state of the female. The growing follicles are divided into five stages: primary, secondary, tertiary, Graafian, and atretic. Follicular growth and steroidogenesis depend on the presence of GONADOTROPINS.
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.

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. (1/1528)

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)

Expression of oestrogen receptor alpha and beta mRNA in corpus luteum of human subjects. (2/1528)

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)

Expression of estrogen receptor beta1, beta2, and beta5 messenger RNAs in human breast tissue. (3/1528)

A triple-primer PCR assay was developed, based on the coamplification of estrogen receptor (ER)-beta1, -beta2, and -beta5 cDNAs, to investigate the relative expressions of the corresponding mRNAs in breast cancer lines and in 53 independent breast tumors. The expression of ER-beta2 and ER-beta5 mRNAs was higher than that of ER-beta1 mRNA in both cancer cell lines and breast tumors. In breast tumors, increases in the ER-beta2:ER-beta1 and ER-beta5:ER-beta1 mRNA expression ratios were observed, which positively correlated with the level of tumor inflammation and tumor grade, respectively. A trend toward an increase of these ratios was also found in tumors, as compared to the normal adjacent breast tissue available for 13 cases. Our data suggest that changes in the relative expression of ER-beta1, -beta2, and -beta5 mRNAs occur during breast tumorigenesis and tumor progression.  (+info)

Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha and ER beta. (4/1528)

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)

Ligand-independent recruitment of SRC-1 to estrogen receptor beta through phosphorylation of activation function AF-1. (5/1528)

The estrogen receptors (ERs) alpha and beta possess a constitutive N-terminal activation function (AF-1) whose activity can be modulated by kinase signalling pathways. We demonstrate here that phosphorylation of AF-1 by MAP kinase (MAPK) leads to the recruitment of steroid receptor coactivator-1 (SRC-1) by ER beta in vitro. Enhancement of the interaction between SRC-1 and ER beta AF-1 is also observed in vivo in cells either treated with EGF or expressing activated Ras. Two serine residues in ER beta AF-1, of which one is contained within a motif present in other steroid receptors, are critical for physical interaction with SRC-1 and transcriptional activation. Our results establish a role for nuclear receptor phosphorylation in the recruitment of SRC-1 and provide a molecular basis for ligand-independent activation by ER beta via the MAPK pathway.  (+info)

Expression of human estrogen receptor-alpha and -beta, progesterone receptor, and androgen receptor mRNA in normal and malignant ovarian epithelial cells. (6/1528)

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)

Variant estrogen and progesterone receptor messages in human vascular smooth muscle. (7/1528)

BACKGROUND: Estrogens stimulate growth of breast or uterine cells but have the opposite effect on vascular smooth muscle cells, in which they protect against coronary artery disease with or without concomitant administration of progesterone. A possible cause of differences in hormone action is variable tissue-specific expression of hormone receptor. Therefore, we analyzed the structure of estrogen receptors (ERs) and progesterone receptors (PRs) in human vascular smooth muscle. METHODS AND RESULTS: RNA was isolated from human vascular smooth muscle, and the functional domains of ER-alpha and PR were characterized by reverse transcriptase and polymerase chain reaction. Interestingly, in addition to wild-type ER-alpha and PR, 5 variant ER-alpha and 2 variant PR transcripts were found. These variants contained precise deletions of exons encoding regions of the hormone-binding domain. The PR transcripts lacked exon 4 (PRDelta4) and exon 6 (PRDelta6). The ER-alpha transcripts were missing exon 4 (ERDelta4), exon 5 (ERDelta5), exon 6 (ERDelta6), exon 7 (ERDelta7), and exons 6 and 7, (ERDelta6,7). ER-beta variants were also detected. The PR variants were functionally characterized, and PRDelta6 was found to be a dominant-negative transcription inhibitor of wild-type receptors. Variant PR was present in premenopausal women but absent in postmenopausal women. CONCLUSIONS: Variant PR and ER transcripts are extensively expressed in human vascular smooth muscle. The complex tissue-specific effects of sex hormones may be mediated by the expression of heterogeneous forms of their cognate receptors. The presence of variant ERs and PRs may be of importance in altering the physiological effects of estrogens or progestins in vascular smooth muscle.  (+info)

Oestrogen receptor alpha and beta mRNA expression in human endometrium throughout the menstrual cycle. (8/1528)

We examined the localization of oestrogen receptor (ER) beta mRNA in the human endometrium throughout the menstrual cycle using non-radioactive in-situ hybridization with Brigati-tailed oligonucleotides. The findings were compared with those of ERalpha in order to examine the possible biological significance of ERbeta in the human endometrium. Both ERalpha and ERbeta mRNA expression were detected in all major human uterine cell types, including glandular epithelial cells, stromal cells and smooth muscle cells of the uterine wall, at every menstrual cycle stage. However, ERalpha mRNA expression was more prominent than that of ERbeta in all cell types throughout the menstrual cycle. In proliferative phase endometrium, ERalpha mRNA was expressed in both glandular epithelial and stromal cells, while ERbeta mRNA was expressed predominantly in glandular epithelial cells. Although the same pattern was observed in the secretory phase, both the ERalpha and ERbeta mRNA expression was relatively weaker. These results suggest that oestrogenic effects occur predominantly through ERalpha, but that ERbeta may also play a role in the modulation of oestrogenic action, especially on glandular epithelial cells in the human endometrium throughout the menstrual cycle.  (+info)

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The molecular mechanisms involved in adrenocortical tumorigenesis are still not completely understood. In this study, using the H295R cell line as a model system, we investigated the role of estrogens and estrogen receptor (ER) alpha and ER beta in the growth regulation of adrenocortical tumors. We demonstrated that H295R cells are able to convert androgens to estrogens by a constitutive expression of active cytochrome P450 aromatase protein and express ER beta to a greater extent than ER alpha. Moreover, physiological concentrations of 17beta-estradiol (E2) determined an increase of thymidine incorporation, suggesting the presence of an autocrine mechanism in maintaining H295R cell proliferation. Evaluating the response to ER antagonists like 4-hydroxytamoxifen (OHT) and ICI 182 780 (ICI), we observed an up-regulation of ER beta and a dose-dependent inhibition of H295R cell proliferation. Whereas ICI determined the growth arrest of H295R cells, OHT induced morphological changes that were ...
TY - JOUR. T1 - Oestrogen receptor beta in breast cancer. T2 - good, bad or still too early to tell?. AU - Speirs, Valerie. N1 - Copyright 2002 John Wiley & Sons, Ltd.. PY - 2002/6. Y1 - 2002/6. N2 - Two oestrogen receptors (ERs), ER alpha and ER beta, have been identified. ER alpha is by far the better characterized and is an established predictive marker in breast cancer which influences decisions on whether or not to give adjuvant anti-oestrogens, such as tamoxifen. In contrast, the function of ER beta in breast pathobiology is unclear, partly because most studies have focused on its mRNA rather than the protein. In this review, the significance of ER beta in the human breast is reviewed with respect to recent literature and its possible implications are discussed.. AB - Two oestrogen receptors (ERs), ER alpha and ER beta, have been identified. ER alpha is by far the better characterized and is an established predictive marker in breast cancer which influences decisions on whether or not to ...
Prostate cancer is the commonest, non-cutaneous cancer in men. At present, there is no cure for the advanced, castration-resistant form of the disease. Estrogen has been shown to be important in prostate carcinogenesis, with evidence resulting from epidemiological, cancer cell line, human tissue and animal studies. The prostate expresses both estrogen receptor alpha (ERA) and estrogen receptor beta (ERB). Most evidence suggests that ERA mediates the harmful effects of estrogen in the prostate, whereas ERB is tumour suppressive, but trials of ERB-selective agents have not translated into improved clinical outcomes. The role of ERB in the prostate remains unclear and there is increasing evidence that isoforms of ERB may be oncogenic. Detailed study of ERB and ERB isoforms in the prostate is required to establish their cell-specific roles, in order to determine if therapies can be directed towards ERB-dependent pathways. In this review, we summarise evidence on the role of ERB in prostate cancer and
BioAssay record AID 404864 submitted by ChEMBL: Activation of human estrogen receptor beta expressed in HEK293 cells at 1 nM beta-galactosidase reporter gene assay relative to control.
Estrogen Receptor beta兔多克隆抗体(ab3576)可与小鼠, 大鼠, 羊, 人, 猪, 非人类灵长类动物样本反应并经WB, IHC, ICC, Inhib, ICC/IF实验严格验证,被11篇文献引用…
article{c840d53a-503c-49f5-b0d1-477f7736c951, abstract = {Acute treatment with 17β-estradiol provides effective neuroprotection during the first days after acute brain injury, however, effects of chronic activation of estrogen receptor beta (ERβ) on recovery of function after experimental stroke have not been investigated. The present study, therefore, was conducted to test if delayed treatment with the specific ERβ ligand 4-(1-phenyl-cyclohexyl)-phenol (AC-131) improves recovery of lost neurological function after permanent focal stroke induced by photothrombosis in adult Sprague-Dawley rats. Treatment was initiated on day 2 after photothrombosis and AC-131 (1, 10, and 50mg/kg) was administered by daily subcutaneous injections for 14 days. On day 2, 4, 6, 8, 11, 14, and 17 after photothrombosis, functional deficits were assessed by the paw placement test, a standardized grip strength test and an adhesive removal test. Daily treatment with AC-131 significantly improved test scores in all ...
Sequence variants of estrogen receptor beta and risk of prostate cancer in the National Cancer Institute Breast and Prostate Cancer Cohort Consortium. ...
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In brief, the currently available estrogen therapies used to treat menopausal symptoms are non-selective to both of the two known estrogen receptors, alpha and beta. Because of this non-selectivity, all estrogens marketed to treat menopausal symptoms have the potential to cause elevated risks for breast and uterine cancers due to the proliferative effects on breast and uterine tissues mediated through the estrogen receptor alpha. Selective activation of the estrogen receptor beta, however, does not lead to proliferation of MCF-7 breast cancer cell lines or an increase for uterine cancer in mouse xenograph models. Bionovo is taking advantage of the differential effects caused by the two estrogen receptors on cancer formation by developing selective estrogen receptor beta drugs. The mechanism of action of MF101 as a selective estrogen receptor beta therapy may provide a safer, long-term alternative to treat menopausal symptoms ...
TY - JOUR. T1 - Body mass index, mammographic density, and breast cancer risk by estrogen receptor subtype. AU - Shieh, Yiwey. AU - Scott, Christopher G.. AU - Jensen, Matthew R.. AU - Norman, Aaron D.. AU - Bertrand, Kimberly A.. AU - Pankratz, V. Shane. AU - Brandt, Kathleen R. AU - Visscher, Daniel W. AU - Shepherd, John A.. AU - Tamimi, Rulla M.. AU - Vachon, Celine M. AU - Kerlikowske, Karla. PY - 2019/4/3. Y1 - 2019/4/3. N2 - Background: Obesity and elevated breast density are common risk factors for breast cancer, and their effects may vary by estrogen receptor (ER) subtype. However, their joint effects on ER subtype-specific risk are unknown. Understanding this relationship could enhance risk stratification for screening and prevention. Thus, we assessed the association between breast density and ER subtype according to body mass index (BMI) and menopausal status. Methods: We conducted a case-control study nested within two mammography screening cohorts, the Mayo Mammography Health Study ...
|p|Erteberel (LY500307) is a potent and selective ERβ (estrogen receptor beta) agonist (EC50 = 0.66 nM). [1]|/p| |p|Estrogen receptors are nuclear hormone receptors that act as a ligand-activated transcription factor. It regulates gene expression, cell p
BioAssay record AID 747467 submitted by ChEMBL: Agonist activity at human estrogen receptor-beta by yeast two-hybrid assay in presence of SRC1.
A molecular ribbon model of estrogen receptor beta, a protein encoded by the ESR2 gene, found primarily in the kidneys, brain, bone, heart, lungs, intestinal mucosa, prostate and endothelial cells. After activated by estrogen hormones, estrogen receptors bind to DNA to regulate gene expression. Abnormal activity by estrogen receptors have been observed in cases of breast cancer, ovarian cancer, colon cancer, prostate cancer and endometrial cancer. The loss of estrogen receptor beta proteins can disrupt the process of apoptosis and are often associated with advanced colon cancer and the development of tumours. - Stock Image C027/6387
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.
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As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
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 ...
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 ...
Davies, M. P. A., ONeill, P. A., Innes, H., Sibson, D. R., Prime, W., Holcombe, C., & Foster, C. S. (2004). Correlation of mRNA for oestrogen receptor beta splice variants ER beta 1, ER beta 2/ER beta cx and ER beta 5 with outcome in endocrine-treated breast cancer. JOURNAL OF MOLECULAR ENDOCRINOLOGY, 33(3), 773-782. doi:10.1677/jme. ...
Rabbit polyclonal Estrogen Receptor beta antibody validated for WB, IHC, ICC, Inhibition, ICC/IF and tested in Human, Mouse and Rat. Referenced in 28…
Additional Physical Format: Online version: Berko, Frances G. Management of brain damaged children. Springfield, Ill., Thomas [] (OCoLC)
ERβ agonists significantly and specifically inhibit the proliferation of BLM melanoma cells.(A) BLM cells were treated with different doses of the classical ER
マウス・モノクローナル抗体 ab288 交差種: Ms,Hu,Mk,Bb 適用: WB,IHC-P,IHC-Fr,Flow Cyt,ChIP,ICC/IF…Estrogen Receptor…
Esr2 - Esr2 (untagged ORF) - Rat estrogen receptor 2 (ER beta) (Esr2), (10 ug) available for purchase from OriGene - Your Gene Company.
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BACKGROUND: The causes of prostate cancer are poorly understood, but genetic factors may be more important than for many other malignancies, and dietary phytoestrogens may be protective. Because phytoestrogens bind tightly to the estrogen receptor-beta, we conducted an epidemiologic investigation of synergistic effects between phytoestrogen intake and estrogen receptor-beta gene polymorphisms. METHODS: We performed a population-based case-control study in Sweden. All participants reported their phytoestrogen intake and donated a blood sample. We identified four haplotype-tagging single nucleotide polymorphisms (htSNPs) and genotyped these htSNPs in 1314 prostate cancer patients and 782 controls. Odds ratios were estimated by multivariate logistic regression. Interactions between phytoestrogen intake and estrogen receptor-beta SNPs on prostate cancer risk were evaluated considering both multiplicative and additive effect scales. RESULTS: We found a significant multiplicative interaction (P = ...
TY - JOUR. T1 - The roles of membrane estrogen receptor subtypes in modulating dopamine transporters in PC-12 cells. AU - Alyea, Rebecca A.. AU - Laurence, Stephanie E.. AU - Kim, Sung H.. AU - Katzenellenbogen, Benita S.. AU - Katzenellenbogen, John A.. AU - Watson, Cheryl S.. PY - 2008/8. Y1 - 2008/8. N2 - The effects of 17β-estradiol (E2) on dopamine (DA) transport could explain gender and life-stage differences in the incidence of some neurological disorders. We tested the effects of E2 at physiological concentrations on DA efflux in nerve growth factor-differentiated rat pheochromocytoma cells that express estrogen receptors (ER) α, ERβ, and G-protein coupled receptor 30 (GPR30), and DA transporter (DAT). DAT efflux was determined as the transporter-specific loss of 3H-DA from pre-loaded cells; a 9-15 min 10-9 M E2 treatment caused maximal DA efflux. Such rapid estrogenic action suggests a non-genomic response, and an E2-dendrimer conjugate (limited to non-nuclear actions) caused DA ...
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 - ...
Feedback regulation of luteinizing hormone-releasing hormone (LHRH) neurons by estradiol plays important roles in the neuroendocrine control of reproduction. Recently, we found that the majority of LHRH neurons in the rat contain estrogen receptor-beta (ER-beta) mRNA, whereas, they seemed to lack ER …
PubMed journal article: Dietary intake of phytoestrogens, estrogen receptor-beta polymorphisms and the risk of prostate cancer. Download Prime PubMed App to iPhone, iPad, or Android
In the present study we used leptin-deficient ob/ob mice, an animal model of type 2 diabetes. ob/ob mice become hyperglycemic and hyperinsulinemic from the age of 1-2 months, at which point body weight also starts to increase, compared with wild-type animals (Westman 1968). At 5-6 months of age, the animals reach maximum body weight, which remains stable until 13-17 months of age (Westman 1968). Hyperglycemia and hyperinsulinemia also increase with age, and the highest mean blood glucose and insulin values are obtained in 4-6 month old animals.. We have shown that treatment of 3-month-old female ob/ob mice with E2 for 30 days significantly decreased basal blood glucose levels and improved glucose tolerance and insulin sensitivity (Gao et al. 2006). The insulin response to glucose in vivo was also significantly improved. In this study, we demonstrate that glucose tolerance and insulin sensitivity are significantly improved in ob/ob mice from 7 days of treatment with E2, which confirms the strong ...
Prostate cancer is the leading cause of cancer death in men of the Western world. A castration-resistant prostate cancer (CRPC) eventually will arise when a local restricted prostate carcinoma was not cured duly by radical prostatectomy or radiation therapy. According to the study by the Hormone and Obesity Center Bahnhofsalle, posted in PubMed, phytoestrogens feature tumour preventive characteristics and most probably are involved in the low incidence rate of hormone related cancers in Asian countries. Phytoestrogens such as isoflavones can have a marked impact on the most essential therapy target of CRPC i.e. the androgen receptor. Furthermore, functional analyses solidified the notion of such drugs as androgen antagonistic. Phytoestrogens commonly feature low toxicity combined with a potential of targeted therapy. Thus, these drugs qualify for conceivable implementation in prostate cancer patients under active surveillance. In addition, relapse prevention with these drugs after radical ...
TY - JOUR. T1 - Generation of an estrogen receptor beta-iCre knock-in mouse. AU - Cacioppo, Joseph A.. AU - Koo, Yongbum. AU - Lin, Po Ching Patrick. AU - Osmulski, Sarah A.. AU - Ko, Chunjoo D.. AU - Ko, Chemyong. N1 - Funding Information: The authors thank Dr. Lori Raetzman for ROSA26 reporter mice, Dr. Jing Yang for FLP mice, Red Gal reagent, and support in cassette generation, Dr. Fuming Pan for embryonic stem cell DNA insertion and generation of chimeric mice, Stephanie Martynenko for tissue collection, and Karen Doty for histological assistance. PY - 2016/1/1. Y1 - 2016/1/1. N2 - Summary: A novel knock-in mouse that expresses codon-improved Cre recombinase (iCre) under regulation of the estrogen receptor beta (Esr2) promoter was developed for conditional deletion of genes and for the spatial and/or temporal localization of Esr2 expression. ESR2 is one of two classical nuclear estrogen receptors and displays a spatiotemporal expression pattern and functions that are different from the other ...
TY - JOUR. T1 - The activation by estrogen receptor agonists of the BKCa-channel in human cardiac fibroblasts. AU - Wang, Ya Jean. AU - Lin, Ming Wei. AU - Wu, Sheng-Nan. AU - Sung, Ruey J.. PY - 2007/5/1. Y1 - 2007/5/1. N2 - The agonists selective for estrogen receptor (ER)-α (4,4′,4′′-(4-propyl-[1H]-pyrazole-1,3,5-triyl) tris-phenol, PPT) and ER-β (2,3-bis(4-hydroxyphenyl)-propionitrile, DPN) are known to stimulate ER-α and ER-β receptors, respectively. It remains unknown whether these two agents regulate the activity of ion channels via a direct stimulation. In this study, we tested the hypothesis that DPN or PPT stimulates the large-conductance Ca2+-activated K+ (BKCa) channels in cultured human cardiac fibroblasts (HCFs). In whole-cell configuration, depolarizing pulses evoked K+ outward currents in an outward rectification in HCFs, the amplitude of which was increased in the presence of DPN or PPT. In inside-out patches, the activity of BKCa-channel with a conductance of 167 ± 8 ...
Natalie Angier article explains recent discovery of second estrogen receptor, protein through which potent hormone can convey its messages to bodys cells; estrogen receptor beta, considered only last year just a backup to true receptor, has now been found in organs with little or no evidence of alpha receptor, and that were never considered to be under estrogens dominance; organs include lungs, kidneys, intestines, bladder and colon; diagram; beta receptor also exists in certain cells of bone and blood vessels where original receptor is scarce; discovery could help resolve longstanding puzzles about estrogens effects on female bodies, and influence breast cancer and heart treatment; new work also alters view of estrogen as female hormone, since receptor was found while screening rodent prostate tissue in search of androgen receptor; Dr Jan-Ake Gustafson comments on work with colleagues at Karolinska Institute in Sweden (M)
The researchers found that proteins involved in binding and breaking down oestrogen were present in pre-cancerous and cancerous HNSCC cells grown in the laboratory. These proteins were also present in tissue from both males and females, and levels of a protein that binds to oestrogen (called oestrogen receptor beta) and the CYP1B1 enzyme (the product of the CYP1B1 gene) were higher in HNSCC tissue than normal tissue.. Treating pre-cancerous HNSCC cells with oestrogen in the laboratory caused the CYP1B1 gene to increase in activity about threefold. However, when cancerous HNSCC cells were treated with oestrogen, an increase in CYP1B1 gene activity was not seen. Treating pre-cancerous HNSCC cells with oestrogen did not affect their movement or division. When the researchers switched off the CYP1B1 gene in these cells, however, they became less able to move and divide.. Exposing pre-cancerous HNSCC cells to oestrogen also reduced the number of cells that died by cell suicide (apoptosis). Treating ...
The estrogen receptor beta (ERβ) is the predominant ER in the human colonic epithelium. Levels of ERβ are reduced in colorectal cancer compared to normal colon tissue. In a previous study, we generated ERβ-expressing colon cancer cells and showed that ERβ inhibits proliferation as well as colon cancer xenograft growth, as a consequence of ERβ mediated inhibition of cell-cycle pathways.. The present study was conducted to investigate genome wide changes by ERβ in three human colon cancer cell lines (SW480, HT29 and HCT116). They have very low or no levels of ERβ expression and were transduced with lentivirus containing an ERβ expression cassette. Microarray studies showed that ERβ regulated 623, 643 and 124 genes for SW480, HT29 and HCT116, respectively.. Comparisons showed few genes in common for the three cell lines. However, over representation analysis showed that several themes, such as cell proliferation, cell communication and apoptosis were regulated in all of the cell ...
Sárvári, Miklós and Kalló, Imre and Hrabovszky, Erik and Solymosi, Norbert and Liposits, Zsolt (2017) Ovariectomy Alters Gene Expression of the Hippocampal Formation in Middle-Aged Rats. Endocrinology, 158 (1). pp. 69-83. ISSN 0013-7227 (print), 1945-7170 (online) Vastagh, Csaba and Rodolosse, Annie and Solymosi, Norbert and Liposits, Zsolt (2016) Altered Expression of Genes Encoding Neurotransmitter Receptors in GnRH Neurons of Proestrous Mice. Frontiers in cellular neuroscience, 10. pp. 1-16. ISSN 1662-5102, ESSN: 1662-5102 Molnár, Csilla and Sárvári, Miklós and Vastagh, Csaba and Maurnyi, Csilla and Fekete, Csaba and Liposits, Zsolt and Hrabovszky, Erik (2016) Altered gene expression profile of the hypothalamic arcuate nucleus of male mice suggests profound developmental changes in peptidergic signaling. NEUROENDOCRINOLOGY. ISSN 0028-3835 (In Press) Bálint, Flóra and Liposits, Zsolt and Farkas, Imre (2016) Estrogen Receptor Beta and 2-arachidonoylglycerol Mediate the Suppressive ...
The chemical structure of ERα ligand determines the agonistic or antagonistic biological responses by the virtue of their binding mode, conformation of the liganded-ERα complex and the context of the cellular function.
Clark JH, Schrader WT, OMalley BW (1992) Mechanisms of ac- Of great interest was the finding that E2 adminis- tion of steroid hormones. In Wilson J, ed. Textbook of Endocri- tration induced a marked increase in nuclear AR label- nology. Philadelphia, WB Saunders, 35-90 ing and a decrease in cytoplasmic AR staining. This Couse JF, Lindzey JKG, Gustafsson JA, Korach KS (1997) Tissue distribution and quantitative analysis of estrogen receptor-alpha suggests that estrogens, even in the absence of circulat- (ERalpha) and estrogen receptor-beta (ERbeta) messenger ribo- ing androgens, can activate AR, leading to transfer of nucleic acid in the wild-type and ERalpha-knockout mouse. En- the receptors from the cytoplasm to the nucleus. Such an activation of AR might result from direct interac- El-Alfy M, Luu-The V, Huang XF, Berger L, Labrie F, Pelletier G (1999) Localization of type 5 17␤-hydroxysteroid dehydroge- tion of E2 with AR. Other mechanisms, such as an in- nase, 3␤-hydroxysteroid ...
Estrogen Receptor-α Knock-Out Mouse Model is an eagle-i resource of type Mus musculus at Charles Drew University of Medicine and Science.
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Rabbit polyclonal GABA A Receptor beta 3 antibody validated for WB, IHC and tested in Mouse and Rat. Immunogen corresponding to synthetic peptide
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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 ...
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 - 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 ...
Rheumatoid arthritis (RA) is a chronic inflammatory disease that produces synovial proliferation and joint erosions. The pathologic lesions of RA are driven through the production of inflammatory mediators in the synovium mediated, in part, by the transcription factor NF-κB. We have identified a non-steroidal estrogen receptor ligand, WAY-169916, that selectively inhibits NF-κB transcriptional activity but is devoid of conventional estrogenic activity. The activity of WAY-169916 was monitored in two models of arthritis, the HLA-B27 transgenic rat and the Lewis rat adjuvant-induced model, after daily oral administration. In both models, a near complete reversal in hindpaw scores was observed as well as marked improvements in the histological scores. In the Lewis rat adjuvant model, WAY-169916 markedly suppresses the adjuvant induction of three serum acute phase proteins: haptoglobin, α1-acid glycoprotein (α1-AGP), and C-reactive protein (CRP). Gene expression experiments also demonstrate a global
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 ...
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 ...
In the early 1980s, McMichael and Potter (12) proposed the hypothesis that female sex hormones may be protective against colorectal cancer, citing the protective effect of parity, a potential protective effect of high-dose oral contraceptives, and biological evidence that sex hormones modify hepatic cholesterol metabolism and reduce bile acids. Since then, observational studies (1) and randomized controlled trials (2, 13) have found a protective effect of exogenous hormonal therapy on risk of colorectal cancer. Exogenous and endogenous estrogens have been shown to stimulate cell proliferation and tumor development in the breast and uterus. These protumorigenic effects are thought to be mediated through the estrogen receptor subtype ERα, which is predominant in these tissues (14). It has been hypothesized that estrogens may be protective against colorectal cancer because the predominant estrogen receptor subtype in the colon, ERβ, has been shown to inhibit transcription and induce apoptosis on ...
During the later stages of follicular growth (Figure 2), activins and estradiol, the predominant estrogen in humans, enhance the actions of FSH (65, 66) (Figure 2). In mice, activins activate the transcription factors SMAD2/3 and SMAD4, which coordinately regulate several FSH-induced genes including those encoding the cell cycle regulator CCND2 and the steroidogenic enzyme aromatase (67), which converts theca cell-derived androgens to estradiol. Estradiol, acting primarily via estrogen receptor beta (ERS2), has recently been shown to suppress expression of phosphodiesterase 1C (Pde1c), thereby increasing intracellular levels of cAMP induced by FSH (66). Because activins facilitate proliferation of granulosa cells and enhance FSH actions, in part by increasing estradiol, these interactions may help explain why, when activin actions are unopposed by inhibins (as occurs in mice lacking inhibin α subunit, which is encoded by Inha), activins promote GCT growth. The WNT signaling target β-catenin ...
Tumors from 58 ovarian cancer patients contained less messenger RNA for the ER beta than found in ovarian samples from healthy patients, said Lazennec, whose team included scientists from France and Italy. To understand how the loss of ER beta affected the ovarian cells during cancer progression, the gene for ER beta was replaced in ovarian cancer cell lines that no longer expressed the estrogen-triggered nuclear receptor. The ER beta reintroduced into the cancer cell lines did not share the classic functions attributed to estrogen receptors, including induction of progesterone receptor expression and fibuline-1C, and it s ability to decrease the expression of the cyclin D1 gene was completely opposite of it s counterpart, ER beta ...
Background: Cigarette smoking (smoking), hormone therapy (MHT), and folate intake (folate) are each thought to influence colorectal cancer (CRC) risk, but the underlying molecular mechanisms remain incompletely defined. Expression of estrogen receptor beta (ESR2) has been associated with CRC stage and survival. Methods: In this prospective cohort study, we examined smoking, MHT, and folate -associated CRC risks by ESR2protein expression level among participants in the Iowa Womens Health Study (IWHS). Self-reported exposure variables were assessed at baseline. Archived, paraffin-embedded CRC tissue specimens were collected and evaluated for ESR2protein expression by immunohistochemistry. Multivariate Cox regression models were fit to estimate relative risks (RRs) and 95% confidence intervals (CIs) for associations between smoking, MHT, or folate and ESR2-defined CRC subtypes. Results: Informative environmental exposure and protein expression data were available for 491 incident CRC cases. ...
Dear Mr. Berko: My husband and I are 77. We both had jobs for 40 years, raised four children and lived frugally; our home is paid for, and we managed to save $285,000 in two IRAs, which are now worth $223,000 from the market collapse. This money is now in CDs earning 1.75 percent, and we need more income. Together, we get $21,000 from Social Security after health insurance payments, plus $4,300 from our IRA CDs. We really need a new car, our air conditioning and heating system must be replaced, and we have the same kitchen and bathrooms when we bought the house new 37 years ago.
This study investigates the molecular mechanisms by which critical genes are differentially regulated in the male and female brain. The hormone, estrogen, is cr...
Perturbation of endocrine signaling during critical developmental windows has been implicated in decreased fertility and reproductive disorders. Using the developmental origins of disease paradigm, we examined the differentiation of the Müllerian duct into female reproductive tract structures. Müllerian duct development involves estrogen signaling, and is thus susceptible to disruption via environmental contaminants. The alligator is a useful model for studying reproductive system development, because sex determination is not genetic, but reliant on egg incubation temperature. To identify and characterize critical events in the differentiation of the alligator oviduct, we investigated pathways leading to sex reversal. Alligator eggs incubated at a temperature that produces 100% males (33.5 C) were treated with estradiol-17beta (E2) or 4,4,4-(4-Propyl-[1H]-pyrazole-1,3,5 -triyl)trisphenol (PPT), a specific agonist for estrogen receptor alpha (ERα), at a stage just prior to sex ...
The estrogen receptor alpha (ERα) is the central transcriptional regulator of ductal mammary epithelial lineage specification and is an important p...
IL3 Receptor beta antibody [N1N3] (colony stimulating factor 2 receptor, beta, low-affinity (granulocyte-macrophage)) for FACS, WB. Anti-IL3 Receptor beta pAb (GTX104118) is tested in Human samples. 100% Ab-Assurance.
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anti-PDGF Receptor beta (Phospho-Tyr1021), pAb is a polyclonal antibody that crossreacts with human, mouse protein. Works in WB. Important for Inflammation, Oxidative Stress, ROS, Immunology research.
Studies with live cells demonstrate that agonist and antagonist rapidly (within minutes) modulate the subnuclear dynamics of estrogen receptor alpha (ER) and st
By exploiting high-throughput microscopy and a new cell line, researchers have uncovered how the transcription regulator estrogen receptor-α can
Cardarine, often also referred to as GW 1516 or GW 501516, is a chemical compound classified as a selective agonist of certain receptors in the human body. The receptors that the compound activates are known as Peroxisome Proliferator-Activator Receptor Beta. These receptors are sometimes also referred to as NR1C2.
"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- ...
Imamov, Otabek (15 July 2005). "Estrogen Receptor beta in Health and Disease". Biology of Reproduction. 73 (5): 866-871. doi: ... The biological effects of estrogens (and xenoestrogens) are mediated through the estrogen receptor (ER). Estrogen receptors, ... neurotransmitter receptors such as the serotonin receptor, dopamine receptor, norepinephrine receptor), orphan receptors (e.g ... by the estrogen receptor ER CALUX bioassay consisting of the human T-47D breast tumor cell line expressing estrogen receptors ( ...
"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 ...
"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 ...
"Structure-based design of estrogen receptor-beta selective ligands". J. Am. Chem. Soc. 126 (46): 15106-19. doi:10.1021/ ... Radiolabeled [16α-125I]iodo-E2 has been employed in imaging to study the estrogen receptor. 16α-LE2 Clomestrone Mytatrienediol ... a high affinity ligand for the estrogen receptor". J. Steroid Biochem. 25 (5A): 615-8. doi:10.1016/0022-4731(86)90002-6. PMID ... 16α-Iodo-E2, or 16α-iodoestradiol, is a synthetic, steroidal, potent estrogen with slight preference for the ERα over the ERβ ...
... of the inflammatory response in experimental arthritis is mediated via estrogen receptor alpha but not estrogen receptor beta ... Nelson AW, Tilley WD, Neal DE, Carroll JS (2014). "Estrogen receptor beta in prostate cancer: friend or foe?". Endocr. Relat. ... ERB-26 is a synthetic estrogen and a selective agonist of the ERβ. It is the active enantiomer of the racemic mixture ERB-79. ... It has no antagonistic activity at either receptor. ERB-26 is active in prevention of prostate cancer development in ...
Nelson AW, Tilley WD, Neal DE, Carroll JS (2014). "Estrogen receptor beta in prostate cancer: friend or foe?". Endocr. Relat. ... Khalil RA (2013). "Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease". Biochem. ... "Oestrogen-mediated cardioprotection following ischaemia and reperfusion is mimicked by an oestrogen receptor (ER)alpha agonist ... "Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists". J. ...
"Estrogen receptor beta selective nonsteroidal estrogens: seeking clinical indications". Expert Opin Ther Pat. 20 (4): 507-34. ... Paterni I, Granchi C, Katzenellenbogen JA, Minutolo F (November 2014). "Estrogen receptors alpha (ERα) and beta (ERβ): subtype- ... "Estrogen receptor-{beta}-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice". J. Biol. Chem. ... "Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue ...
Weiser MJ, Wu TJ, Handa RJ (2009). "Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S- ... Deroo BJ, Buensuceso AV (2010). "Minireview: Estrogen receptor-beta: mechanistic insights from recent studies". Mol. Endocrinol ... 51-. ISBN 978-1-4816-0836-7. Kudwa AE, McGivern RF, Handa RJ (2014). "Estrogen receptor β and oxytocin interact to modulate ... synthesis and evaluation of estrogen receptor β-selective ligands". J. Med. Chem. 55 (1): 528-37. doi:10.1021/jm201436k. PMC ...
October 2003). "Evaluation of an estrogen receptor-beta agonist in animal models of human disease". Endocrinology. 144 (10): ... Harris HA (2006). "Preclinical characterization of selective estrogen receptor beta agonists: new insights into their ... "Reflections on the discovery and significance of estrogen receptor beta". Endocrine Reviews. 26 (3): 465-78. doi:10.1210/er. ... and highly selective agonist of the ERβ subtype of the estrogen receptor. It is used in scientific research to elucidate the ...
"Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... "Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta". Endocrinology. 139 (10): 4252-4263. doi: ... However, continued exposure inhibited the growth of the uterus and decreased levels of estrogen receptors within uterine tissue ... when women have a much lower level of estrogen in their bodies, or when used conjunctively with anti-estrogen therapies. Most ...
"Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta". Endocrinology. 139 (10): 4252-4263. doi: ... Coumestrol has about the same binding affinity for the ER-β estrogen receptor as 17β-estradiol, but much less affinity than 17α ... although the estrogenic potency of coumestrol at both receptors is much less than that of 17β-estradiol. Because of the ...
"Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes". J. Immunol. 180 (1): 630-6. doi: ... Roman-Blas JA, Castañeda S, Cutolo M, Herrero-Beaumont G (2010). "Efficacy and safety of a selective estrogen receptor β ... "Modulators of Vascular Sex Hormone Receptors and their Effects in Estrogen-Deficiency States Associated with Menopause". Recent ... WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ. It is 100-fold selective ...
"Estrogen receptor alpha interacts with mitochondrial protein HADHB and affects beta-oxidation activity". Molecular & Cellular ... Trifunctional enzyme subunit beta, mitochondrial (TP-beta) also known as 3-ketoacyl-CoA thiolase, acetyl-CoA acyltransferase, ... This gene encodes the beta subunit of the mitochondrial trifunctional protein, a catalyst of mitochondrial beta-oxidation of ... "Trifunctional enzyme subunit beta, mitochondrial". Cardiac Organellar Protein Atlas Knowledgebase (COPaKB). Archived from the ...
"Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta". J. Med. Chem. 52 (3): 858-67. doi: ... FERb 033 is a synthetic, nonsteroidal estrogen that was synthesized in 2009 and is used in scientific research. It is a potent ...
"Alternative O-glycosylation/O-phosphorylation of the murine estrogen receptor beta". Biochemistry. 39 (38): 11609-11620. doi: ... has been observed on other proteins including murine estrogen receptor β, RNA Pol II, tau, p53, CaMKIV, p65, β-catenin, and α- ... "Glucose Stimulates Protein Modification by O-linked GlcNAc in Pancreatic Beta Cells: Linkage of O-linked GlcNAc to Beta Cell ... Sakabe, K; Wang, Z; Hart, GW (2010-11-16). "Beta-N-acetylglucosamine (O-GlcNAc) Is Part of the Histone Code". Proceedings of ...
"CYP7B generates a selective estrogen receptor beta agonist in human prostate". J. Clin. Endocrinol. Metab. 89 (6): 2928-35. doi ... Tang W, Norlin M (2006). "Regulation of steroid hydroxylase CYP7B1 by androgens and estrogens in prostate cancer LNCaP cells". ...
Estrogen (alpha and beta) and androgen receptor-mediated responses in yeast assays.. ...
"Evaluation of ligand selectivity using reporter cell lines stably expressing estrogen receptor alpha or beta". Biochemical ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Estriol is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ.[1][6][7] It is a far less potent ... Oettel M, Schillinger E (6 December 2012). Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens ...
Zhou, Z.; Zhou, J.; Du, Y. (2012). "Estrogen Receptor Alpha Interacts with Mitochondrial Protein HADHB and Affects Beta- ... a receptor triggered by estrogen. In 2009, Taylor et al. identified a human mitochondrial protein, monolysocardiolipin ... MTP is a hetero-octamer composed of four alpha and four beta subunits: HADHA HADHB The three functions are 2-enoyl coenzyme A ( ... Fatty acid beta-oxidation (FAO) and oxidative phosphorylation (OXPHOS) are two major metabolism pathways in the mitochondria. ...
"Estrogen receptor {beta}1 expression is regulated by miR-92 in breast cancer". Cancer Research. 70 (11): 4778-84. doi:10.1158/ ... Down regulation of oestrogen receptors β1 and α have been associated with various forms of breast cancer. While the mode of ... this was demonstrated by growing MCF-7 cells in oestrogen depleted conditions and adding antagonists to the oestrogen receptors ... PTCH is the receptor for Sonic hedgehog (SHH). This SHH signalling pathway is crucial during early development and SSH is the ...
"Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Hackenberg, Reinhard; Turgetto, Inga; Filmer, Angelika; Schulz, Klaus-Dieter (1993). "Estrogen and androgen receptor mediated ...
"Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor modulators. Estrogen receptor modulators. ...
Hypersensitivity to estrogens in "at risk" breast lesions may be due to a decrease in the estrogen beta receptor. In total, ... including estrogen beta receptor) in pre-cancerous breast lesions. Fibulin 1, induced by estrogens, is secreted in excess by ... Cancer Inst., 82, (1990), p. 602-606 P.Roger , J.A.Gustafson, et al., « Decreased expression of estrogen receptor beta protein ... 1. Pharmacology of sex steroid receptors. Some androgens are estrogenic when they interact with estrogen receptors (ER) (1-3). ...
... estrogen receptor ligands possessing estrogen receptor beta antagonist activity". Journal of Medicinal Chemistry. 47 (24): 5872 ... 95-. ISBN 978-2-88919-078-2. Cytoplasmic and Nuclear Receptors-Advances in Research and Application: 2012 Edition. ... and highly selective antagonist of ERβ that is used in scientific research to study the function of this receptor. It possesses ...
... through protein interaction with estrogen receptor beta". Genomics. 69 (1): 63-71. doi:10.1006/geno.2000.6299. PMID 11013076. " ... Haribabu B, Snyderman R (1993). "Identification of additional members of human G-protein-coupled receptor kinase multigene ...
In humans, it is hypothesized to bind to the estrogen receptor beta (ERβ) protein-coding gene. The primary sources of 20- ... "Estrogen receptor beta is involved in skeletal muscle hypertrophy induced by the phytoecdysteroid ecdysterone". Molecular ... action of 20-Hydroxyecdysone on human muscle cells is relatively selective activation of the beta form of the estrogen receptor ... Indeed, the main receptor of these hormone signals - the ecdysone receptor - is an intracellular protein. 20-Hydroxyecdysone ...
... estrogen receptor alpha, which is responsible for the negative feedback estradiol-LH loop, and estrogen receptor beta, which is ... "Converse regulatory functions of estrogen receptor-alpha and -beta subtypes expressed in hypothalamic gonadotropin-releasing ... Estrogen levels may affect thyroid behavior.[32] For example, during the luteal phase (when estrogen levels are lower), the ... Since these GABA receptors are inhibitory, nerve cells with more delta receptors are less likely to fire than cells with lower ...
Duarte FH, Jallad RS, Bronstein MD (November 2016). "Estrogens and selective estrogen receptor modulators in acromegaly". ... Salicylic acid is a topically applied beta-hydroxy acid that stops bacteria from reproducing and has keratolytic properties.[ ... C. acnes' ability to bind and activate a class of immune system receptors known as toll-like receptors (TLRs), especially TLR2 ... It is usually combined with an estrogen to avoid menstrual irregularities and estrogen deficiency.[113] The medication appears ...
Massive overdose can be associated with increased sympathetic activity and thus require treatment with beta-blockers.[18] ... T4 and T3 bind to thyroid receptor proteins in the cell nucleus and cause metabolic effects through the control of DNA ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... "Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists". J. Lipid Res ... 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 ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER).[26][27] ... "Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on ... "The stimulation of cell proliferation by quercetin is mediated by the estrogen receptor". (primary). Molecular Nutrition & Food ...
... and are analogous to selective estrogen receptor degraders (SERDs) like fulvestrant (a drug used to treat estrogen receptor- ... Effects of the anti-androgen TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one) on the secretion of gonadotrophins". Acta ... 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][ ...
Bufe B, Hofmann T, Krautwurst D, et al. (2002). "The human TAS2R16 receptor mediates bitter taste in response to beta- ... 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 ... Receptor ukusa tip 2 član 19 je protein koji je kod ljudi kodiran TAS2R19 genom.[1] ...
Low-density lipoproteins are taken into the cell by LDL receptor-mediated endocytosis in clathrin-coated pits, and then ... The role of cholesterol in such endocytosis can be investigated by using methyl beta cyclodextrin (MβCD) to remove cholesterol ... estrogens, and testosterone (the sex hormones), and their derivatives. It provides the basic structure of all the steroids. In ... By serving as ligands for specific receptors on cell membranes, the apolipoproteins that reside on the surface of a given ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... amyloid-beta binding. • signal transducer activity. • Wnt-protein binding. • protein binding. • protein kinase binding. • ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... estratrien-17 beta-yl)-3-hydroxypropylamine, a novel amino-estrogen". Steroids. 45 (2): 159-70. PMID 3841425.. ... "In vivo estrogen bioactivities and in vitro estrogen receptor binding and transcriptional activities of anticoagulant synthetic ... estratrien-17 beta-yl)-3-hydroxypropylamine; an amino-estrogen with prolonged anticoagulant and brief estrogenic effects". ...
The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... Studies suggest that neurotrophic factors have a protective role against amyloid beta toxicity.[85] ... 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. • ...
GnRH and gonadotropin receptor modulators. Androgens and antiandrogens. Estrogens and antiestrogens. Progestogens and ... See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators • GnRH and gonadotropins ... is achieved through receptor downregulation by internalization of receptors.[11] Generally this induced and reversible ... They are agonists of the GnRH receptor and work by increasing or decreasing the release of gonadotropins and the production of ...
... activation of the D2 receptor promoter by members of the retinoic acid receptor-retinoid X receptor family". Proceedings of the ... Isotretinoin has a low affinity for retinoic acid receptors (RAR) and retinoid X receptors (RXR), but may be converted ... transcriptional activation of the dopamine D2 receptor - in addition to serotonin and glutamate receptors - is regulated by ... Isotretinoin is also thought to affect the serotonergic system - it increases expression of 5-HT1A receptors in the pre- ...
TGF beta receptors: Endoglin/Alk-1/SMAD4 (Hereditary hemorrhagic telangiectasia). *TGFBR1/TGFBR2 (Loeys-Dietz syndrome) ... Firstly, oestrogen is used in tablet or gel form in order to maximise breast development, then a combination of oestrogen and ... Oestrogen (females) or testosterone (males) is essential for maintaining bone density.[18] Deficiency in either testosterone or ... Early morning hormonal testing including FSH, LH, testosterone, oestrogen and prolactin.. *GnRH and/or hCG stimulation test to ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... What is more clear is that DDE is a weak androgen receptor antagonist and can produce male genital tract abnormalities.[16][17] ...
Ribociclib are US FDA approved CDK4 and CDK6 inhibitors for the treatment of estrogen receptor positive/ HER2 negative advanced ... Beta adrenergic receptor kinase (EC 2.7.11.15). *Beta adrenergic receptor kinase. *Beta adrenergic receptor kinase-2 ... 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 ...
Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... Properties of lysylalanyl-beta-naphthylamide hydrolysis: inhibition by cations, distribution in tissues, and subcellular ... receptor antagonists (e.g., domperidone, metoclopramide, risperidone). *Estrogens (e.g., estradiol). *Progestogens (e.g., ...
Keutmann HT, Hua QX, Weiss MA (1992). "Structure of a receptor-binding fragment from human luteinizing hormone beta-subunit ... Posteljica: hCG • HPL • estrogen • progesteron. Druge endokrine. žlezde. Pankreas: glukagon • insulin • amilin • somatostatin • ... hCG beta) and luteinizing hormone beta (hLH beta) in the human testis". FEBS Lett. 343 (3): 229-33. DOI:10.1016/0014-5793(94) ... Beta polipeptid luteinizirajućeg hormona (lutropinska podjedinica beta) je protein koji je kod ljudi kodiran LHB genom.[1][2] ...
General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... Premarin (conjugated estrogens, introduced in 1942) and Prempro (a combination estrogen-progestin pill, introduced in 1995) ... Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ... beta-receptor agonists, follicle stimulating hormone, luteinising hormone, LHRH. gamolenic acid, gonadotropin release inhibitor ...
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-).[ ... As IGF2 promotes development of fetal pancreatic beta cells, it is believed to be related to some forms of diabetes mellitus. ... 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 ...
receptor binding. • neurotrophin TRKB receptor binding. • growth factor activity. Cellular component. • cytoplasm. • ... Studies suggest that neurotrophic factors have a protective role against amyloid beta toxicity.[84] ... The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... regulation of receptor activity. • activation of phospholipase C activity. • neurotrophin TRK receptor signaling pathway. • ...
Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... receptor antagonists (e.g., domperidone, metoclopramide, risperidone). *Estrogens (e.g., estradiol). *Progestogens (e.g., ... Activators: beta-Hydroxy beta-methylbutyric acid. *Hydroxynorketamine. *Leucine. *NV-5138. *Inhibitors: Rapalogs: Everolimus ... It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. ...
Timus: Timozin (Timozin α1, Timozin beta) • Timopoietin • Timulin Organi za varenje: Želudac: gastrin • grelin • Duodenum: CCK ... Chegini N, Rong H, Dou Q, et al. (1996). "Gonadotropin-releasing hormone (GnRH) and GnRH receptor gene expression in human ... Posteljica: hCG • HPL • estrogen • progesteron. Druge endokrine. žlezde. Pankreas: glukagon • insulin • amilin • somatostatin • ... Alfa-endorfin • Beta-endorfin • Gama-endorfin • α-neo-endorfin • β-neo-endorfin ...
The ACTH receptor is a seven-membrane-spanning G protein-coupled receptor.[7] Upon ligand binding, the receptor undergoes ... beta-endorphin. 237-267 met-enkephalin. 237-241 In order to regulate the secretion of ACTH, many substances secreted within ... 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 ... Zha J, Huang YF (September 2009). "[TGF-beta/Smad in prostate cancer: an update]". Zhonghua Nan Ke Xue (in Chinese). 15 (9): ... 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][ ...
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat ... gde X predstavlja hidrofobni ostatak koji je bilo aromatičan ili beta-razgranati alifatik. N-terminalni region varira između ... Tahikininski receptor 1 (TACR1, neurokininski 1 receptor, NK1R, ili receptor supstance P, SPR) je G protein spregnuti receptor ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
... and not exogenous human prolactin induces estrogen receptor α and prolactin receptor expression and increases estrogen ... "Mouse models of transforming growth factor beta impact in breast development and cancer". Endocr. Relat. Cancer. 12 (4): 749- ... "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. ...
Beta-glukan[12]. Literatura[uredi - уреди , uredi izvor]. *↑ Thomas J. Kindt, Richard A. Goldsby, Barbara Anne Osborne, Janis ... Lang, TJ (2004). "Estrogen as an immunomodulator". Clin Immunol 113: 224-230. PMID 15507385. doi:10.1016/j.clim.2004.05.011. ... Insights from Genetic Models of Hormones and Hormone Receptor Deficiency". Endocrine Reviews 21: 292-312. PMID 10857555. doi: ... vakcine (BCG vakcina, Melanoma vakcina) • beta-glukan (Lentinan) • Mifamurtid • tiazolidin (Pidotimod) • heterociklična ...
Timus: Timozin (Timozin α1, Timozin beta) • Timopoietin • Timulin Organi za varenje: Želudac: gastrin • grelin • Duodenum: CCK ... "Exploring the role of sex steroids through studies of receptor deficient mice". Journal of Molecular Medicine (Berlin, Germany ... Posteljica: hCG • HPL • estrogen • progesteron. Druge endokrine. žlezde. Pankreas: glukagon • insulin • amilin • somatostatin • ...
ESTROGEN RECEPTOR BETA. A, B. 240. Homo sapiens. Mutation(s): 0 Gene Names: ESR2, ESTRB, NR3A2. ... Design and Structure of Stapled Peptides Binding to Estrogen Receptors.. Phillips, C., Roberts, L.R., Schade, M., Bazin, R., ... Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors ... Here we describe the design of a series of novel stapled peptides that bind the coactivator peptide site of estrogen receptors ...
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 ...
Rabbit polyclonal Estrogen Receptor beta antibody validated for WB, IHC, ICC, Inhibition, ICC/IF and tested in Human, Mouse and ... Anti-Estrogen Receptor beta antibody. See all Estrogen Receptor beta primary antibodies. ... Immunofluorescent analysis using Estrogen Receptor beta polyclonal antibody (ab3576) shows nuclear localization of Estrogen ... All lanes : Anti-Estrogen Receptor beta antibody (ab3576) at 1/2000 dilution. Lane 1 : CAL region of Human brain - Whole cell ...
Pharmacological Actions : ER alpha receptor up-regulation, ER beta receptor up-regulation, Estrogen Receptor Modulators, ... Estrogen Receptor Modulators, Selective estrogen enzyme modulator (SEEM), Selective Estrogen Receptor Modulators ... Pharmacological Actions : Antiproliferative , Apoptotic, Estrogen Receptor Modulators. Additional Keywords : Estrogen Receptor ... 14 Abstracts with Estrogen Receptor Beta Research. Filter by Study Type. Animal Study. ...
... and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. ... Binds estrogens with an affinity similar to that of ER-alpha, ... sp,Q9PTU5,ESR2_CHICK Estrogen receptor beta OS=Gallus gallus OX ... Estrogen receptor betaAdd BLAST. 472. Proteomic databases. PaxDb, a database of protein abundance averages across all three ... IPR028355 ER-beta/gamma. IPR021064 Estrogen_rcpt_beta_N. IPR035500 NHR_like_dom_sf. IPR000536 Nucl_hrmn_rcpt_lig-bd. IPR001723 ...
... and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform ... suppresses ER-alpha and ER-beta1 mediated transcriptional activation and may act as a dominant negative regulator of estrogen ... Binds estrogens with an affinity similar to that of ER-alpha, ... Estrogen receptor betaAdd BLAST. 530. Amino acid modifications ... Cluster: Estrogen receptor beta. 23. Q62986-3. Q62986-4. UPI000A30F704. D3ZQD5. UPI000157E37D. D4AEI3. UPI000157E37C. Mus ...
Disruption of estrogen receptor beta gene impairs spatial learning in female mice. Proc Natl Acad Sci U S A. 2002 Mar 19;99(6): ... Disruption of estrogen receptor beta gene impairs spatial learning in female mice. Proc Natl Acad Sci U S A. 2002 Mar 19;99(6): ... Estrogen receptor (ER)beta knockout mice reveal a role for ERbeta in migration of cortical neurons in the developing brain. ... Estrogen receptor alpha, not beta, is a critical link in estradiol-mediated protection against brain injury. Proc Natl Acad Sci ...
... in estrogen-related tumors and understanding the potential role of ERs in the pathophysiology of cancer. Objectives: To ... oncological research has been focused on evaluating estrogen receptors (ERs) ... Objectives: To investigate the significance of estrogen receptor beta (ERβ) in melanoma. Methods: We prospectively evaluated ER ... Background: oncological research has been focused on evaluating estrogen receptors (ERs) in estrogen-related tumors and ...
Estrogen receptor beta. A, B. 241. Homo sapiens. Mutation(s): 0 Gene Names: ESR2, NR3A2, ESTRB. ... Structure-Based Design Of Estrogen Receptor-beta Selective Ligands. Manas, E.S., Unwalla, R.J., Xu, Z.B., Malamas, M.S., Miller ... CRYSTAL STRUCTURE OF ESTROGEN RECEPTOR BETA COMPLEXED WITH WAY-397. *DOI: 10.2210/pdb1U9E/pdb ... We present the structure-based optimization of a series of estrogen receptor-beta (ERbeta) selective ligands. X-ray cocrystal ...
ER beta) Antibody Products from leading suppliers on Biocompare. View specifications, prices, citations, reviews, and more. ... Your search returned 394 Estrogen Receptor 2 (ER beta) Antibodies across 18 suppliers. ...
"Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists". ... "Human estrogen receptor beta binds DNA in a manner similar to and dimerizes with estrogen receptor alpha". The Journal of ... "Estrogen receptor-beta agonist diarylpropionitrile counteracts the estrogenic activity of estrogen receptor-alpha agonist ... "Tissue distribution and quantitative analysis of estrogen receptor-alpha (ERalpha) and estrogen receptor-beta (ERbeta) ...
... Br J Surg. 2000 Apr;87(4):405-9. doi: 10.1046/j.1365- ... Endocrine therapy for breast cancer is now well established and with the identification of a second oestrogen receptor, ERbeta ... 3 years ago it is timely to review the possible significance of this receptor in breast cancer management. ... Receptors, Estrogen / analysis * Receptors, Estrogen / genetics * Receptors, Estrogen / metabolism* * Selective Estrogen ...
Estrogen-related receptor beta (ERR-β), also known as NR3B2 (nuclear receptor subfamily 3, group B, member 2), is a nuclear ... "Differential and opposing regulation of PAI-1 promoter activity by estrogen receptor alpha and estrogen receptor beta in ... EStrogen Related Receptor Beta) gene .[1] Function. This gene encodes a protein with sequence similarity to the estrogen ... Kruijver FP, Balesar R, Espila AM, Unmehopa UA, Swaab DF (Nov 2003). "Estrogen-receptor-beta distribution in the human ...
EStrogen Related Receptor Beta) gene . This gene encodes a protein with sequence similarity to the estrogen receptor, a member ... "Differential and opposing regulation of PAI-1 promoter activity by estrogen receptor alpha and estrogen receptor beta in ... Estrogen-related receptor beta (ERR-β), also known as NR3B2 (nuclear receptor subfamily 3, group B, member 2), is a nuclear ... "Entrez Gene: ESRRB estrogen-related receptor beta". Giguère V, Yang N, Segui P, Evans RM (Jan 1988). "Identification of a new ...
ER beta)), Authors: Chunyan Zhao, Karin Dahlman-Wright, Jan-Ake Gustafsson. Published in: Atlas Genet Cytogenet Oncol Haematol ... cell-cell signaling zinc ion binding enzyme binding estrogen receptor activity estrogen receptor activity estrogen receptor ... cell-cell signaling zinc ion binding enzyme binding estrogen receptor activity estrogen receptor activity estrogen receptor ... Cellular signaling of estrogen is mediated through two estrogen receptors (ERs), ER alpha and ER beta. The first ER, now known ...
Estrogen receptor beta (human). Find diseases associated with this biological target and compounds tested against it in ...
about estrogen receptor beta negtive cell lines - can anyone give me some suggestion about ER beta negtive cell lines? (Aug/31/ ... I have some problem to get a negtive control of estrogen receptor beta for western blot? anybody have any suggestion? thanks. ... Expression profiling of nuclear receptors in the NCI60 cancer cell panel reveals receptor-drug and receptor-gene interactions. ... if you look at this paper, they profiled all 49 nuclear receptor expressions in 51 human cancer cell lines. In the ...
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 ...
Estrogen Receptor-beta Coactivator Binding Inhibitors ELISA Secondary Assay. ...
... induced estrogen receptor beta in breast cancer cells [39].. *Estrogen receptor beta is coexpressed with ERalpha and PR and ... Both estrogen receptor alpha and estrogen receptor beta agonists enhance cell proliferation in the dentate gyrus of adult ... Estrogen receptor beta (ESR2) polymorphisms in interaction with estrogen receptor alpha (ESR1) and insulin-like growth factor I ... The Ah receptor inhibits estrogen-induced estrogen receptor beta in breast cancer cells. Kietz, S., Thomsen, J.S., Matthews, J ...
Estrogens. Estrogen Antagonists. Selective Estrogen Receptor Modulators. Estrogen Receptor Modulators. Skin Diseases. ... Adjuvant Endocrine Therapy for Estrogen Receptor-beta Positive Triple Negative Breast Cancer (AETNBC). The safety and ... The ER-beta positive TNBC patients who had undergone modified radical mastectomy or breast-conserving surgery were randomly (1: ... Evaluation of Adjuvant Endocrine Therapy for Operable ER-beta Positive, ER-alpha/PR Negative, Her-2 Negative Breast Cancer ...
Estrogen receptor-beta / NR3A2 - data and references - Guide to Pharmacology. *Estrogen receptor-alpha / NR3A1 - data and ... The rat estrogen receptor (ER) exists as two subtypes, ER alpha and ER beta, which differ in the C-terminal ligand binding ... Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.. Kuiper ... 17 beta-estradiol , estrone, genistein , estriol , nafoxidine, 5-androstene-3 beta, 17 beta-diol , 17 alpha-estradiol, ...
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... estrogen receptor-beta polymorphisms and the risk of prostate cancer. Download Prime PubMed App to iPhone, iPad, or Android ... AdultAgedCase-Control StudiesDietEstrogen Receptor betaFoodHumansLignansMaleMiddle AgedPhytoestrogensPolymorphism, Single ... Estrogen receptor beta polymorphism is associated with prostate cancer risk.. *Dietary phytoestrogen, serum enterolactone and ... "Dietary Intake of Phytoestrogens, Estrogen Receptor-beta Polymorphisms and the Risk of Prostate Cancer." The Prostate, vol. 66 ...
... beta is the predominant ER in granulosa cells of the ovary. ERbeta is expressed at high levels in granulosa cell tumors (GCT) ... Transrepression of Estrogen Receptor Beta Signaling by Nuclear Factor-Kappab in Ovarian Granulosa Cells Mol Endocrinol. 2004 ... Estrogen receptor (ER) beta is the predominant ER in granulosa cells of the ovary. ERbeta is expressed at high levels in ... We therefore examined the possibility that activation of these pathways was responsible for the lack of a response to estrogen ...
Abstract 2819: Intestinal estrogen receptor beta attenuates colon cancer signaling pathways in vivo. Linnea Pettersson, Ashish ... Intestinal estrogen receptor beta attenuates colon cancer signaling pathways in vivo [abstract]. In: Proceedings of the ... Abstract 2819: Intestinal estrogen receptor beta attenuates colon cancer signaling pathways in vivo ... Abstract 2819: Intestinal estrogen receptor beta attenuates colon cancer signaling pathways in vivo ...
... cell receptors, biomarkers, diagnostic pathology, immunopathology, and hematology. ... Estrogen Receptor Beta Displays Cell Cycle-Dependent Expression and Regulates the G1 Phase through a Non-Genomic Mechanism in ... but the specific contributions and mechanisms of action of the estrogen receptor beta (ERβ) remain elusive. ... Background: It is well known that estrogens regulate cell cycle progression, ...
Estrogen receptor beta (ER,i ,β,/i,) and G-protein-coupled receptor 1 (GPER1) were immunocytochemically identified in human ... Subtypes of estrogen receptors and their signaling mechanisms identified in HCVECs could be applicable for developing estrogen- ... like compounds to specifically bind to a subtype of estrogen receptors with greater specific action on the cerebral arteries, ... without the estrogen-dependent side effects on the reproductive organs, to prevent cerebral aneurysm formation in menopausal ...
The Efficacy and Safety of a Selective Estrogen Receptor Beta Agonist (LY500307) for Negative Symptoms and Cognitive Impairment ... The Efficacy and Safety of a Selective Estrogen Receptor Beta Agonist (LY500307) for Negative Symptoms and Cognitive Impairment ... Estrogens. Hormones. Hormones, Hormone Substitutes, and Hormone Antagonists. Physiological Effects of Drugs. ... there was no suggestion of ERα receptor activation (i.e., no pattern of TT decreases or feminization AEs) at either dose (25 mg ...
Estrogen, a steroid hormone, is a key regulator of growth and differentiation in a broad range of target tissues and, it is ... Estrogen receptor beta (full length, C-term DDK tag). Not available. Recombinant protein of human estrogen receptor 2 (ER beta ... Estrogen receptor beta antibody. Not available. Rabbit anti-ESR2 (Estrogen Receptor-beta, Phospho-Ser118) polyclonal antibody ( ... Estrogen receptor beta antibody. Not available. Rabbit anti-ESR2 (Estrogen Receptor-beta, Phospho-Ser167) polyclonal antibody ( ...
  • DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual. (abcam.com)
  • There are two different forms of the estrogen receptor, alpha and beta, encoded by separate genes (ESR1 and ESR2, respectively). (linscottsdirectory.com)
  • Microsatellites in the estrogen receptor (ESR1, ESR2) and androgen receptor (AR) genes and breast cancer risk in African American and Nigerian women. (uchicago.edu)
  • Rabbit IgG polyclonal antibody for Estrogen receptor beta(ESR2) detection. (bosterbio.com)
  • We investigated the association of five intronic single-nucleotide polymorphism (SNP) at the estrogen receptor beta (ESR2) gene locus and the susceptibility of developing Alzheimer's disease (AD) in 387 subjects with clinically diagnosed probable AD and 467 cognitively normal individuals derived from eastern Finland. (cdc.gov)
  • 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)
  • The estrogen receptors α ( ESR1 gene) and β ( ESR2 gene) are nuclear proteins. (biomedcentral.com)
  • Summary: A novel knock-in mouse that expresses codon-improved Cre recombinase (iCre) under regulation of the estrogen receptor beta (Esr2) promoter was developed for conditional deletion of genes and for the spatial and/or temporal localization of Esr2 expression. (illinois.edu)
  • ESR2 is one of two classical nuclear estrogen receptors and displays a spatiotemporal expression pattern and functions that are different from the other estrogen receptor, ESR1. (illinois.edu)
  • The National Cancer Institute Breast and Prostate Cancer Cohort Consortium has systematically selected haplotype tagging SNPs in genes along the steroid hormone synthesis, metabolism and binding pathways, including the estrogen receptor beta (ESR2) gene. (ox.ac.uk)
  • By Western blot, this antibody detects an ~55 kDa protein representing ER beta from Rat brain homogenate. (abcam.com)
  • Photomicrograph of human ovary immunostained for estrogen receptor beta using monoclonal antibody Cat. (acris-antibodies.com)
  • Non-transfected (-) and transfected (+) 293T whole cell extracts (30 μg) were separated by 7.5% SDS-PAGE, and the membrane was blotted with Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:5000. (genetex.com)
  • Various tissue extracts (20 μg) were separated by 7.5% SDS-PAGE, and the membrane was blotted with Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:500. (genetex.com)
  • Estrogen Receptor beta antibody [14C8] detects Estrogen Receptor beta protein at nucleus by immunohistochemical analysis. (genetex.com)
  • Estrogen Receptor beta stained by Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:200. (genetex.com)
  • The IHC-P analysis of Estrogen Receptor beta antibody [14C8] was published by Hata S and colleagues in the journal Cancer Med in 2013. (genetex.com)
  • The IHC-P analysis of Estrogen Receptor beta antibody [14C8] was published by Samartzis N and colleagues in the journal Reprod Biol Endocrinol in 2012. (genetex.com)
  • Immunostaining for ERα, ERβ and PgR (progesterone receptor) was performed using monoclonal antibodies against ERα, PgR (DakoCytomation), and polyclonal antibody against ERβ (Chemicon). (biomedcentral.com)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Estrogen Receptor Beta (ERb) in serum, plasma, tissue homogenates, cell lysates, cell culture supernates and other biological fluids. (signetlabs.com)
  • We present the structure-based optimization of a series of estrogen receptor-beta (ERbeta) selective ligands. (rcsb.org)
  • Endocrine therapy for breast cancer is now well established and with the identification of a second oestrogen receptor, ERbeta, 3 years ago it is timely to review the possible significance of this receptor in breast cancer management. (nih.gov)
  • Estrogen receptor beta (ERbeta) in endometrial simple hyperplasia and endometrioid carcinoma. (curehunter.com)
  • Progesterone receptor protein expression was influenced by ERalpha levels and not by ERbeta as shown by regression analysis in non-neoplastic and neoplastic endometrium. (curehunter.com)
  • The estrogen receptor beta (ERbeta) is, together with ERalpha, a member of the nuclear receptor superfamily and a key mediator ofestrogen action. (ens-lyon.fr)
  • Here, we identify a novel level of regulation of estrogen signaling where ERbeta, but not ERalpha, is controlled by circadian clock proteins. (ens-lyon.fr)
  • Furthermore, using small interfering RNA-mediated knockdown assays, we show that the expression levels ofthe circadian regulatory factors directly influence estrogen signaling by regulating the intracellular levels of endogenous ERbeta. (ens-lyon.fr)
  • 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)
  • The purpose of this study was to understand the role of estrogen receptor-beta, (ERbeta) on cortical and cancellous bone during growth and aging by comparing the bone phenotype of 6- and 13-month-old female mice with or without ERbeta. (galileo-training.com)
  • The involvement of estrogen receptor beta (ERbeta) in prostate carcinogenesis has been hypothesized. (inserm.fr)
  • However, the expression pattern of FOXP1 in normal breast tissue is more reminiscent of the second receptor, ERbeta, which has an emerging role as a tumour suppressor in breast cancer and critically may underlie the ability of some ERalpha-negative tumours to respond to tamoxifen. (ox.ac.uk)
  • FOXP1 is not estrogen regulated and silencing FOXP1 expression, using siRNA, did not affect ERalpha, ERbeta or progesterone receptor expression, suggesting ER and FOXP1 co-expression may reflect a common regulatory mechanism. (ox.ac.uk)
  • Objectives: We previously observed increases in lesion calcification in the aortic sinus of ApoEnull mice treated with testosterone (T) associated with suppression of estrogen receptor (ER) alpha but not ERbeta expression. (edu.au)
  • We conclude that ERbeta and the ERalpha/beta ratio is critical for lesion calcification in this model. (edu.au)
  • Analysis by immunohistochemistry for the following antigens was performed: estrogen receptor β (ERβ), ERα, PR (progesterone receptor), AR (androgen receptor), Thyroid transcription factor 1 (TTF1), synaptophysin and for chromograninA. (omicsonline.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)
  • Triple Negative breast cancer (TNBC) is a subtype of breast cancer that lacks the expression of estrogen receptor (ER), progesterone receptor, and human epidermal growth factor receptor 2. (escholarship.org)
  • The aim of this study was to assess the frequency of ERα, ERβ, PgR (progesterone receptor) and HER-2 expression in breast cancer patients with mutated BRCA1 gene and in the control group. (biomedcentral.com)
  • In endometriotic stromal cells, the levels of progesterone receptor (PR), particularly the PR-B isoform, are significantly decreased, leading to a loss of paracrine signaling. (cumhuriyet.edu.tr)
  • In this review, we propose a molecular model that may be responsible for changes in ER beta and ER alpha leading to PR loss and progesterone resistance in endometriosis. (cumhuriyet.edu.tr)
  • Mammary proliferation and estrogen sensitivity is higher in young female mice than in old or parous female mice, particularly during pubertal mammary gland development. (wikipedia.org)
  • ER-beta deficiency also leads to increase epithelial proliferation, decreased apoptosis, and accumulation of incompletely differentiated cells in mouse ventral prostrates (5). (acris-antibodies.com)
  • Estrogen receptor beta (ERβ) is expressed in the large intestine and seems to modulate colonic cell proliferation and apoptosis in a beneficial way regarding colon carcinogenesis [1] . (egms.de)
  • However, the activation of ER-beta led to an increase in cell proliferation and keratin-19 expression, as well as a decrease in galectin-1 expression. (uni-muenchen.de)
  • 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)
  • As sex steroids contribute to cell proliferation in various human tissues, we aimed at characterising the expression of steroid receptors in a broad cohort of probes from NET of the lungs and evaluated their possible prognostic impact. (omicsonline.org)
  • It is well known that sex steroid hormones play important roles in various human tissues contributing to cell proliferation through the interaction with intracellular receptors. (omicsonline.org)
  • In contrast to estrogen receptor alpha, which appears to be involved in cell survival and proliferation, the natural function of estrogen receptor beta seems to be that of a tumor suppressor. (ascopost.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)
  • 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)
  • Expression of estrogen receptor beta in prostate carcinoma cells inhibits invasion and proliferation and triggers apoptosis. (inserm.fr)
  • The two-pore domain potassium channel KCNK5: induction by estrogen receptor alpha and role in proliferation of breast cancer cells. (semanticscholar.org)
  • Estrogen receptor beta inhibits 17beta-estradiol-stimulated proliferation of the breast cancer cell line T47D. (semanticscholar.org)
  • 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 ability of various endoxifen concentrations to block estrogen-induced proliferation of MCF7 parental and ERβ-expressing cells was determined. (biomedcentral.com)
  • Additionally, low concentrations of endoxifen observed in tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher endoxifen concentrations are needed when ERβ is absent. (biomedcentral.com)
  • Tamoxifen, a selective estrogen receptor modulator (SERM), remains an important therapeutic agent in the treatment of women with endocrine sensitive breast cancer as it is known to effectively inhibit the proliferation-inducing effects of 17β-estradiol (estrogen) in ERα positive breast tumor cells. (biomedcentral.com)
  • Past studies from this laboratory support these clinical findings as we have demonstrated that endoxifen is the most potent tamoxifen metabolite responsible for inhibiting estrogen induced gene expression changes and proliferation rates in ERα positive breast cancer cells at clinically relevant concentrations [ 16 ]. (biomedcentral.com)
  • This manuscript summarizes recent data showing that estrogens and their receptors play an important role in modulating cholangiocyte proliferation. (uthscsa.edu)
  • Cholangiocyte proliferation, during BDL, is impaired by estrogen antagonists (tamoxifen, ICI 182,780) which furthermore, induce the overexpression of Fas antigen and activate apoptosis of proliferating cholangiocytes. (uthscsa.edu)
  • This indicates a major involvement of the ERK system in the estrogen modulation of cholangiocyte proliferation. (uthscsa.edu)
  • WAY-200070, the more brain-soluble of the two, also increased levels of the glutamate receptor GluR1 and postsynaptic density 95, two proteins important in synaptic activity. (alzforum.org)
  • Estrogen receptors (ERα and ERβ) are ligand activated nuclear receptor proteins that mediate the action of estradiol and structurally related compounds. (aacrjournals.org)
  • Binding of ligand activates ERs, by a mechanism that involves dissociation of heat shock proteins and dimerization of receptor proteins. (atlasgeneticsoncology.org)
  • However, these proteins antagonize the ability of estrogen receptor (ER) alpha to stimulate estrogen response element (ERE)-dependent transcriptional activity, potentially through the formation of a co-regulator complex. (inserm.fr)
  • Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. (abcam.com)
  • Isoform beta-3 is found in testis. (abcam.com)
  • Isoform beta-4 is expressed in testis, and at a lower level in spleen, thymus, ovary, mammary gland and uterus. (abcam.com)
  • Isoform 2 shows loss of ligand binding affinity and suppresses ER-alpha and ER-beta1 mediated transcriptional activation and may act as a dominant negative regulator of estrogen action. (uniprot.org)
  • Activating just the β isoform of the estrogen receptor (ERβ) is enough to improve learning and memory in mice, according to a paper published in the February 24 Nature Neuroscience. (alzforum.org)
  • Alternatively, activation of ERα (with E 2 , which is a ligand for both ERα and ERβ) may produce opposing effects on cognition and/or the activation of ERα and ERβ vs. either receptor isoform alone may produce a different pattern of effects. (pubmedcentralcanada.ca)
  • Recently, a new ER isoform, ER-beta (also known as ER-betal) was cloned from a rat prostatic cDNA library and is present in murine and human prostates. (allindianpatents.com)
  • 5p152 (Estrogen receptor 2 (ER beta), isoform CRA_a) is proteolytically cut by matrix metallopeptidase-26 (M10.029) cleavage. (burnham.org)
  • Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. (abcam.com)
  • Like all steroid hormones, estrogen readily diffuses across cell membrane and binds to and activates estrogen receptors (α and β) which then up-regulate the expression of many genes. (acris-antibodies.com)
  • 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)
  • Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. (biomedcentral.com)
  • Variants in estrogen-related genes and risk of Parkinson's disease. (uchicago.edu)
  • Estrogen Receptor alpha (ERα) and beta (ERβ) are the translated products of separate genes located on different chromosomes. (leicabiosystems.com)
  • Androgens in androgen-receptor (AR) positive SCLC cell lines have been shown to elicit proliferative effects that could be counteracted by anti-androgens like flutamide or cyproteroneacetate [ 8 , 9 ]. (omicsonline.org)
  • Prostate biopsy samples were taken at baseline and after 6 months and were analyzed for androgen receptor and estrogen receptor-beta expression. (isoflavones.info)
  • The researchers found that consumption of soy protein isolate and isoflavones for six months significant lowered expression of androgen receptor, but did not influence on estrogen receptor-beta expression or circulating hormones. (isoflavones.info)
  • Consumption of low-isoflavones soy protein isolate increased serum estradiol and the effect on the androgen receptor was intermediate to that of high isoflavones protein isolate and milk protein isolate, suggesting that very low levels of isoflavones, or other components in soy protein isolate, could have an effect on androgen receptor. (isoflavones.info)
  • Only men who consumed no soy protein isolate or isoflavones, but dairy milk protein isolate, showed a significant increase in androgen receptor from baseline. (isoflavones.info)
  • The study concluded that soy protein isolate consumption suppressed androgen receptor expression in the prostate and could be beneficial in preventing prostate cancer. (isoflavones.info)
  • Colonic Neoplasms and 26 others ) and proposed to participate in processes (behavioral fear response, brain development, epithelial cell maturation involved in prostate gland development, learning or memory, negative regulation of androgen receptor signaling pathway and 13 others ). (nrresource.org)
  • 4-OH-estradiol, tamoxifen, moxestrol for the ER beta protein. (nih.gov)
  • Tamoxifen, a synthetic anti-estrogen compound that is a mixed agonist/antagonist of estrogen receptor α (ERα) and a pure antagonist of ERβ, has moderate beneficial effects in human astrocytic neoplasms. (ovid.com)
  • 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). (biomedcentral.com)
  • Human ER beta was initially cloned and characterized from testis. (linscottsdirectory.com)
  • The human ER-beta is a newly discovered estrogen receptor initially cloned and characterized from testis. (genetex.com)
  • ER beta is found widely in many tissues throughout the body and can act as a potent tumor suppressor, playing a crucial role in many cancer types such as prostate cancer, autism spectrum disorder, medullary thyroid carcinoma, De Quervain Disease and risk of cardiovascular disease. (linscottsdirectory.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)
  • 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 receptor protein expression was evaluated by immunohistochemistry using the Allred Scoring System. (curehunter.com)
  • The binding affinities of genistein, dihydrogenistein and equol are comparable to the binding affinity of 17 beta-estradiol. (nih.gov)
  • The concentration required for maximal gene expression is much higher than expected from the binding affinities of the compounds, and the maximal activity induced by these compounds is about half the activity of 17 beta-estradiol. (nih.gov)
  • An alternative approach to reaping a neurologic benefit from estrogen signaling is to selectively target estrogen receptors, something estradiol itself doesn't do. (alzforum.org)
  • Upon binding to 17-β-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor α that interact with specific DNA sequences to activate transcription. (wikipedia.org)
  • Saturation ligand binding analysis of in vitro synthesized human ER alpha and rat ER beta protein revealed a single binding component for 16 alpha-iodo-17 beta-estradiol with high affinity [dissociation constant (Kd) = 0.1 nM for ER alpha protein and 0.4 nM for ER beta protein]. (nih.gov)
  • Although the cells bind estradiol (E2), transcriptional activation of a transfected estrogen-responsive reporter vector construct (ERE2-luc) by E2 was not observed. (nih.gov)
  • There are three major forms of estrogen, estradiol, estrone, and estriol, in which 17 β -estradiol has the highest affinity to estrogen receptors. (hindawi.com)
  • 17 β -Estradiol binds to estrogen receptor alpha (ER α ) and/or estrogen receptor beta (ER β ) in the cell's nucleus [ 10 ] and mediates long-term genomic effects (hours to days) in remodeling or lipid alteration. (hindawi.com)
  • Acute treatment with 17β-estradiol provides effective neuroprotection during the first days after acute brain injury, however, effects of chronic activation of estrogen receptor beta (ERβ) on recovery of function after experimental stroke have not been investigated. (lu.se)
  • 17 beta-estradiol is a neuromodulator capable of regulating several cellular processes including the activity of ion channels, in a rapid and non-genomic manner. (iisc.ac.in)
  • The G protein-coupled estrogen receptor (GPER) is known to facilitate rapid actions of 17 beta-estradiol, though its role in modulation of ion channels is not widely explored. (iisc.ac.in)
  • Several studies have shown both TREK1 and 17 beta-estradiol to be neuromodulatory but the interaction between them is not known. (iisc.ac.in)
  • In the present study, using single channel cell-attached patch clamp electrophysiology in HEK293 cells, we show that 17 beta-estradiol increases the activity of hTREK1 channel by acting through hGPER and increasing the channel opening probability within minutes. (iisc.ac.in)
  • The potentiation induced by 17 beta-estradiol is pertussis toxin sensitive involving action of G beta gamma), subunits while the inhibitory effect of cAMP-PKA pathway on TREK1 is reduced. (iisc.ac.in)
  • Protein phosphatases were also found to be important for the action of 17 beta-estradiol, which in concert with reduced activity of PKA, may alter the phosphorylation state of the channel and thus increase channel activity. (iisc.ac.in)
  • Mutational studies revealed the serines at positions 315 and 348 in the C-terminal domain of hTREK1 to be the target sites for dephosphorylation induced by 17 beta-estradiol action through hGPER. (iisc.ac.in)
  • Elucidation of the pathway for the potentiating action of 17 beta-estradiol via hGPER on hTREK1 channel activity will help us understand better one of the many possible neuroprotective mechanisms of 17 beta-estradiol and hTREK1 channel. (iisc.ac.in)
  • Estrogen receptor beta (ERβ) is one of the two key receptors (ERα, ERβ) that facilitate biological actions of 17β-estradiol (E2). (uthscsa.edu)
  • Benzophenone-3 (oxybenzone) and benzophenone-2 are structurally related to steroid receptor ligands and may act as endocrine disruptor. (greenmedinfo.com)
  • Our results provide insights into the folding/unfolding of ERα and ERβ and the conformational transitions of these receptors under the influence of ligands such as E 2 and the ERE. (aacrjournals.org)
  • ER alpha and ER beta have a high sequence homology and share affinity for the same ligands and DNA response elements. (atlasgeneticsoncology.org)
  • Estrogen receptor-{beta}-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice. (docphin.com)
  • Sareddy, GR & Vadlamudi, RK 2015, ' Cancer therapy using natural ligands that target estrogen receptor beta ', Chinese Journal of Natural Medicines , vol. 13, no. 11, pp. 801-807. (uthscsa.edu)
  • Interaction of phytoestrogens with estrogen receptors alpha and beta. (nih.gov)
  • 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)
  • 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 aglycones bind more strongly to hER beta than to hER alpha. (nih.gov)
  • Equol induces transcription most strongly with hER alpha and hER beta. (nih.gov)
  • Cellular signaling of estrogen is mediated through two estrogen receptors (ERs), ER alpha and ER beta. (atlasgeneticsoncology.org)
  • ER alpha and ER beta belong to the superfamily of nuclear receptors and specifically to the family of steroid receptors that act as ligand-regulated transcription factors. (atlasgeneticsoncology.org)
  • ER alpha and ER beta exhibit different affinities for some natural compounds, and distinct expression patterns in a variety of tissues. (atlasgeneticsoncology.org)
  • ER alpha and ER beta have different activities in certain ligand, cell-type, and promoter contexts. (atlasgeneticsoncology.org)
  • In the adult rodent ventral prostate, ER beta is expressed in the epithelial cells, whereas ER alpha is expressed in the stroma. (atlasgeneticsoncology.org)
  • The purpose of this study is to determine the effectiveness of adjuvant endocrine therapy for operable ER-beta positive, ER-alpha/PR negative , Her-2 negative breast cancer ( triple negative breast cancer , TNBC) patients. (clinicaltrials.gov)
  • Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. (nih.gov)
  • The rat estrogen receptor (ER) exists as two subtypes, ER alpha and ER beta, which differ in the C-terminal ligand binding domain and in the N-terminal transactivation domain. (nih.gov)
  • In 996, this receptor was renamed estrogen receptor alpha (ER-alpha) due to cloning of an additional estrogen receptor from rat prostrate. (acris-antibodies.com)
  • Estrogen receptor beta (ER beta) binds estrogens with an affinity similar to that of estrogen receptor alpha. (linscottsdirectory.com)
  • Some ER beta isoforms dominantly inhibit the activity of estrogen receptor alpha in reproductive tissues. (linscottsdirectory.com)
  • The size and structure of ER-beta is very similar to ER-alpha with the ligand and DNA binding domains being highly conserved, while the amino terminus which serves as their transactivation domain has diverged significantly. (genetex.com)
  • Similar in function to ER-alpha ER-beta binds to estrogen with a high affinity and regulates estrogen specific gene activation through direct interaction with estrogen response elements (ERE's). (genetex.com)
  • 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)
  • 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)
  • Prenylation inhibitors stimulate both estrogen receptor alpha transcriptional activity through AF-1 and AF-2 and estrogen receptor beta transcriptional activity. (inserm.fr)
  • Reproductive experience modifies the effects of estrogen receptor alpha activity on anxiety-like behavior and corticotropin releasing hormone mRNA expression. (semanticscholar.org)
  • Impact of estrogen receptor beta on gene networks regulated by estrogen receptor alpha in breast cancer cells. (semanticscholar.org)
  • Each year, nearly 1.3 million women are diagnosed with breast cancer worldwide and about two-thirds of these individuals are determined to have hormone sensitive tumors based on the expression of estrogen receptor-alpha (ERα). (biomedcentral.com)
  • estrogen receptor alpha (ERα) and beta (ERβ). (houstonmethodist.org)
  • 3-Beta, 17-beta-androstanediol is a major metabolite of dihydrotestosterdne (DHT), the 5-alpha-reduced active intracellular androgen in male accessory sex organs. (allindianpatents.com)
  • With the recent identification of ER-beta, and the recognition that ER-alpha and ER-beta have different biological roles, ER-selective modulators would similarly possess significant clinical utility. (allindianpatents.com)
  • Thus, ER-beta agonists will display different therapeutic profiles compared to ER-alpha antagonists or agonists, and would be preferentially beneficial in tissues relying on ER-beta signaling. (allindianpatents.com)
  • We previously identified a correlation between estrogen receptor alpha (ERalpha) and the candidate tumour suppressor gene Forkhead Box P1 (FOXP1), whose nuclear protein expression in breast tumours was associated with improved patient survival. (ox.ac.uk)
  • We speculate that alterations in the relative levels of ER beta and ER alpha in endometrial tissue dictate E2-regulated PR expression, such that a decreased ER alpha-ER beta ratio may result in suppression of PR. (cumhuriyet.edu.tr)
  • estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ), both of which are found in the prostate. (theurologyfoundation.org)
  • The prostate expresses both estrogen receptor alpha (ERA) and estrogen receptor beta (ERB). (ox.ac.uk)
  • Since most of the biological actions of E2 are mediated through the classical estrogen receptors alpha (ERα) and/or beta (ERβ), and both these receptors are present in the heart, we examined the role of ERα and ERβ in the rescue action of E2 against HF. (biomedcentral.com)
  • Isoflavone glycoside binds weakly to both receptors and estrogen receptor-dependent transcriptional expression is poor. (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)
  • Some isoforms dominantly inhibit the activity of other estrogen receptor family members. (wikipedia.org)
  • They also report that ERβ-selective compounds developed at Wyeth (WAY-200070 and WAY-202779) mimic the effect of estrogen on the hippocampus in ways that the ERα agonist PPT (4,4',4''-[4-propyl-(1H)-pyrazole-1,3,5-triyl]trisphenol) does not. (alzforum.org)
  • Fittingly, in rat wounds treated with the ER-beta agonist (DPN), epidermal regeneration was accelerated. (uni-muenchen.de)
  • 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 beta. (nrresource.org)
  • Multiple functional therapeutic effects of the estrogen receptor β agonist indazole-Cl in a mouse model of multiple sclerosis. (blogspot.com)
  • Here, the effects of the highly selective estrogen receptor (ER) β agonist indazole chloride (Ind-Cl) on functional remyelination in chronic experimental autoimmune encephalomyelitis (EAE) mice were investigated by assessing pathologic, functional, and behavioral consequences of both prophylactic and therapeutic (peak EAE) treatment with Ind-Cl. (blogspot.com)
  • The canonical model for ER-mediated regulation of gene expression involves the direct binding of dimeric ER to DNA sequences known as estrogen response elements (EREs), followed by recruitment of a variety of coregulators to alter chromatin structure and facilitate recruitment of the RNA polymerase II (Pol II) transcriptional machinery. (atlasgeneticsoncology.org)
  • ER beta seems to have a weaker corresponding AF-1 function and thus depends more on the AF-2 for its transcriptional activation function. (atlasgeneticsoncology.org)
  • ERβ is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. (wikipedia.org)
  • Estrogen Receptors (ER) are members of the steroid/thyroid hormone receptor superfamily of nuclear receptors. (linscottsdirectory.com)
  • Background: oncological research has been focused on evaluating estrogen receptors (ERs) in estrogen-related tumors and understanding the potential role of ERs in the pathophysiology of cancer. (biomedsearch.com)
  • Clinical data seem to implicate estrogen as a major player in ovarian cancer, with a large number of ovarian tumors expressing estrogen receptor beta. (ascopost.com)
  • Nearly 60% of the tumors showed a medium level of estrogen receptor beta 1 nuclear staining without cytoplasmic immunoreactivity. (ascopost.com)
  • In a correlation analysis with genome-wide expression data in a subcohort of 154 tumors, we found a strong negative correlation (Spearman R=-0.62) between beta-alanine and 4-aminobutyrate aminotransferase (ABAT). (diva-portal.org)
  • ERα is the highly characterized estrogen receptor cloned originally from a human breast cancer cell line with ERβ more recently identified in rodents and now in humans. (leicabiosystems.com)
  • This gene encodes a protein with sequence similarity to the estrogen receptor, a member of nuclear hormone receptor family of steroid hormone receptors. (wikipedia.org)
  • Recent studies have implicated the constitutive activity of estrogen receptor (ER) ß as an important regulator of metabolic diseases. (docphin.com)
  • To shed light on the prognostic role of estrogen receptor beta in ovarian cancer, the investigators examined the pattern of expression of the full-length estrogen receptor beta (estrogen receptor beta 1) and two estrogen receptor beta splice variant isoforms (estrogen receptor beta 2 and 5) in 56 patients with advanced serous ovarian cancer. (ascopost.com)
  • Although the investigators admitted that their cohort is small and the functional role of cytoplasmic estrogen receptor beta is far from clear, the prognostic role of estrogen receptor beta 2 in advanced serous ovarian cancer is promising. (ascopost.com)
  • Because phytoestrogens bind tightly to the estrogen receptor-beta, we conducted an epidemiologic investigation of synergistic effects between phytoestrogen intake and estrogen receptor-beta gene polymorphisms. (unboundmedicine.com)
  • Study of estrogen receptor-α and receptor-β gene polymorphisms on Alzheimer's disease. (cdc.gov)
  • Silymarin exhibits antiosteoporotic and selective estrogen receptor modulator activity in ovariectomized rats. (greenmedinfo.com)
  • Subtypes of estrogen receptors and their signaling mechanisms identified in HCVECs could be applicable for developing estrogen-like compounds to specifically bind to a subtype of estrogen receptors with greater specific action on the cerebral arteries, without the estrogen-dependent side effects on the reproductive organs, to prevent cerebral aneurysm formation in menopausal and postmenopausal woman. (hindawi.com)
  • 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)
  • The estrogen receptor (ER) is currently the only member of the steroid subfamily of nuclear receptors that has different subtypes. (allindianpatents.com)
  • We have recently demonstrated that rat cholangiocytes express both estrogen receptors (ER)-α and -β subtypes, while hepatocytes only express ER-α. (uthscsa.edu)
  • Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative approach to small molecules for the modulation of receptor signaling and subsequent gene expression. (rcsb.org)
  • Nuclear hormone receptor. (abcam.com)
  • Dandelion extract up-regulates reproductive hormone receptor expression in mice. (greenmedinfo.com)
  • Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor-a nuclear receptor which is activated by the sex hormone estrogen. (wikipedia.org)
  • Estrogen, a steroid hormone, is a key regulator of growth and differentiation in a broad range of target tissues and, it is also implicated in breast and endometrial cancer and osteoporosis (1). (acris-antibodies.com)
  • 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. (linscottsdirectory.com)
  • 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)
  • Consumption of soy products have been linked with lower prostate cancer risk and may act through altering hormones or hormone receptor signalling. (isoflavones.info)
  • 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 receptor beta (ERβ) is a ligand inducible transcription factor regulating gene expression in response to the female sex hormone estrogen. (omicsdi.org)
  • Estrogen (the 'female' hormone) has been shown to be important in PC development. (theurologyfoundation.org)
  • The compounds of the present invention are useful as Estrogen Receptor beta agonists. (allindianpatents.com)
  • such agonists are useful for the treating estrogen receptor beta mediated diseases such as prostate cancer. (allindianpatents.com)
  • Estrogen-modulated gene transcription is exerted via different mechanisms: the genomic and the nongenomic pathways. (atlasgeneticsoncology.org)
  • AP-1 and NF-kappaB are known to cause transrepression of both ERalpha- and glucocorticoid receptor-mediated transcription. (nih.gov)
  • 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)
  • The two estrogen receptors belong to a family of ligand-regulated transcription factors. (biomedcentral.com)
  • Expression of the forkhead transcription factor FOXP1 is associated with that of estrogen receptor-beta in primary invasive breast carcinomas. (ox.ac.uk)
  • Junn Yanagisawa (Tsukuba university): Turning off estrogen receptor beta-mediated transcription requires estrogen-dependent receptor proteolysis. (blogspot.com)
  • A failure of endothelial cells in the cerebral arterial wall to adequately express estrogen receptors abrogates the possibility of direct interaction between estrogen receptors and circulating estrogen, which can trigger inflammation, upregulation of proteolytic pathways, loss of the arterial wall matrix, and degradation of the arterial wall [ 5 , 6 ]. (hindawi.com)
  • To this regard, previous studies showed that a majority of non-small cell lung cancer (NSCLC) express estrogen receptors (ERs) [ 1 - 3 ] and that their growth can be stimulated by estrogen in nude mouse xenografts [ 4 ]. (omicsonline.org)
  • Estrogen Receptor beta (ER beta, NR3A2) protein is approximately 55kD, though multiple isoforms ranging from 36-59kD have been described. (linscottsdirectory.com)
  • 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)
  • Sequence variants of estrogen receptor beta and risk of prostate cancer in the National Cancer Institute Breast and Prostate Cancer Cohort Consortium. (diva-portal.org)
  • A synthetic peptide corresponding to a sequence at the N-terminus of human Estrogen Receptor beta(27-50aa HGSIYIPSSYVDSHHEYPAMTFYS), different from the related rat and mouse sequences by four amino acids. (bosterbio.com)
  • It is well-known for more than a decade that breast cancer exhibits distinct gene expression patterns depending on the molecular subtype defined by estrogen receptor (ER) and HER2 status. (diva-portal.org)
  • 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 conducted to identify altered cellular processes. (biomedcentral.com)
  • We found a significant multiplicative interaction (P = 0.04) between dietary intake of phytoestrogens and a promoter SNP in the estrogen receptor-beta gene (rs 2987983-13950), but not with any of the three other htSNPs (P = 0.11, 0.69, 0.85). (unboundmedicine.com)
  • 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)
  • After identification of human estrogen receptor (ER) β gene and its first transcript, several splice variants of this mRNA have been identified. (egms.de)
  • As no biopsy specimens are possibly obtained during surgery because of high risk of bleeding, there is an increasing interest to develop a cellular model to directly investigate the effect of estrogen deficiency and whether it causes a decline in the function and/or number of estrogen receptors, which may promote inflammation and apoptosis in the endothelial cells of cerebral arterial walls. (hindawi.com)
  • Transactivation was also not observed with cotransfected ERalpha or beta. (nih.gov)
  • Estrogen receptor (ER) beta is the predominant ER in granulosa cells of the ovary. (nih.gov)
  • The ER-beta positive TNBC patients who had undergone modified radical mastectomy or breast- conserving surgery were randomly (1:1) enrolled to receive toremifene (60 mg per day for premenopausal and perimenopausal patients) /anastrozole(1mg per day for postmenopausal patients) or observation within 4 weeks after adjuvant chemotherapy and/or radiation therapy if necessary.The follow-up time will be at least five years. (clinicaltrials.gov)
  • Thus, 204 estrogen receptor positive (ER+) and 67 estrogen receptor negative (ER-) breast cancer tissues were investigated using GC-TOFMS based metabolomics. (diva-portal.org)
  • Beta-alanine demonstrated the strongest change between ER- and ER+ breast cancer (fold change=2.4, p=1.5E-20). (diva-portal.org)
  • Estrogen receptor beta inhibits angiogenesis and growth of T47D breast cancer xenografts. (semanticscholar.org)
  • Estrogen receptor-beta is a potential target for triple negative breast cancer treatment. (escholarship.org)
  • Purpose: Significant controversy exists regarding the expression patterns of estrogen receptor beta (ERβ) in normal and diseased breast tissue. (elsevier.com)
  • Estrogen receptors (ERs) are commonly considered as important markers for breast cancer. (waocp.org)
  • Breast cancers (BC) in women carrying mutations in BRCA1 gene are more frequently estrogen receptor negative than the nonhereditary BC. (biomedcentral.com)
  • The identification of the second human estrogen receptor, ERβ, raised a question of its role in hereditary breast cancer. (biomedcentral.com)
  • We used deep sequencinge technology to profile the transcriptome, gene copy number, and CpG island methylation status simultaneously in eight commonly used breast cell lines to develop a model for how these genomic features are integrated in estrogen receptor positive (ER+) and negative breast cancer. (omicsdi.org)
  • Haplotypes of the estrogen receptor beta gene and breast cancer risk. (ox.ac.uk)
  • Targeted disruption of ER beta in mice has suggested roles for ER beta in many tissues and organs, including the ovary, uterus, mammary gland, brain, immune system and ventral prostate. (atlasgeneticsoncology.org)
  • The localization of the estrogen receptor beta (ERβ) in human normal and cancer tissues was studied in paper IV. (diva-portal.org)
  • Estrogen receptor β (ERβ) is the second identified receptor mediating the effects of estrogen on target tissues. (ovid.com)
  • It also can bind to G-protein coupled estrogen receptor (GPER) [ 11 ] and mediates nongenomic action that is rapid in onset and short in duration such as changes in vasomotor tones through kinase activation and intracellular signaling pathway [ 12 ]. (hindawi.com)
  • As such, studies were conducted to begin to address the role of actions at the β form of the intracellular estrogen receptor (ERβ) for E 2 's cognitive effects in adult female mice. (pubmedcentralcanada.ca)
  • Estrogens play important roles in the development and homeostasis of the reproductive, central nervous, skeletal, and cardiovascular systems of both males and females. (allindianpatents.com)
  • Esrrβ is a nuclear receptor associated with cell survival in low-oxygen environments, pluripotency in embryonic stem cells, regulation of energy metabolism, and oxidative stress. (arvojournals.org)
  • The aim of this study was to analyze the expression of estrogen receptor (ER) beta in endometrioid carcinoma in comparison to non-neoplastic endometrium. (curehunter.com)
  • This study is reportedly the first to analyze the subcellular expression of estrogen receptor beta isoforms in advanced serous ovarian cancers. (ascopost.com)
  • Anomalies in the cytoplasmic expression of estrogen receptor beta 2 appear to be associated with poorer outcomes in patients with advanced serous ovarian cancer, according to the results of a study reported by Ciucci et al in Gynecologic Oncology . (ascopost.com)
  • Immunocytochemical staining of ER beta in cells overexpressing the Human protein results in nuclear staining. (abcam.com)
  • Genomic organization of human ER beta gene, protein and functional domains. (atlasgeneticsoncology.org)
  • Hi, if you look at this paper, they profiled all 49 nuclear receptor expressions in 51 human cancer cell lines. (protocol-online.org)
  • Little is known about estrogen receptors and their signaling mechanisms in human cerebral vascular endothelial cells, which is important for understanding cerebral aneurysm pathogenesis in menopausal and postmenopausal women. (hindawi.com)
  • Estrogen receptor beta (ER β ) and G-protein-coupled receptor 1 (GPER1) were immunocytochemically identified in human cerebral vascular endothelial cells (HCVECs). (hindawi.com)
  • Staining of formalin fixed, paraffin embedded Human Placenta with Mouseanti Human estrogen Receptor (Cat. (acris-antibodies.com)
  • Staining of formalin fixed, paraffin embedded Human Placenta with Mouse anti Human estrogen Receptor (Cat. (acris-antibodies.com)
  • Amino acids 1-153 of human ER-beta expressed in E. coli. (genetex.com)
  • 14C8 is specific for human ER-beta. (abcam.co.jp)
  • Estrogen has been shown to be important in prostate carcinogenesis, with evidence resulting from epidemiological, cancer cell line, human tissue and animal studies. (ox.ac.uk)
  • This receptor was regarded as the only ER that mediates estrogenic effects, until a second ER, now known as ER beta, was cloned from rat prostate. (atlasgeneticsoncology.org)
  • Estrogens can have profound effects on prostate growth and differentiation as well as in the pathogenesis of prostate cancer. (atlasgeneticsoncology.org)
  • Interactions between phytoestrogen intake and estrogen receptor-beta SNPs on prostate cancer risk were evaluated considering both multiplicative and additive effect scales. (unboundmedicine.com)
  • Our study provides strong evidence that high intake of phytoestrogens substantially reduce prostate cancer risk among men with specific polymorphic variation in the promoter region of the estrogen receptor-beta gene. (unboundmedicine.com)
  • 1999 ) Estrogen receptor expression in prostate cancer and premalignant prostatic lesions. (biologists.org)
  • Estrogen receptor beta in prostate cancer: friend or foe? (ox.ac.uk)
  • Most evidence suggests that ERA mediates the harmful effects of estrogen in the prostate, whereas ERB is tumour suppressive, but trials of ERB-selective agents have not translated into improved clinical outcomes. (ox.ac.uk)
  • It is well known that estrogens regulate cell cycle progression, but the specific contributions and mechanisms of action of the estrogen receptor beta (ER β ) remain elusive. (hindawi.com)