• A dual cell-line GFP expression system was constructed to study EDs with activities as estrogen receptor agonists or antagonists. (cornell.edu)
  • The term hormone therapy is used to encompass estrogen therapy (ET) and estrogen-progestogen therapy (EPT) when outcomes are not specific to one or the other treatment, although whenever possible the different effects of ET, EPT, and estrogen-receptor (ER) agonists or antagonists are included. (medscape.com)
  • They act as complete or partial agonist or as antagonist. (harvard.edu)
  • Both estrogen receptors could interact with estrogen-mimicking compounds such as the fluorescent phytoestrogen coumestrol, which acts both in an agonist or antagonist fashion. (nel.edu)
  • For example, the ligand tamoxifen, a commonly used breast cancer pharmaceutical, exhibits an ER antagonist response in the breast and an ER agonist response in the bone. (umsystem.edu)
  • Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ and the vitamin D receptor. (nature.com)
  • Moreover, because testosterone (T) can be aromatized into estrogen in the hypothalamus ( Lephart, 1996 ) and because the androgen receptor is not expressed in MNCs, it is conceivable that effects of T could also be mediated through ER-β. (jneurosci.org)
  • The purpose of this study was to determine the ontogeny of cellular changes in the expression of estrogen receptors (ERα, ERβ), G protein-coupled estrogen receptor 1 (GPER1), and progesterone receptors (PRs) in endometriosis using a mouse model. (springer.com)
  • Estrogen receptor-β, estrogen receptor-α, and progesterone resistance in endometriosis. (springer.com)
  • Progesterone receptor modulators for endometriosis. (springer.com)
  • These are common symptoms related to shifts in estrogen and progesterone and the balance between these two hormones. (terrywahls.com)
  • High levels of estrogen and possibly progesterone (female hormones) seem to stimulate their growth. (msdmanuals.com)
  • No endogenous ligands of ERRα have been identified to date, hence ERRα is classified as an orphan receptor. (wikipedia.org)
  • Ligands agonist ERβ have the potential activity to inhibit the proliferation of glioma cells and the discovery of this ligand has opened new therapy through the ERβ to prolong survival in cancer patients. (chemoprev.org)
  • Paterni I, Granchi C, Katzenellenbogen JA, Minutolo F. Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential. (springer.com)
  • From the screen, we identified a family of ERbeta-selective agonists whose members contain bulky oxabicyclic scaffolds in place of the planar scaffolds common to most ER ligands. (rcsb.org)
  • To provide insight into the molecular mechanisms of their activity and selectivity, we determined the crystal structures of the ERalpha ligand-binding domain (LBD) and a peptide from the glucocorticoid receptor-interacting protein 1 (GRIP1) coactivator complexed with the ligands OBCP-3M, OBCP-2M, and OBCP-1M. (rcsb.org)
  • this is an exogenous agent that interferes in the production, liberation, transport, metabolism, the union to a receptor or a modifier of the action or elimination of natural ligands responsible for maintaining homeostasis and the regulation and development of the organism. (ivis.org)
  • Estrogens are well recognized as important hormones in male reproduction and act as ligands to alpha and beta estrogen receptors. (nel.edu)
  • Estrogen-related receptor alpha (ERRα), also known as NR3B1 (nuclear receptor subfamily 3, group B, member 1), is a nuclear receptor that in humans is encoded by the ESRRA (Estrogen Related Receptor Alpha) gene. (wikipedia.org)
  • Currently, ERRα is considered an orphan nuclear receptor. (wikipedia.org)
  • The protein encoded by this gene is a nuclear receptor that is closely related to the estrogen receptor. (wikipedia.org)
  • ERRα has been suggested to act as a transcriptional activator of CYP11B1 and CYP11B2, which indicates that this nuclear receptor may be required for the production of cortisol and aldosterone in the adrenal gland. (wikipedia.org)
  • ERRα is related to mitochondrial function but studies involving ERRα knockout mice suggested that this receptor, while dispensable for basal cellular function, is definitely necessary to provide the levels of energy necessary to respond to physiological and pathological insults in diverse tissues, the lack of that nuclear receptor leading to impaired fat metabolism and absorption. (wikipedia.org)
  • Estrogen-related receptor α (ERRα) belongs to a nuclear receptor superfamily characterized by their high levels of sequence identity to estrogen receptors, and the primary role of ERRα is in energy metabolism ( 9 ). (spandidos-publications.com)
  • Expression and estrogen sensitivity of target genes and nuclear receptor coregulators were altered at mRNA and protein levels in adult uterus, prostate and brain. (researchgate.net)
  • A direct effect on steroid receptor sites in breast tissue is also possible. (drugbank.com)
  • Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. (nature.com)
  • Phytoestrogens, plant-based compounds that also stimulate estrogen receptors, can ease problems associated with estrogen dominance as well as improve symptoms associated with perimenopause and menopause. (terrywahls.com)
  • These same compounds can provide estrogen support for perimenopausal and menopausal women, stimulating estrogen receptors and gently reducing symptoms, stabilizing mood, protecting brain tissues, and improving bone mineralization. (terrywahls.com)
  • These exogenous estrogen-mimicking compounds have been termed xenoestrogens. (umsystem.edu)
  • The isoflavone phytoestrogens genistein and daidzein are non-selective ERR agonists, while XCT790 has been identified as a potent and selective inverse agonist of ERRα. (wikipedia.org)
  • AC 186 is a potent and selective ER β agonist (EC 50 values are 6 and 5000 nM for ER β and ER α respectively). (tocris.com)
  • It was approved by the U.S. Food and Drug Administration (FDA) as the first drug to specifically treat endometriosis, but its role as a treatment for endometriosis has been largely replaced by the gonadotropin-releasing hormone (GnRH) agonists. (drugbank.com)
  • BACKGROUND: LY01005 (Goserelin acetate sustained-release microsphere injection) is a modified gonadotropin-releasing hormone (GnRH) agonist injected monthly. (bvsalud.org)
  • This protein acts as a site-specific (consensus TNAAGGTCA) transcription regulator and has been also shown to interact with estrogen and the transcription factor TFIIB by direct protein-protein contact. (wikipedia.org)
  • The binding and regulatory activities of this protein have been demonstrated in the regulation of a variety of genes including lactoferrin, osteopontin, medium-chain acyl coenzyme A dehydrogenase (MCAD) and thyroid hormone receptor genes. (wikipedia.org)
  • Kolkova Z, Noskova V, Ehinger A, Hansson S, Casslén B. G protein-coupled estrogen receptor 1 (GPER, GPR 30) in normal human endometrium and early pregnancy decidua. (springer.com)
  • Expression of the G protein-coupled estrogen receptor (GPER) in endometriosis: a tissue microarray study. (springer.com)
  • In this work, in vitro systems, including stable cells lines with estrogen induced green fluorescence protein (GFP) expression and micro cell culture analog (microCCA) devices, were developed to study EDs. (cornell.edu)
  • Immunocytochemistry demonstrated that the decrease in ER-β mRNA was translated into depletion of receptor protein content in hyper-osmotic animals. (jneurosci.org)
  • RT‑qPCR and western blotting results showed that treatment with 30 mM glucose for 12, 24 and 48 h increased the expression level of estrogen‑related receptor α (ERRα) mRNA and protein. (spandidos-publications.com)
  • TCDD for every step of the mechanism described for 2,3,7,8-TCDD carcinogenesis in humans including receptor binding, gene expression, protein activity changes, cellular replication, oxidative stress, promotion in initiation-promotion studies and complete carcinogenesis in laboratory animals. (who.int)
  • Estrogen biosynthesis and its regulation in endometriosis. (springer.com)
  • Estrone is only a weak agonist of estrogen receptor but it serves as a precursor for biosynthesis of 17β-estradiol, 16α-hydroxyestrone and catechol estrogens. (helsinki.fi)
  • Matsuzaki S, Murakami T, Uehara S, Canis M, Sasano H, Okamura K. Expression of estrogen receptor alpha and beta in peritoneal and ovarian endometriosis. (springer.com)
  • Danazol also depresses the preovulatory surge in output of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), thereby reducing ovarian estrogen production. (drugbank.com)
  • In fibrocystic breast disease, the exact mechanism of action of danazol is unknown, but may be related to suppressed estrogenic stimulation as a result of decreased ovarian production of estrogen. (drugbank.com)
  • Estrogen receptors alpha (ERalpha) and beta (ERbeta) have distinct functions and differential expression in certain tissues. (rcsb.org)
  • Following the treatment used to control local disease, adjuvant endocrine therapy with tamoxifen alone is given to reduce the rate of recurrence and improve survival in postmenopausal patients with lymph node involvement and positive hormone receptors. (pharmacology2000.com)
  • Tamoxifen is non-steroidal anti-estrogen drugs. (lookchem.com)
  • However, Tamoxifen Z isomer enters into the cell, competitively binding with ER to form receptor complexes, inhibiting that estrogen plays an role, and inhibiting proliferation of breast cancer cells. (lookchem.com)
  • In investigating the role of estrogen receptors and estrogen in SLE and other autoimmune diseases, our team has identified novel targets of estrogen that are significantly up-regulated in SLE patients and play a critical role in regulating inflammation. (osu.edu)
  • Assessing indoor dust interference with human nuclear hormone receptors in cell-based luciferase reporter assays. (cdc.gov)
  • We propose that the variable outcomes in hormonal therapy for endometriosis could be possibly due to heterogeneity in the expression of steroid hormone receptors in the ectopic endometrium. (springer.com)
  • ERRs are similar to estrogen receptors in structure, but they are not estrogen receptors and have a very different function in that they regulate cellular energetics in tissues with high requirements for energy production (skeletal muscle, heart, brain)," he explained. (medicalnewstoday.com)
  • Its structure is similar to estrogen, existing Z type and O type isomers. (lookchem.com)
  • Thus, estrogen receptor activators can be expected to lead to the modulation of cell metabolism in estrogen receptor positive cells. (canada.ca)
  • Estrogen receptor (ER) activity has a profound effect on breast cancer cell growth through a number of metabolic changes driven by its effect on transcription of several enzymes, including carbonic anhydrases, Stearoyl-CoA desaturase-1, and oncogenes including HER2. (canada.ca)
  • ERR agonists represent a potential new class of drugs that could be used to treat metabolic diseases such as type 2 diabetes and obesity, as well as muscle weakness in the elderly. (medicalnewstoday.com)
  • Dr. Cameron Heinz , an attendant care provider, who was not involved in this study, noted that "the research exploring the use of a synthetic ERR agonist to alleviate metabolic syndrome is highly promising. (medicalnewstoday.com)
  • If this synthetic agonist proves effective in alleviating metabolic syndrome, it could offer a new avenue for treating this widespread health problem," Dr. Heinz explained. (medicalnewstoday.com)
  • UDP-glucuronosyltransferases (UGTs) are phase II metabolic enzymes that conjugate estrogens with glucuronic acid to render them more watersoluble. (helsinki.fi)
  • Hypoimmune anti-CD19 chimeric antigen receptor T cells provide lasting tumor control in fully immunocompetent allogeneic humanized mice. (ucsf.edu)
  • If the estrogen receptor (ER) is present in breast cancer cells, estrogen enters into tumor cells and binds with ER, promoting mRNA and DNA synthesis of tumor cells, stimulating tumor cell growth. (lookchem.com)
  • Chemicals found in the environment have been found to behave like the body's natural estrogen, estradiol. (umsystem.edu)
  • Both estradiol and xenoestrogens can bind two estrogen receptors (ERs), ER alpha and ER beta, to elicit biological responses. (umsystem.edu)
  • While estradiol binds both receptors equally, some xenoestrogens have been shown to bind ER beta preferentially. (umsystem.edu)
  • Estrogen receptor β modulates apoptosis complexes and the inflammasome to drive the pathogenesis of endometriosis. (springer.com)
  • To investigate the presence of Coumestrol-Estrogen Receptor complexes by fluorescence in testis and epididymis, its effect in the ER expression by immunostain in the same tissues and the effect of this binding in the testis histological characteristics. (nel.edu)
  • Stabilization of MORC2 by estrogen and antiestrogens through GPER1- PRKACA-CMA pathway contributes to estrogen-induced proliferation and endocrine resistance of breast cancer cells. (harvard.edu)
  • SHON is a novel estrogen-regulated oncogene in mammary carcinoma that predicts patient response to endocrine therapy. (harvard.edu)
  • With regard to estetrol, it is by definition an oestrogen receptor agonist and therefore also considered an endocrine active substance. (janusinfo.se)
  • An agonist is something that activates or turns on a receptor when it binds to it. (medicalnewstoday.com)
  • This dual ligand quality characterizes what is now known as a selective estrogen receptor modulator (SERM). (umsystem.edu)
  • Clinically it is mainly used for high levels of estrogen in breast cancer patients, which combines with androgen and other anticancer drugs (such as doxorubicin, etc., enhancing the effectiveness and showing good effect in postmenopausal patients with advanced breast cancer. (lookchem.com)
  • ERRα was originally cloned by DNA sequence homology to the estrogen receptor alpha (ERα, NR3A1), but subsequent ligand binding and reporter-gene transfection experiments demonstrated that estrogens did not regulate ERRα. (wikipedia.org)
  • Cholesterol has recently been found to bind to and activate the ERRα, and may be the endogenous ligand for the receptor. (wikipedia.org)
  • An ERR is a type of receptor that closely resembles receptors that bind estrogen, but has no known ligand (binding partner) in the body. (medicalnewstoday.com)
  • The receptors are ligand inducible transcription factors that exhibit unique biological actions. (umsystem.edu)
  • Estrogen Receptor Modulators" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
  • This graph shows the total number of publications written about "Estrogen Receptor Modulators" by people in Harvard Catalyst Profiles by year, and whether "Estrogen Receptor Modulators" was a major or minor topic of these publication. (harvard.edu)
  • Below are the most recent publications written about "Estrogen Receptor Modulators" by people in Profiles. (harvard.edu)
  • Estrogens are female sex hormones that have genotoxic and proliferation-enhancing effects in cells. (helsinki.fi)
  • 2 Black cohosh may be exerting its beneficial effects through selective estrogen receptor modulation, serotonin pathways, antioxidant effects, and anti-inflammation effects. (terrywahls.com)
  • However, the effect of rapid signaling via ERβ on dendritic spines and the signaling pathways initiated by this receptor in cortical neurons are unknown. (jneurosci.org)
  • The pleiotropic harmful effects of EDCs act through hormone-dependent downstream signaling pathways responsible for gonad development either through direct interaction with steroid hormone receptor or via epigenetic regulation. (intechopen.com)
  • Direct regulators of nuclear-encoded mitochondrial genes are members of the estrogen-related receptor (ERR) family, encoded by Esrra , Esrrb and Esrrg . (nature.com)
  • These agonists are 10-50-fold selective for ERbeta in competitive binding assays and up to 60-fold selective in transactivation assays. (rcsb.org)
  • Women who smoke have lower levels of estrogen compared to nonsmokers, and they often go through menopause earlier. (daviddarling.info)
  • Estrogen receptor alpha (ERα) and estrogen-related receptor alpha (ERRα) have been found to regulate many of the same genes. (wikipedia.org)
  • Previous analyses of dopaminergic (DAergic) neurons from patients with Lewy-body pathology revealed a deficiency in nuclear-encoded genes for mitochondrial respiration, many of which are targets for the transcription factor estrogen-related receptor gamma ( Esrrg /ERRγ). (nature.com)
  • in fact, these genes are targets of the transcriptional coactivator and master regulator of transcription of mitochondrial genes peroxisome proliferator-activated receptor gamma coactivator-1 alpha (PGC-1α) 12 . (nature.com)
  • A fluorescence resonance energy transfer-based assay was used to screen a 10,000-compound chemical library for ER agonists. (rcsb.org)
  • Fluorescence and inmunohistological detection of estrogen receptors in dog testis and epidydimis after oral coumestrol administration. (nel.edu)
  • Serrano H, Perez-Rivero J, Martinez-Maya J, Aguilar-Setien A, Perez-Martinez M, Garcia-Suarez M. Fluorescence and inmunohistological detection of estrogen receptors in dog testis and epidydimis after oral coumestrol administration. (nel.edu)
  • Phytoestrogens may reduce symptoms from excessive estrogen dominance in young women with painful periods, heavy bleeding, and mood instability. (terrywahls.com)
  • While 16α-hydroxyestrone has relatively weak affinity for estrogen receptor, it has prolonged effect due to covalent binding to the receptor. (helsinki.fi)
  • Because of the eminent role of receptors for mediating the biological effects of steroid hormones, changes in receptor expression could alter responsiveness of the target cells and determine the physiological circumstances in which gonadal steroids become important regulators of cell function. (jneurosci.org)
  • 10-12 In rats that had their ovaries removed, chasteberry improved memory and cognitive performance via stimulation of estrogen receptors. (terrywahls.com)
  • Generally, subfamily UGT1A enzymes conjugate the 3-hydroxyls of estrogens, while the activity of subfamily UGT2B is directed towards 16- and 17-hydroxyls. (helsinki.fi)
  • The vasopressin (VP) magnocellular neurosecretory cells (MNCs) in the supraoptic and paraventricular (PVN) nuclei are regulated by estrogen and exhibit robust expression of estrogen receptor (ER)-β. (jneurosci.org)
  • A study has demonstrated that activation of the peroxisome proliferator-activated receptor g coactivator 1-α (PGC-1α)/ERRα pathway increases VEGF expression and angiogenesis in endothelial cells, which suggests that ERRα may be involved in the pathogenesis of DR ( 10 ). (spandidos-publications.com)
  • The two stable cell lines, Ishikawa-GFP (uterine origin) and MCF7-GFP (breast origin), displayed increased intracellular GFP intensity with estrogens. (cornell.edu)
  • The farnesoid X receptor (FXR) regulates the homeostasis of bile acids, lipids and glucose. (nature.com)
  • Members of this family show sequence homology with estrogen receptors but are incapable of being bound by estrogen. (nature.com)
  • Brain-synthesized estrogen has been shown to influence synaptic structure, function, and cognitive processes. (jneurosci.org)
  • Research suggests that glabridin, an isoflavone in licorice, is an estrogen-receptor agonist and supports normal breast cell growth. (terrywahls.com)
  • Detection of estrogens was demonstrated on a microCCA device integrated with the micropump. (cornell.edu)