• 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)
  • This protein is a member of nuclear hormone receptor family of steroid hormone receptors. (wikipedia.org)
  • For cells, cell lines and tissues in culture till half confluency.The receptors are ligand binding factors of type 1, 2 or 3 and protein-molecules that receive chemical-signals from outside a cell. (hla-a.com)
  • In this sense, am olfactory receptor is a protein-molecule that recognizes and responds to endogenous-chemical signals, chemokinesor cytokines e.g. an acetylcholine-receptor recognizes and responds to its endogenous-ligand, acetylcholine. (hla-a.com)
  • 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)
  • Immunocytochemistry demonstrated that the decrease in ER-β mRNA was translated into depletion of receptor protein content in hyper-osmotic animals. (jneurosci.org)
  • Breast cancer cells are sensitized by piperine to radiotherapy through estrogen receptor-α mediated modulation of a key NHEJ repair protein- DNA-PK. (bvsalud.org)
  • The protein encoded by this gene can bind to a functionally important site in the T-cell receptor-alpha enhancer, thereby conferring maximal enhancer activity. (cancer-genetics.org)
  • 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)
  • It can also protect it from deactivation from the selective estrogen receptor modulator 4-hydroxytamoxifen. (wikipedia.org)
  • Pharmacologic therapy for osteoporosis includes most commonly the use of antiresorptive agents to decrease bone resorption, such as bisphosphonates, denosumab, and the selective estrogen-receptor modulator (SERM) raloxifene. (medscape.com)
  • Estrogen-related receptor gamma (ERR-gamma), also known as NR3B3 (nuclear receptor subfamily 3, group B, member 3), is a nuclear receptor that in humans is encoded by the ESRRG (EStrogen Related Receptor Gamma) gene. (wikipedia.org)
  • No physiological activating ligand is known for this orphan receptor, but 4-hydroxytamoxifen and diethylstilbestrol act as inverse agonists and deactivate ESRRG. (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)
  • Direct regulators of nuclear-encoded mitochondrial genes are members of the estrogen-related receptor (ERR) family, encoded by Esrra , Esrrb and Esrrg . (nature.com)
  • 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)
  • Estrogen act through binding to Estrogen Receptor α (ERα) which is a member of the nuclear receptor superfamily of ligand activated transcription factors. (qscience.com)
  • In addition, piperine shares common pharmacophore features with most of the known estrogen agonists and antagonists. (bvsalud.org)
  • 2009). Molecular Characterization of Novel and Selective Peroxisome Proliferator-Activated Receptor {alpha} Agonists with Robust Hypolipidemic Activity in Vivo. (columbiabiosciences.com)
  • Title: Efficient discovery of selective small molecule agonists of estrogen-related receptor gamma using combinatorial approach. (aablocks.com)
  • X-ray crystal structures of the ligand binding domain (LBD) of the estrogen-related receptor-gamma (ERRgamma) were determined that describe this receptor in three distinct states: unliganded, inverse agonist bound, and agonist bound. (rcsb.org)
  • Title: X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation. (aablocks.com)
  • The mechanisms that silence the estrogen receptor gene alpha, in certain breast cancer cell lines may be closer to being unlocked, according to a new study. (sciencedaily.com)
  • The researcher says this study provides a basis for understanding how the complex pattern of estrogen receptor gene alpha methylation and transcriptional silencing is generated, as well as for understanding the relationship between this pattern and its function during breast cancer progression. (sciencedaily.com)
  • The mechanisms that silence the estrogen receptor gene alpha (ER-α) in certain breast cancer cell lines may be closer to being unlocked, according to a study by researchers at Temple University's Sbarro Institute for Cancer Research and Molecular Medicine. (sciencedaily.com)
  • In a previous study, the researchers found that in estrogen receptor-positive and estrogen receptor-negative mammary cell lines of women who have been affected with breast cancer, the tumor-suppressing gene pRb2/p130 binds to a specific region of the estrogen receptor gene alpha and forms molecular complexes recruiting and/or interacting with several proteins. (sciencedaily.com)
  • In the current study, lead by Antonio Giordano, M.D., Ph.D., director of the Sbarro Institute, the researchers showed that the presence of specific pRb2/p130 multimolecular complexes bound to the estrogen receptor gene strongly correlates with the methylation (chemical modification) of the gene. (sciencedaily.com)
  • Our hypothesis is that the sequence of epigenetic events for establishing and maintaining the silenced state of the estrogen receptor gene alpha during the breast cancer progression is mediated by pRb2/p130 in association with specific proteins that modified the DNA structure through specific mechanisms," said Giordano, who discovered the Rb2 gene while working at Temple's Fels Cancer Institute in the early 1990s. (sciencedaily.com)
  • In other words, the presence of a specific pRb2/p130 multimolecular complex may dictate a local change of the DNA structure of the estrogen receptor alpha gene and influence its susceptibility to chemical modification (DNA methylation), as well as to different epigenetic alterations leading to estrogen receptor alpha silencing," added Marcella Macaluso, research assistant professor at the Sbarro Institute and the study's lead author. (sciencedaily.com)
  • Title: An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. (aablocks.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)
  • Title: Identification of pyrido[1,2-α]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor α. (aablocks.com)
  • They discovered that in estrogen receptor-negative cells - which are able to silence the expression of the estrogen receptor - pRb2/p130 forms a specific molecular complex recruiting a different sequence of proteins than in the estrogen receptor-positive cells. (sciencedaily.com)
  • The researchers reported their findings, "Epigenetic Modulation of Estrogen Receptor-α by pRb Family Proteins: A Novel Mechanism in Breast Cancer," in the Aug. 15 issue of the journal Cancer Research (abstract 67/16/7731). (sciencedaily.com)
  • It altered the estrogen receptor α/ß ratio and the expression of estrogen -responsive proteins of DDR and NHEJ pathway. (bvsalud.org)
  • In conclusion, our study for the first time reported that piperine sensitizes breast cancer cells to radiation by accumulating DNA breaks , through altering the expression of DNA-PK Complex, and DDR proteins , via selective estrogen receptor modulation, offering a novel strategy for combating radioresistance. (bvsalud.org)
  • In contrast to the conventional mechanism of nuclear receptor ligand activation, activation of ERRgamma by GSK4716 does not appear to involve a major rearrangement or significant stabilization of the C-terminal helix. (rcsb.org)
  • Nevertheless, the effects of estrogen-related genes (ERGs) on THCA stages, immunological infiltration, and treatment susceptibility have not been well explored. (biomedcentral.com)
  • Univariate Cox and least absolute shrinkage and selection operator (LASSO) analyses were used to identify the set of estrogen-related differentially expressed genes (ERDEGs) associated with progression-free intervals (PFI) and to establish a prediction model. (biomedcentral.com)
  • This indicates that estrogen and related genes play an important role in thyroid cancer, but the specific mechanism needs further exploration. (biomedcentral.com)
  • This study aimed to use a database and experimental validation to better understand the role of estrogen-related genes (ERGs) in THCA. (biomedcentral.com)
  • Correlation analysis was used to identify estrogen-related differentially expressed genes (ERDEGs). (biomedcentral.com)
  • Title: Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. (aablocks.com)
  • The farnesoid X receptor (FXR) regulates the homeostasis of bile acids, lipids and glucose. (nature.com)
  • Estrogens are known to play an important role in regulating bone homeostasis. (qscience.com)
  • This effect is at least in part due to altered calcium permeability of the cell membrane, reduction of chloride influx through the gamma-aminobutyric acid (GABA)-A receptor, and action of estrogen as a glutamate agonist in the hippocampus. (medscape.com)
  • 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)
  • d) Identify the liver GDF15 receptor and elucidate its signaling pathway in the liver. (upenn.edu)
  • Using piperine, we propose a new strategy for overcoming acquired radioresistance through estrogen receptor -mediated modulation of the NHEJ pathway. (bvsalud.org)
  • The piperine effect on Estrogen receptor modulation, DNA - Damage, DNA -Damage-Response, and apoptosis was done by western blotting , immunofluorescence , yeast -based- estrogen -receptor-LacZ-reporter assay, and nuclear translocation analysis . (bvsalud.org)
  • Although hormone therapy with an anti-estrogen agent is an optional therapy for recurrent epithelial ovarian cancers, both basic and clinical researches are insufficient. (biomedcentral.com)
  • Exactly which of the components is responsible for the anti-estrogen effect the researchers do not know. (ergo-log.com)
  • Supplements that also have an anti-estrogen effect are Ginkgo biloba, green tea and gamma-linoleic acid. (ergo-log.com)
  • At menarche, pituitary gonadotropins (FSH and LH) and ovarian steroids (estrogen and progesterone) increase in overall concentration. (medscape.com)
  • Estrogen causes proliferation of ovarian cancer cells. (biomedcentral.com)
  • Estrogen receptor (ER)α was assayed in four ovarian cancer cell lines by the RT-PCR method. (biomedcentral.com)
  • After menopause, ovarian estrogen production ceases, while ovarian androgen production varies. (msdmanuals.com)
  • Members of this family show sequence homology with estrogen receptors but are incapable of being bound by estrogen. (nature.com)
  • 2002). T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. (columbiabiosciences.com)
  • Peroxisome proliferator-activated receptor coactivator-1alpha (PGC-1alpha) coactivates the cardiac-enriched nuclear receptors estrogen-related receptor-alpha and -gamma. (harvard.edu)
  • Development of a homogeneous, fluorescence resonance energy transfer-based in vitro recruitment assay for peroxisome proliferator-activated receptor delta via selection of active LXXLL coactivator peptides. (columbiabiosciences.com)
  • Interaction of organochlorine compounds with thyroid receptor, transthyretin, and thyroid-binding globulin. (cdc.gov)
  • This all helical domain is involved in binding the hormone in these receptors. (rcsb.org)
  • Besides functioning as an antioxidant and anthelmintic , many isoflavones have been shown to interact with animal and human estrogen receptors , causing effects in the body similar to those caused by the hormone estrogen . (wikipedia.org)
  • Title: Accessibility of the extracellular loops of follicle stimulating hormone receptor and their role in hormone-receptor interaction. (aablocks.com)
  • Some chemicals in hops seem to act similarly to the hormone estrogen and some seem to cause sleepiness. (medlineplus.gov)
  • Some chemicals in hops act like the hormone estrogen. (medlineplus.gov)
  • 1998. Induction of mammary tumors in rats by single- dose gamma irradiation at different ages. (cdc.gov)
  • 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)
  • is determined in men when reduced testosterone production is suspected, e.g. in hypogonadism, estrogen therapy, chromosome aberrations (as in the Klinefelter's syndrome) and liver cirrhosis. (cdc.gov)
  • 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)
  • Although epilepsy may be expressed at this time in part due to this increase in estrogen, cyclic increases in estrogen relative to progesterone appear as a likely trigger for breakthrough seizures. (medscape.com)
  • When such chemical-signals couple or bind to a receptor, they cause some form of cellular/tissue-response, e.g. a change in the electrical-activity of a cell. (hla-a.com)
  • Although the lack of estrogen receptor β (ERβ) is a risk factor for the development of inflammatory bowel disease (IBD) and psychiatric disorders, the underlying cellular and molecular mechanisms are not fully understood. (biomedcentral.com)
  • BPA as well as its nitrated and chlorinated metabolites seems to binds strongly to ERR-γ (dissociation constant = 5.5 nM), but not to the estrogen receptor (ER). (wikipedia.org)
  • 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma. (columbiabiosciences.com)
  • Piperine enhanced the radiation -induced cell death and enhanced the expression and activation of Estrogen receptor ß, while Estrogen receptor α expression and activation were reduced. (bvsalud.org)
  • However, adrenal production of prohormones (eg, dehydroepiandrosterone sulfate [DHEAS]) that are converted to both androgens and estrogens in peripheral cells decreases starting in a woman's 30s. (msdmanuals.com)
  • 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)
  • Since the cloning of estrogen receptor (ER)-β, many studies have demonstrated ER-β expression in MNCs (Shughrue et al. (jneurosci.org)
  • It has been reported that estrogen can stimulate the growth of spinous cells and synapse, while also increase the expression of brain-derived neurotrophic factor ( BDNF ) [ 9 , 10 ]. (psychiatryinvestigation.org)
  • Cytokine levels (IL-1beta, IL-2, IL-6, TNF-alpha, IFN-gamma) and sIL-2R of individual patients before, during (3 months) and after (6 months) therapy were evaluated and correlated to clinical response according to UICC criteria (responder patients-partial or Complete Response versus non-responder patients-Stable/Progression). (nih.gov)
  • Therefore, studying how estrogen and other female hormones affect the initiation, progression, and outcomes of THCA is crucial. (biomedcentral.com)
  • A flurry of studies supports a role for gamma-linolenic acid to further suppress chronic inflammatory reactions. (lifeextension.com)
  • Estrogen, which plays an important role in establishing neural and behavioral sex differences, has been suggested to be related to the sexual dimorphism of ADHD by some scholars [ 7 , 8 ]. (psychiatryinvestigation.org)
  • Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. (nature.com)