Estrogen Receptor alpha

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  Subject Areas on Research

  • 3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding. 
  • A negative coregulator for the human ER. 
  • A role for peroxisome proliferator-activated receptor γ coactivator-1 in the control of mitochondrial dynamics during postnatal cardiac growth. 
  • Activity of a Py-Im polyamide targeted to the estrogen response element. 
  • Allosteric regulation of estrogen receptor structure, function, and coactivator recruitment by different estrogen response elements. 
  • Application of random peptide phage display to the study of nuclear hormone receptors. 
  • Association of genetic polymorphisms of ER-alpha and the estradiol-synthesizing enzyme genes CYP17 and CYP19 with breast cancer risk in Chinese women. 
  • Atenolol induced HDL-C change in the pharmacogenomic evaluation of antihypertensive responses (PEAR) study. 
  • Bazedoxifene exhibits antiestrogenic activity in animal models of tamoxifen-resistant breast cancer: implications for treatment of advanced disease. 
  • Biological and biochemical consequences of global deletion of exon 3 from the ER alpha gene. 
  • Biological assessment of bisphenol A degradation in water following direct photolysis and UV advanced oxidation. 
  • Bisphenol A activates EGFR and ERK promoting proliferation, tumor spheroid formation and resistance to EGFR pathway inhibition in estrogen receptor-negative inflammatory breast cancer cells. 
  • Bisphenol A affects androgen receptor function via multiple mechanisms. 
  • Bisphenol A exposure alters developmental gene expression in the fetal rhesus macaque uterus. 
  • Bisphenol A interacts with the estrogen receptor alpha in a distinct manner from estradiol. 
  • Chemoprevention of NMU-induced rat mammary carcinoma with the combination of melatonin and 9-cis-retinoic acid. 
  • Circulating Biomarkers and Resistance to Endocrine Therapy in Metastatic Breast Cancers: Correlative Results from AZD9496 Oral SERD Phase I Trial. 
  • Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor. 
  • Coactivator AIB1 links estrogen receptor transcriptional activity and stability. 
  • Common estrogen receptor polymorphism augments effects of hormone replacement therapy on E-selectin but not C-reactive protein. 
  • Comparative analyses of mechanistic differences among antiestrogens. 
  • Complexity in endometrial estradiol signaling. 
  • Connections and regulation of the human estrogen receptor. 
  • Constitutively active ESR1 mutations in gynecologic malignancies and clinical response to estrogen-receptor directed therapies. 
  • Coregulators in nuclear estrogen receptor action: from concept to therapeutic targeting. 
  • DNA Sequence Constraints Define Functionally Active Steroid Nuclear Receptor Binding Sites in Chromatin. 
  • Defects of prostate development and reproductive system in the estrogen receptor-alpha null male mice. 
  • Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators. 
  • Delineation of a FOXA1/ERα/AGR2 regulatory loop that is dysregulated in endocrine therapy-resistant breast cancer. 
  • Designer monotransregulators provide a basis for a transcriptional therapy for de novo endocrine-resistant breast cancer. 
  • Development of peptide antagonists that target estrogen receptor beta-coactivator interactions. 
  • Differential interaction of the methoxychlor metabolite 2,2-bis-(p-hydroxyphenyl)-1,1,1-trichloroethane with estrogen receptors alpha and beta. 
  • Differential recruitment of co-regulatory proteins to the human estrogen receptor 1 in response to xenoestrogens. 
  • Differential regulation of estrogen receptor alpha, glucocorticoid receptor and retinoic acid receptor alpha transcriptional activity by melatonin is mediated via different G proteins. 
  • Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. 
  • Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. 
  • Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer. 
  • Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta. 
  • Distinct function of estrogen receptor α in smooth muscle and fibroblast cells in prostate development. 
  • Distinct properties of cell-type-specific and shared transcription factor binding sites. 
  • Dynamic shuttling and intranuclear mobility of nuclear hormone receptors. 
  • Dysregulation of ectonucleotidase-mediated extracellular adenosine during postmenopausal bone loss. 
  • ERAP75 functions as a coactivator to enhance estrogen receptor alpha transactivation in prostate stromal cells. 
  • ERα PvuII and XbaI polymorphisms in postmenopausal women with posterior tibial tendon dysfunction: a case control study. 
  • ERα Signaling Increased IL-17A Production in Th17 Cells by Upregulating IL-23R Expression, Mitochondrial Respiration, and Proliferation. 
  • ESR1 promoter hypermethylation does not predict atypia in RPFNA nor persistent atypia after 12 months tamoxifen chemoprevention. 
  • ESR1/SYNE1 polymorphism and invasive epithelial ovarian cancer risk: an Ovarian Cancer Association Consortium study. 
  • Early Endometriosis in Females Is Directed by Immune-Mediated Estrogen Receptor α and IL-6 Cross-Talk. 
  • Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer. 
  • Epistasis between polymorphisms in COMT, ESR1, and GCH1 influences COMT enzyme activity and pain. 
  • Estradiol replacement enhances cocaine-stimulated locomotion in female C57BL/6 mice through estrogen receptor alpha. 
  • Estrogen Receptor Signaling in the Immune System. 
  • Estrogen mediates neuroprotection and anti-inflammatory effects during EAE through ERα signaling on astrocytes but not through ERβ signaling on astrocytes or neurons. 
  • Estrogen protects against intracranial aneurysm rupture in ovariectomized mice. 
  • Estrogen receptor (ER) modulators each induce distinct conformational changes in ER alpha and ER beta. 
  • Estrogen receptor alpha (ESR1) mutant A908G is not a common feature in benign and malignant proliferations of the breast. 
  • Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women. 
  • Estrogen receptor-beta expression in extraabdominal fibromatoses: an analysis of 40 cases. 
  • Estrogen receptor-beta mediates male-female differences in the development of pressure overload hypertrophy. 
  • Estrogen-mediated epigenetic repression of large chromosomal regions through DNA looping. 
  • Estrogen-related receptor alpha induces the expression of vascular endothelial growth factor in breast cancer cells. 
  • Estrogen-related receptor alpha is critical for the growth of estrogen receptor-negative breast cancer. 
  • Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. 
  • Exemestane's 17-hydroxylated metabolite exerts biological effects as an androgen. 
  • Expression of functional estrogen receptor beta in locus coeruleus-derived Cath.a cells. 
  • Expression of mitochondrial membrane-linked SAB determines severity of sex-dependent acute liver injury. 
  • From empirical to mechanism-based discovery of clinically useful Selective Estrogen Receptor Modulators (SERMs). 
  • Generation and characterization of a complete null estrogen receptor alpha mouse using Cre/LoxP technology. 
  • Genetic and non-genetic factors associated with the phenotype of exceptional longevity & normal cognition. 
  • Genistein and bisphenol A exposure cause estrogen receptor 1 to bind thousands of sites in a cell type-specific manner. 
  • Hormone control and expression of androgen receptor coregulator MAGE-11 in human endometrium during the window of receptivity to embryo implantation. 
  • Hormone signaling and fatty liver in females: analysis of estrogen receptor α mutant mice. 
  • Human Genetic Variability Contributes to Postoperative Morphine Consumption. 
  • IL-23/IL-17A/TRPV1 axis produces mechanical pain via macrophage-sensory neuron crosstalk in female mice. 
  • Identification of a negative regulatory surface within estrogen receptor alpha provides evidence in support of a role for corepressors in regulating cellular responses to agonists and antagonists. 
  • Inhibition of Neu-induced mammary carcinogenesis in transgenic mice expressing ERΔ3, a dominant negative estrogen receptor α variant. 
  • Inhibition of estrogen signaling in myeloid cells increases tumor immunity in melanoma. 
  • Interaction of estrogen receptor alpha with protein kinase C alpha and c-Src in osteoblasts during differentiation. 
  • Interaction of methoxychlor and related compounds with estrogen receptor alpha and beta, and androgen receptor: structure-activity studies. 
  • Lactoferrin gene expression is estrogen responsive in human and rhesus monkey endometrium. 
  • Large, Non-Cavity Distorting Intramural Leiomyomas Decrease Leukemia Inhibitory Factor in the Secretory Phase Endometrium. 
  • Ligand-selective interactions of ER detected in living cells by fluorescence resonance energy transfer. 
  • Loss of epithelial oestrogen receptor α inhibits oestrogen-stimulated prostate proliferation and squamous metaplasia via in vivo tissue selective knockout models. 
  • Lysine-specific histone demethylase 1 inhibitors control breast cancer proliferation in ERα-dependent and -independent manners. 
  • Melatonin inhibits estrogen receptor transactivation and cAMP levels in breast cancer cells. 
  • Mining the complexities of the estrogen signaling pathways for novel therapeutics. 
  • Mitofusins 1/2 and ERRalpha expression are increased in human skeletal muscle after physical exercise. 
  • Modulation of estrogen receptor-alpha transcriptional activity by the coactivator PGC-1. 
  • Molecular mechanisms of development of the human fetal female reproductive tract. 
  • Neomorphic ERα Mutations Drive Progression in Breast Cancer and Present a Challenge for New Drug Discovery. 
  • Neuroendocrine gene polymorphisms and susceptibility to juvenile idiopathic arthritis. 
  • Neuroprotection mediated through estrogen receptor-alpha in astrocytes. 
  • Next-Generation Endocrine Therapies for Breast Cancer. 
  • Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer. 
  • Peptide antagonists of the human estrogen receptor. 
  • Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. 
  • Prediagnostic Smoking Is Associated with Binary and Quantitative Measures of ER Protein and ESR1 mRNA Expression in Breast Tumors. 
  • Pregnancy and Smoothelin-like Protein 1 (SMTNL1) Deletion Promote the Switching of Skeletal Muscle to a Glycolytic Phenotype in Human and Mice. 
  • Prevention of the polycystic ovarian phenotype and characterization of ovulatory capacity in the estrogen receptor-alpha knockout mouse. 
  • Prostate-derived Ets factor, an oncogenic driver in breast cancer. 
  • Radiation-associated breast cancer and gonadal hormone exposure: a report from the Childhood Cancer Survivor Study. 
  • Re: KAI1/CD82 is a novel target of estrogen receptor-mediated gene repression and downregulated in primary human breast cancer (Int J Cancer 123: 2239-2246, 2008). 
  • Reduced prostate branching morphogenesis in stromal fibroblast, but not in epithelial, estrogen receptor α knockout mice. 
  • Regression of NMU-induced mammary tumors with the combination of melatonin and 9-cis-retinoic acid. 
  • Regulation of estrogen receptors and MMP-2 expression by estrogens in human retinal pigment epithelium. 
  • Requirement of estrogen receptor alpha DNA-binding domain for HPV oncogene-induced cervical carcinogenesis in mice. 
  • Resveratrol and endometrium: a closer look at an active ingredient of red wine using in vivo and in vitro models. 
  • Risk factors for breast cancer characterized by the estrogen receptor alpha A908G (K303R) mutation. 
  • Roles of estrogen in the formation of intracranial aneurysms in ovariectomized female mice. 
  • Steroid induction of therapy-resistant cytokeratin-5-positive cells in estrogen receptor-positive breast cancer through a BCL6-dependent mechanism. 
  • Structural basis for an unexpected mode of SERM-mediated ER antagonism. 
  • Structural insights into corepressor recognition by antagonist-bound estrogen receptors. 
  • Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma. 
  • Subglutinol A, an immunosuppressive α-pyrone diterpenoid from Fusarium subglutinans, acts as an estrogen receptor antagonist. 
  • Subtype specific estrogen receptor action protects against changes in MMP-2 activation in mouse retinal pigmented epithelial cells. 
  • Targeted disruption of the estrogen receptor-alpha gene in female mice: characterization of ovarian responses and phenotype in the adult. 
  • Temporally distinct and ligand-specific recruitment of nuclear receptor-interacting peptides and cofactors to subnuclear domains containing the estrogen receptor. 
  • The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. 
  • The Estrogen Receptor α Cistrome in Human Endometrium and Epithelial Organoids. 
  • The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. 
  • The Lineage Determining Factor GRHL2 Collaborates with FOXA1 to Establish a Targetable Pathway in Endocrine Therapy-Resistant Breast Cancer. 
  • The bi-modal effects of estradiol on gonadotropin synthesis and secretion in female mice are dependent on estrogen receptor-alpha. 
  • The estrogen receptor as a mediator of the pathological actions of cholesterol in breast cancer. 
  • The estrogen receptor beta-isoform (ERbeta) of the human estrogen receptor modulates ERalpha transcriptional activity and is a key regulator of the cellular response to estrogens and antiestrogens. 
  • The estrogen receptor-alpha A908G (K303R) mutation occurs at a low frequency in invasive breast tumors: results from a population-based study. 
  • The human estrogen receptor-alpha is a ubiquitinated protein whose stability is affected differentially by agonists, antagonists, and selective estrogen receptor modulators. 
  • The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy. 
  • Tissue interactions and estrogenic response during human female fetal reproductive tract development. 
  • Toxicology of environmental estrogens. 
  • Tumor Cell-Independent Estrogen Signaling Drives Disease Progression through Mobilization of Myeloid-Derived Suppressor Cells. 
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  Keywords of People

  • Berchuck, Andrew, James M. Ingram Distinguished Professor of Gynecologic Oncology, Obstetrics and Gynecology, Gynecologic Oncology
  • McDonnell, Donald Patrick, Glaxo-Wellcome Distinguished Professor of Molecular Cancer Biology, in the School of Medicine, Cell Biology
  • Moorman, Patricia Gripka, Professor Emeritus in Family Medicine and Community Health, Duke Cancer Institute