Estrogen Antagonists

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  Subject Areas on Research

  • 17beta-Estradiol inhibits Ca2+-dependent homeostasis of airway surface liquid volume in human cystic fibrosis airway epithelia. 
  • A negative coregulator for the human ER. 
  • Acute upper airway angioedema secondary to acquired C1 esterase inhibitor deficiency: a case report. 
  • American Society of Clinical Oncology technology assessment of pharmacologic interventions for breast cancer risk reduction including tamoxifen, raloxifene, and aromatase inhibition. 
  • Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. 
  • Anti-estrogenic compounds increase prolactin and growth hormone synthesis in clonal strains of rat pituitary cells. 
  • Antiestrogen can establish nonproductive receptor complexes and alter chromatin structure at target enhancers. 
  • Antifungal activities of antineoplastic agents: Saccharomyces cerevisiae as a model system to study drug action. 
  • BRCA1 expression is not directly responsive to estrogen. 
  • Basal cells are a multipotent progenitor capable of renewing the bronchial epithelium. 
  • Bazedoxifene exhibits antiestrogenic activity in animal models of tamoxifen-resistant breast cancer: implications for treatment of advanced disease. 
  • Cellular mechanisms which distinguish between hormone- and antihormone-activated estrogen receptor. 
  • Circulating Biomarkers and Resistance to Endocrine Therapy in Metastatic Breast Cancers: Correlative Results from AZD9496 Oral SERD Phase I Trial. 
  • Coactivator AIB1 links estrogen receptor transcriptional activity and stability. 
  • Comparative analyses of mechanistic differences among antiestrogens. 
  • Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators. 
  • Definition of the cellular mechanisms which distinguish between hormone and antihormone activated steroid receptors. 
  • Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators. 
  • Development of an ER action indicator mouse for the study of estrogens, selective ER modulators (SERMs), and Xenobiotics. 
  • Development of peptide antagonists that target estrogen receptor beta-coactivator interactions. 
  • Development of peptide antagonists that target estrogen receptor-cofactor interactions. 
  • Differential interaction of the methoxychlor metabolite 2,2-bis-(p-hydroxyphenyl)-1,1,1-trichloroethane with estrogen receptors alpha and beta. 
  • Dissection of the molecular mechanism of action of GW5638, a novel estrogen receptor ligand, provides insights into the role of estrogen receptor in bone. 
  • Effects of single and combined exposures to benzo(a)pyrene and 3,3'4,4'5-pentachlorobiphenyl on EROD activity and development in Fundulus heteroclitus. 
  • Endocrine therapy in metastatic breast cancer. 
  • 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 transactivation in MCF-7 breast cancer cells by melatonin and growth factors. 
  • Estrogen stimulation and tamoxifen inhibition of leiomyoma cell growth in vitro and in vivo. 
  • Estrogen-induced activation of mitogen-activated protein kinase requires mobilization of intracellular calcium. 
  • Estrogen-induced mitogenesis of MCF-7 cells does not require the induction of mitogen-activated protein kinase activity. 
  • Evaluation of a recombinant yeast cell estrogen screening assay. 
  • Expression of functional estrogen receptor beta in locus coeruleus-derived Cath.a cells. 
  • G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. 
  • Glutathione transferase pi class 2 (GSTp2) protects against the cardiac deformities caused by exposure to PAHs but not PCB-126 in zebrafish embryos. 
  • Identification of a negative regulatory function for steroid receptors. 
  • Identification of resting cells by dual-parameter flow cytometry of statin expression and DNA content. 
  • Identification of the sequences within the human complement 3 promoter required for estrogen responsiveness provides insight into the mechanism of tamoxifen mixed agonist activity. 
  • Interaction of methoxychlor and related compounds with estrogen receptor alpha and beta, and androgen receptor: structure-activity studies. 
  • Investigation of antiestrogenic properties of unleaded gasoline in female mice. 
  • Novel estrogen response elements identified by genetic selection in yeast are differentially responsive to estrogens and antiestrogens in mammalian cells. 
  • Pathologic and biologic response to preoperative endocrine therapy in patients with ER-positive ductal carcinoma in situ. 
  • Patterns of heritability of decreased EROD activity and resistance to PCB 126-induced teratogenesis in laboratory-reared offspring of killifish (Fundulus heteroclitus) from a creosote-contaminated site in the Elizabeth River, VA, USA. 
  • Peptide antagonists of the human estrogen receptor. 
  • Preclinical evidence for therapeutic efficacy of selective estrogen receptor modulators for uterine leiomyoma. 
  • Prior breast cancer and tamoxifen exposure does not influence outcomes in women with uterine papillary serous carcinoma. 
  • Proceedings of the Fourth International Conference on Recent Advances and Future Directions in Endocrine Manipulation of Breast Cancer: conference summary statement. 
  • Prognostic and predictive factors for patients with metastatic breast cancer undergoing aggressive induction therapy followed by high-dose chemotherapy with autologous stem-cell support. 
  • Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development. 
  • RU486 exerts antiestrogenic activities through a novel progesterone receptor A form-mediated mechanism. 
  • Regulation of estrogen receptors and MMP-2 expression by estrogens in human retinal pigment epithelium. 
  • Relationship between expression of coactivators and corepressors of hormone receptors and resistance of ovarian cancers to growth regulation by steroid hormones. 
  • Research resource: Transcriptional profiling in a cellular model of breast cancer reveals functional and mechanistic differences between clinically relevant SERM and between SERM/estrogen complexes. 
  • Sex steroid receptor analysis in human melanoma. 
  • Systemic therapy for older women with breast cancer. 
  • Tamoxifen in postmenopausal women a safety perspective. 
  • Tamoxifen versus aromatase inhibitors for breast cancer prevention. 
  • Temporally distinct and ligand-specific recruitment of nuclear receptor-interacting peptides and cofactors to subnuclear domains containing the estrogen receptor. 
  • 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 granulin-epithelin precursor is a steroid-regulated growth factor in endometrial cancer. 
  • The human estrogen receptor-alpha is a ubiquitinated protein whose stability is affected differentially by agonists, antagonists, and selective estrogen receptor modulators. 
  • The management of desmoid tumors. 
  • 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. 
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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