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Showing 1 to 20 of 27 for “"Antiestrogen"”.
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Analysis of Estrogen and Antiestrogen Receptor Complexes
I have used affinity labeling ligands for the estrogen receptor (ER) to examine the structure and relatedness of ER in different target tissues and species. In addition, I have characterized the first efficient and selective affinity labeling estrogen, ketononestrol aziridine (KNA).
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Comparative Study of Antiestrogen Action in the Immature Rat Uterus
Made available in DSpace on 2014-12-14T13:39:39Z (GMT). No. of bitstreams: 1 7708989.pdf: 5722118 bytes, checksum: 2dd30d0473f1d1fca18ad843d0e3ac1c (MD5) Previous issue date: 1976
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Bioactivities of Antiestrogens and Antiestrogen Metabolites in the Rat and Mouse
… that a number of the triarylethylene-type antiestrogens act as pro-drugs, being converted in vivo to metabolites having greater estrogenic and antiestrogenic potency than their parent compounds. This laboratory has revealed that two potent nonsteroidal antiestrogens,
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Potential Antiestrogen-Based Cytotoxic Agents and an Affinity Label for the Estrogen Receptor
My thesis research involved studying the role of the estrogen receptor (ER) mediating the cytotoxicity of various tamoxifen derivatives in human breast cancer cells and examining estrogen structure and function using an affinity labeling compound, tamoxifen aziridine (TA).
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Estrogen and Antiestrogen Action in the Medial Basal Hypothalamus and Pituitary: Dopamine-Prolactin Interrelationships (d-2 Receptors, Bromocriptine)
The actions of estradiol and antiestrogens on dopamine turnover and prolactin levels were studied in the medial basal hypothalamus (MBH), anterior pituitary, and serum of immature female rats. Estradiol increased MBH dopamine levels and turnover and pituitary and serum prolactin concentrations in a …
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Altered estrogen receptor and transforming growth factor pathways in models of estrogen-autonomous and of antiestrogen-resistant MCF-7 human breast cancer cells
… of breast tumors to steroid-autonomous and antiestrogen-resistant phenotypes confounds our ability to treat breast cancer with antiestrogens, the most efficacious hormone treatment used clinically. We developed two models in the MCF-7 cell line, an estrogen receptor-positive human breast …
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Mechanism of Action of Antiestrogens in Breast Cancer and Uterine Cells (Estrogen Receptor)
The actions of antiestrogen (AE) on growth and protein synthesis were studied in human breast cancer cells and rat uterus. Antiestrogens bind with high affinity to the estrogen receptor (ER) and to additional microsomal binding sites to which estrogens do not bind called antiestrogen binding sites …
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Detailed Analysis of Transcriptional Regulation by Activation Functions-1 and -2 of the Human Estrogen Receptor
… of ER, that was promoted by both estradiol and antiestrogen binding. This interaction was transcriptionally productive, however, only in the presence of estradiol. In subsequent studies, we examined the ability of the steroid receptor coactivator-1 (SRC-1) protein to facilitate the integration …
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Hormonal modulation of sex steroid hormone receptors and oncogenes in human breast cancer cells
… and were blocked by addition of excess antiestrogen. Treatment with the progestin R5020 (10 nM) partly reversed E$\sb2$ effects on ER. R5020 and the antiprogestin RU486 (10 nM) both reduced PR mRNA levels by 50% but did not change HER-2/neu. In T47D cells, which contain low ER and high …
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Estrogen Receptor-Mediated Gene Expression in Cultured Epithelial Cells of Rat Efferent Ductules
… reversed by treatment with ICI 182,780, a pure antiestrogen. The differentially displayed products were tested in Northern blot hybridization and some transcripts were confirmed to be genes expressed in the efferent ductules under estrogen regulation. However, the nucleotide sequences of these …
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Ανοσοϊστοχημική μελέτη της έκφρασης των οιστρογονικών υποδοχέων στους όγκους των ωοθηκών με μονοκλωνικά αντισώματα (με την μέθοδο αβιντίνης-βιοτίνης)
… undifferentiates carcinomas, are candidates for antiestrogen endocrine therapy, adjuvant to surgery and chemotherapy. Our method can detect ER in paraffin sections of ovarian tumors with precision, thus making possible both their retrospective examination and the simultaneous comparison of their …
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Interrelationships among estrogen, insulin-like growth factor-I and cyclic adenosine monophosphate in the regulation of uterine progesterone and estrogen receptors
… was suppressed equally by co-treatment with antiestrogen (ICI 164,384) or protein kinase inhibitors, or by pre-treatment of cells with actinomycin D or cycloheximide. These results suggest that regulation of PR occurs at the level of the PR gene, and that induction of PR stimulated by these …
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Expression of Human Estrogen Receptor and Studies of Estrogen-Mediated Transcription and Apoptosis
E2 and the antiestrogen OHT, each induce apoptosis in stably transfected hER positive HeLa-ER5 cells. Using transient transfections and a reporter system to measure p38 activity, we show that E2 induces the p38 activity 12--36 fold in several ER positive cell lines, while OHT induces p38 activity …
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Synthesis of Cytotoxic Antiestrogens and Control Compounds (Nafoxidine)
… cancer, potentially cytotoxic conjugates of an antiestrogen, desmethylnafoxidine, were prepared. Two short and efficient routes for the synthesis of a nafoxidine precursor were developed, one featuring the alpha-phenylation of a ketone and one the nickel-catalyzed cross-coupling of a Grignard …
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The autoregulatory and tissue-specific activation of gene expression by estrogen receptor
… mRNA. This data, and the ability of the antiestrogen, hydroxytamoxifen, to reverse persistent induction of estrogen receptor mRNA, support a model in which transient doses of estradiol-17$\beta$ induce the estrogen receptor and thereby establish an autoregulatory loop. The low levels of …
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Estrogen Receptor -Dependent and Estrogen Receptor-Independent Pathways for Tamoxifen and 4-Hydroxytamoxifen-Induced Programmed Cell Death
… common methods of breast cancer treatment is antiestrogen treatment. The therapeutic efficacy of the selective estrogen receptor modulator tamoxifen (TAM) in cancer therapy is thought to arise from its ability to compete with estrogens for binding to the ER. We show that TAM and its active …
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Necrotic cell death: A novel outcome of BHPI-hyperactivation of the anticipatory unfolded protein response
… binding of estrogen to ERa. These small molecule antiestrogens work by inhibiting the proproliferative actions of estrogen but after years of treatment, many cancers recur as resistant tumors. Recently, we discovered a non-competitive modulator of ERa that works in a strikingly different way. BHPI …
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The anticipatory unfolded protein response and estrogen receptor mutations in breast cancer
… E2:ERα activity often leads to development of antiestrogen resistance. Approximately 30% of patients who have metastatic endocrine therapy resistant breast cancer express ERα mutations. Two of the most common and therefore widely studied mutations are ERαY537S and ERαD538G. Patients whose …
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Effects of acetaminophen on estrogen-responsive alkaline phosphatase in Ishikawa endometrial cancer cells
… of this study looked at the interaction between antiestrogen-4-hydroxy tamoxifen (OHT) and APAP on alkaline phosphatase activity in Ishikawa cells. While OHT inhibited alkaline phosphatase activity ∼50 percent in estradiol-induced cells, addition of 0.03-1mM APAP increased inhibition …
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Factors influencing in vitro maturation of pig oocytes
… steroid free medium in the presence of either an antiestrogen (tamoxifen) or an aromatase inhibitor (4-OHA). Before use, the content of estradiol receptors (ER) in CC and oocytes were determined by a binding assay, before, during and after maturation. The highest levels of ER were observed at 24 …
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