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Gen Comp Endocrinol
January 2024
Guangdong Research Center on Reproductive Control and Breeding Technology of Indigenous Valuable Fish Species, Guangdong Provincial Key Laboratory of Pathogenic Biology and Epidemiology for Aquatic Economic Animals, Fisheries College, Guangdong Ocean University, Zhanjiang 524088, China; Key Laboratory of Utilization and Conservation for Tropical Marine Bioresources of Ministry of Education, Hainan Key Laboratory for Conservation and Utilization of Tropical Marine Fishery Resources, Yazhou Bay Innovation Institute, Hainan Tropical Ocean University, Sanya 572022, China; Southern Marine Science and Engineering Guangdong Laboratory (Zhanjiang), Zhanjiang 524025, China. Electronic address:
Estrogen receptors (ERs) play a critical role in vitellogenesis (Vtgs). However, the contribution of each ER for the regulation of vtgs expression was not analyzed clearly in teleosts. In the present study, three ers isoforms (erα, erβ1, and erβ2) were cloned in pompano (Trachinotus ovatus).
View Article and Find Full Text PDFEur J Med Chem
April 2020
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, CCB - Centrum for Chemistry and Biomedicine, Innsbruck, Austria. Electronic address:
Up to 80% of mammary carcinoma initially exhibit estrogen-dependent growth, which can be treated by aromatase inhibitors or SERMs/SERDs. To increase the options after failure of the hormonal therapy with these drugs, the search for alternatives with a different mode of action to prevent estrogen action is of high relevance. Therefore, this study focused on the inhibition of coactivator recruitment at the estrogen receptor (ER) by targeted attachment of bivalent compounds at the coactivator binding site besides the primary binding at the ligand binding domain.
View Article and Find Full Text PDFTalanta
February 2008
Chemistry Department, Pontifícia Universidade Católica do Rio de Janeiro (PUC-RJ), Rio de Janeiro, RJ 22453-900, Brazil.
In this work, a fluorimetric approach for the determination of cyclofenil, 4-4'-(cyclohexylidenemethylene)bis(phenylacetate), is presented. The method was based on the intense fluorescence (250/410 nm) observed after a UV photochemical treatment of cyclofenil. The influence of the pH and solvent system and UV exposure time on the fluorescence magnitude was studied.
View Article and Find Full Text PDFJ Endocrinol Invest
February 1990
Istituto Clinica Ostetrica e Ginecologica, Università di Modena, Italy.
The aim of the present study was to evaluate the effects of estrogens and androgens on hypothalamic beta-endorphin (beta-EP) concentrations. Intact or castrated female rats were chronically (2 weeks) treated with estrogen (estradiol benzoate) and/or antiestrogens (clomiphene, cyclophenil or epimestrol), and with androgens (dihydrotestosterone or dehydroepiandrosterone sulphate) and/or antiandrogen (cyproterone acetate). A group of rats treated with vehicle were studied as comparison.
View Article and Find Full Text PDFSynthetic nonsteroidal antiestrogens are bound intracellularly by two high affinity saturable bindings sites, the estrogen receptor and the microsomal antiestrogen-binding site (AEBS). In order to further define the structural requirements for ligand binding to AEBS from rat liver and the MCF 7 human breast cancer cell line, the relative binding affinities of an extensive series of structurally related ligands were investigated using competitive binding assay techniques. The groups of compounds studied were: analogues of the triphenylethylene antiestrogens, Cl 628 and tamoxifen; analogues of cyclofenil; bibenzyl and stilbene derivatives; analogues of the cytochrome P-450 inhibitor SKF-525A; phenothiazine derivatives; and a series of structurally related compounds with a variety of pharmacological activities.
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