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Molecular cloning of estrogen receptor and its function on vitellogenesis in pompano (Trachinotus ovatus).
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 PDFDistinct Roles of Estrogen Receptors in the Regulation of Vitellogenin Expression in Orange-Spotted Grouper ().
Int J Mol Sci
August 2022
State Key Laboratory of Biocontrol and School of Life Sciences, Southern Marine Science and Engineering Guangdong Laboratory (Zhuhai), Guangdong Provincial Key Laboratory for Aquatic Economic Animals and Guangdong Provincial Engineering Technology Research Center for Healthy Breeding of Important Economic Fish, Sun Yat-Sen University, Guangzhou 510275, China.
During their breeding season, estrogen induces vitellogenin (VTG) production in the liver of teleost fish through estrogen receptors (ERs) that support oocyte vitellogenesis. There are at least three ER subtypes in teleost fish, but their roles in mediating E-induced VTG expression have yet to be ascertained. In this study, we investigated the expression of and in the liver of orange-spotted grouper ().
View Article and Find Full Text PDFImprovement in aqueous solubility of achiral symmetric cyclofenil by modification to a chiral asymmetric analog.
Sci Rep
June 2021
Graduate School of Life Sciences, Tohoku University, 2-1-1, Katahira, Aoba-ku, Sendai, Miyagi, 980-8577, Japan.
Decreasing the partition coefficient (LogP) by the introduction of a hydrophilic group is the conventional approach for improving the aqueous solubility of drug candidates, but is not always effective. Since melting point is related to aqueous solubility, we and other groups have developed alternative strategies to improve solubility by means of chemical modification to weaken intermolecular interaction in the solid state, thereby lowering the melting point and increasing the solubility. Here, we show that converting the symmetrical molecular structure of the clinically used estrogen receptor (ER) antagonist cyclofenil (1) into asymmetrical form by introducing an alkyl group enhances the aqueous solubility.
View Article and Find Full Text PDFDevelopment of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.
Eur 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 PDFEstrogen Receptors Alpha and Beta in POA-AHA Region Regulate Asymmetrically Ovulation.
Cell Mol Neurobiol
November 2019
Reproductive Biology Research Unit, Neuroendocrinology Laboratory, Facultad de Estudios Superiores Zaragoza, UNAM, Col. Ejército de Oriente, Campus II, Batalla 5 de mayo s/n esquina, Iztapalapa, Fuerte De Loreto, C.P 09230, Mexico.
We examined the role of the estrogen receptors alpha (ERα) and beta (ERβ) in of the preoptic-anterior hypothalamic area (POA-AHA) in the regulation of ovulation in rats. The number of ERα- and ERβ-immunoreactive (-ir) cells was determined at 09:00, 13:00, and 17:00 h of each stage of the estrous cycle in intact rats. Additionally, the effects of blocking ERα and ERβ on ovulation rate at 09:00 h on diestrus-2 or proestrus day through the microinjection of methyl-piperidino-pyrazole (MPP) or cyclofenil in either side of POA-AHA were evaluated.
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