Ligand structure-dependent activation of estrogen receptor alpha/Sp by estrogens and xenoestrogens.

The Journal of Steroid Biochemistry and Molecular Biology
Fei WuS Safe

Abstract

This study investigated the effects of E2, diethylstilbestrol (DES), antiestrogens, the phytoestrogen resveratrol, and the xenoestrogens octylphenol (OP), nonylphenol (NP), endosulfan, kepone, 2,3,4,5-tetrachlorobiphenyl-4-ol (HO-PCB-Cl(4)), bisphenol-A (BPA), and 2,2-bis-(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) on induction of luciferase activity in breast cancer cells transfected with a construct (pSp1(3)) containing three tandem GC-rich Sp binding sites linked to luciferase and wild-type or variant ERalpha. The results showed that induction of luciferase activity was highly structure-dependent in both MCF-7 and MDA-MB-231 cells. Moreover, RNA interference assays using small inhibitory RNAs for Sp1, Sp3 and Sp4 also demonstrated structure-dependent differences in activation of ERalpha/Sp1, ERalpha/Sp3 and ERalpha/Sp4. These results demonstrate for the first time that various structural classes of ER ligands differentially activate wild-type and variant ERalpha/Sp-dependent transactivation, selectively use different Sp proteins, and exhibit selective ER modulator (SERM)-like activity.

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Citations

Jul 26, 2012·Angiogenesis·Nicolas ClereSébastien Faure
Sep 25, 2012·Asian Journal of Andrology·Stephen Safe
Sep 6, 2008·Journal of Molecular Endocrinology·Stephen Safe, Kyounghyun Kim
Feb 17, 2009·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·E L GregoraszczukE Ropstad
Jan 9, 2015·Environment International·Jayshree Annamalai, Vasudevan Namasivayam
Sep 20, 2012·Journal of Environmental and Public Health·Sam De Coster, Nicolas van Larebeke
Jul 14, 2016·Environmental Health : a Global Access Science Source·Vincent NedellecWilliam Dab

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