scholarly journals Synthesis of Biphenyl Proteomimetics as Estrogen Receptor-α Coactivator Binding Inhibitors

2009 ◽  
Vol 11 (23) ◽  
pp. 5370-5373 ◽  
Author(s):  
Anna B. Williams ◽  
Patrick T. Weiser ◽  
Robert N. Hanson ◽  
Jillian R. Gunther ◽  
John A. Katzenellenbogen
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Α ◽  
Coactivator Binding Inhibitors ◽  
Binding Inhibitors

scholarly journals Perturbation of Estrogen Receptor α Localization with Synthetic Nona-Arginine LXXLL-Peptide Coactivator Binding Inhibitors

2009 ◽  
Vol 16 (7) ◽  
pp. 702-711 ◽  
Author(s):  
Maëlle Carraz ◽  
Wilbert Zwart ◽  
Trang Phan ◽  
Rob Michalides ◽  
Luc Brunsveld
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Α ◽  
Coactivator Binding Inhibitors ◽  
Binding Inhibitors

scholarly journals Bisphenol A derivatives act as novel coactivator binding inhibitors for estrogen receptor β

2021 ◽  
Author(s):  
Masaki Iwamoto ◽  
Takahiro Masuya ◽  
Mari Hosose ◽  
Koki Tagawa ◽  
Tomoka Ishibashi ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Bisphenol A ◽  
Wild Type ◽  
Chemical Library ◽  
Ligand Interaction ◽  
Docking Simulations ◽  
Coactivator Binding Inhibitors ◽  
Direct Binding ◽  
Interaction Position ◽  
Binding Inhibitors

Bisphenol A and its derivatives are recognized endocrine disruptors based on their complex effects on estrogen receptor (ER) signaling. While the effects of bisphenol derivatives on ERα have been thoroughly evaluated, how these chemicals affect ERβ signaling is not well understood. Herein, we identified novel ERβ ligands by screening a chemical library of bisphenol derivatives. Many of the compounds identified showed intriguing dual activities as ERα agonists and ERβ antagonists. Docking simulations suggested that these compounds act as coactivator binding inhibitors (CBIs). Direct binding experiments using wild-type and mutated ERβ demonstrated the presence of a second ligand interaction position at the coactivator binding site in ERβ. Our study is the first to propose that bisphenol derivatives act as CBIs, presenting a critical view point for future ER signaling-based drug development.

scholarly journals Bisphenol A derivatives act as novel coactivator binding inhibitors for estrogen receptor β

2021 ◽  
pp. 101173
Author(s):  
Masaki Iwamoto ◽  
Takahiro Masuya ◽  
Mari Hosose ◽  
Koki Tagawa ◽  
Tomoka Ishibashi ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Bisphenol A ◽  
Estrogen Receptor Β ◽  
Coactivator Binding Inhibitors ◽  
Binding Inhibitors

1322: The Expression of Estrogen Receptor α and Estrogen Receptor β in the Human Fetal Prostate

2004 ◽  
Vol 171 (4S) ◽  
pp. 348-348
Author(s):  
Ellen Shapiro ◽  
Hongying Huang ◽  
Rachael R. Mash ◽  
Eliza Ng ◽  
Deborah E. McFadden ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Α ◽  
Estrogen Receptor Β
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