Bisphenol A derivatives act as novel coactivator-binding inhibitors for estrogen receptor β.

ABSTRACT: Bisphenol A and its derivatives are recognized as 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 less well understood. Herein, we sought to identify novel ERβ ligands using a radioligand competitive binding assay to screen a chemical library of bisphenol derivatives. Many of the compounds identified showed intriguing dual activities as both ERα agonists and ERβ antagonists. Docking simulations of these compounds and ERβ suggested that they bound not only to the canonical binding site of ERβ but also to the coactivator binding site located on the surface of the receptor, suggesting that they act as coactivator-binding inhibit

SUBMITTER: Iwamoto M 

PROVIDER: S-EPMC8551653 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature