Structure–activity relationships of bisphenol A analogs at estrogen receptors (ERs): Discovery of an ERα-selective antagonist

K Maruyama, M Nakamura, S Tomoshige…

Index: Maruyama, Keisuke; Nakamura, Masaharu; Tomoshige, Shusuke; Sugita, Kazuyuki; Makishima, Makoto; Hashimoto, Yuichi; Ishikawa, Minoru Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 14 p. 4031 - 4036

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Citation Number: 17

Abstract

Our multi-template approach for drug discovery, focusing on protein targets with similar fold structures, has yielded lead compounds for various targets. We have also shown that a diphenylmethane skeleton can serve as a surrogate for a steroid skeleton. Here, on the basis of those ideas, we hypothesized that the diphenylmethane derivative bisphenol A (BPA) would bind to the ligand-binding domain of estrogen receptors (ERs) in a similar ...