Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity

Chen, ZX; Hu, B; Rej, RK; Wu, DM; Acharyya, RK; Wang, ML; Xu, TF; Lu, JF; Metwally, H; Wang, Y; Mceachern, D; Bai, LC; Gersch, CL; Wang, ML; Zhang, WJ; Li, QX; Wen, B; Sun, DX; Rae, JM; Wang, SM

Wang, SM (通讯作者)，Univ Michigan, Dept Internal Med, Div Hematol Oncol, Ann Arbor, MI 48109 USA.;Wang, SM (通讯作者)，Univ Michigan, Rogel Canc Ctr, Ann Arbor, MI 48109 USA.;Wang, SM (通讯作者)，Univ Michigan, Coll Pharm, Dept Med Chem, Dept Pharmacol, Ann Arbor, MI 48109 USA.

JOURNAL OF MEDICINAL CHEMISTRY, 2023; 66 (17): 12559

Abstract

Estrogen receptor a (ERa) is a prime target for the treatment of ER-positive (ER+) breast cancer. Despite the development of several effective therapi......

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