Article
Somatic estrogen receptor α mutations that induce dimerization promote receptor activity and breast cancer proliferation.
The Journal of clinical investigation - 2 Jan 2024
Irani Seema, Tan Wuwei, Li Qing, Toy Weiyi, Jones Catherine, Gadiya Mayur, Marra Antonio, Katzenellenbogen John A, Carlson Kathryn E, Katzenellenbogen Benita S, Karimi Mostafa, Segu Rajappachetty Ramya, Del Priore Isabella S, Reis-Filho Jorge S, Shen Yang, Chandarlapaty Sarat
Abstract excerpt
Physiologic activation of estrogen receptor α (ERα) is mediated by estradiol (E2) binding in the ligand-binding pocket of the receptor, repositioning helix 12 (H12) to facilitate binding of coactivator proteins in the unoccupied coactivator binding groove. In breast cancer, activation of ERα is often observed through point mutations that lead to the same H12 repositioning in the absence of E2. Through expanded...
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