Article
Expanding Addressable KRAS Mutations through the Structure- and Property-Based Design of Dual-State (GDP/GTP), Reversible Pan-KRAS Inhibitors.
Journal of medicinal chemistry - 23 Jul 2026
Wurz Ryan P, Allen Jennifer R, Allen John G, Amegadzie Albert, Chen Ning, Eshon Josephine, Li Kexue, Li Xiaofen, Li Yunxiao, Manoni Francesco, Medina Jose M, Navaratne Primali, Pettus Liping H, Rahimoff René, Stellwagen John, Tercenio Quentin, Weires Nicholas, Wigman Benjamin, Yamano Michael, Zhao Wei, Husemoen Gitte, Leth-Petersen Sebastian, Bauer David, Frohn Mike J, Mukhina Olga A, Boursier Michelle, Vaish Amit, Poppe Leszek, Mohr Christopher, Chen Ying-Chu, Diaz Gilbert Joseph, Gaida Kevin, Hughes Paul E, Khetan Jawahar, Mohn Deanna, Osgood Tao, Saiki Anne Y, Rex Karen, Verma Rati, Wang Paul, Rui Huan, Yu Jason, Dahal Upendra P, Li Yanfei, Agarwal Prashant, Wegesser Teresa, Lanman Brian A
Abstract excerpt
Therapeutically targeting mutant KRAS represents a clinically validated approach for the treatment of solid tumors, including lung, colon, and pancreatic cancers. The approval of covalent KRASG12C inhibitors, such as sotorasib and adagrasib, has fueled intense interest in expanding KRAS-directed therapies to mutations beyond KRASG12C, such as KRASG12D, KRASG12V, and KRASG13D. Here, we describe the structure- and...
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