KRAS is vulnerable to reversible switch-II pocket engagement in cells

Vasta, JD; Peacock, DM; Zheng, QH; Walker, JA; Zhang, ZY; Zimprich, CA; Thomas, MR; Beck, MT; Binkowski, BF; Corona, CR; Robers, MB; Shokat, KM

Robers, MB (通讯作者)，Promega Corp, Madison, WI 53711 USA.;Shokat, KM (通讯作者)，Univ Calif San Francisco, Howard Hughes Med Inst, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA.

NATURE CHEMICAL BIOLOGY, 2022; 18 (6): 596

Abstract

Current small-molecule inhibitors of KRAS(G12C) bind irreversibly in the switch-II pocket (SII-P), exploiting the strong nucleo-philicity of the acqui......

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