Article
Oncogenic KRAS G12C: Kinetic and redox characterization of covalent inhibition.
The Journal of biological chemistry - 1 Aug 2022
Huynh Minh V, Parsonage Derek, Forshaw Tom E, Chirasani Venkat R, Hobbs G Aaron, Wu Hanzhi, Lee Jingyun, Furdui Cristina M, Poole Leslie B, Campbell Sharon L
Abstract excerpt
The recent development of mutant-selective inhibitors for the oncogenic KRASG12C allele has generated considerable excitement. These inhibitors covalently engage the mutant C12 thiol located within the phosphoryl binding loop of RAS, locking the KRASG12C protein in an inactive state. While clinical trials of these inhibitors have been promising, mechanistic questions regarding the reactivity of this thiol remain....
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