Article

Strain-release alkylation of Asp12 enables mutant selective GTP-state targeting of K-Ras(G12D)

2023-07-02

Abstract excerpt

K-Ras is the most commonly mutated oncogene in human cancer, yet direct small-molecule targeting of K-Ras mutants has been mostly unsuccessful until recently. The discovery of an allosteric pocket under Switch-II with covalent cysteine-crosslinking molecules has allowed for the development of targeted therapies that selectively engage the highly reactive acquired cysteine in the K-Ras(G12C) mutation without affect...

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Literature Corpus work: e941205c-6b83-5719-85e2-7d488ce24901
DOI: 10.1101/2023.07.01.547359

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