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Ace-ylation in the hole

Mutant-selective KRAS-targeting drugs hold great promise for the treatment of some of the most aggressive forms of cancer. Building on the breakthrough success of KRAS-G12C inhibitors, researchers have now found a way to target another mutant KRAS with serine-modifying covalent inhibitors.

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Fig. 1: Targeting KRAS-G12S with covalent inhibitors that react with a non-catalytic serine.


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Correspondence to Micah J. Niphakis or Benjamin F. Cravatt.

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J. Niphakis, M., F. Cravatt, B. Ace-ylation in the hole. Nat Chem Biol (2022).

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