4.6 Article

Oncogenic KRAS G12C: Kinetic and redox characterization of covalent inhibition

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

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Summary: KRAS(G12D), the most common oncogenic KRAS mutation, is a promising target for solid tumor treatment. Selective inhibition of KRAS(G12C) presents a significant challenge due to the requirement of high affinity inhibitors to bind the mutant protein. The discovery of the noncovalent, potent, and selective KRAS(G12C) inhibitor MRTX1133, shown to be efficacious in a mouse tumor model, represents a significant advancement in the field.

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