Article

A non-conserved histidine residue on KRAS drives paralog selectivity of the KRAS G12D inhibitor MRTX1133

2022-12-19

Abstract excerpt

The discovery of small molecule inhibitors against mutant KRAS protein was a recent breakthrough in targeted therapy. Understanding the mechanism of selectivity by KRAS inhibitors and the mechanism of resistance to them can guide the future development of KRAS inhibitors. MRTX1133 was the first non-covalent inhibitor against the KRAS G12D mutant that demonstrated specificity and potency in pre-clinical tumor model...

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Literature Corpus work: 9c82979f-b324-5010-8668-2774e7ad6ad7
DOI: 10.1101/2022.12.16.520846

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