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Article

A Nonconserved Histidine Residue on KRAS Drives Paralog Selectivity of the KRASG12D Inhibitor MRTX1133.

Cancer research - 1 Sept 2023

Keats Miles A, Han John J W, Lee Yeon-Hwa, Lee Chih-Shia, Luo Ji

Abstract excerpt

MRTX1133 is the first noncovalent inhibitor against the KRASG12D mutant that demonstrated specificity and potency in preclinical tumor models. Here, we used isogenic cell lines expressing a single RAS allele to evaluate the selectivity of this compound. In addition to KRASG12D, MRTX1133 showed significant activity against several other KRAS mutants as well as wild-type KRAS protein. In contrast, MRTX1133...

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Identifiers

PMID: 37339170
DOI: 10.1158/0008-5472.CAN-23-0592
PMCID: PMC10528543

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