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Article

Biophysical and structural analysis of KRAS switch-II pocket inhibitors reveals allele-specific binding constraints.

The Journal of biological chemistry - 1 Jul 2025

Alexander Patrick, Chan Albert H, Rabara Dana, Swain Monalisa, Larsen Erik K, Dyba Marcin, Chertov Oleg, Ashraf Mariam, Champagne Allison, Lin Ken, Maciag Anna, Gillette William K, Nissley Dwight V, McCormick Frank, Simanshu Dhirendra K, Stephen Andrew G

Abstract excerpt

RAS mutations are observed in 20% of all cancers, with the KRAS isoform highly mutated in colorectal, lung and pancreatic cancers. The last several years have seen the development of clinical compounds that target KRAS G12C mutations, with other compounds under clinical development. In this study, a series of KRAS small-molecule inhibitors were compared for their binding affinity against a panel of KRAS mutant...

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Identifiers

PMID: 40473215
DOI: 10.1016/j.jbc.2025.110331
PMCID: PMC12270674

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KRAS

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