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Article

Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile.

Journal of the American Chemical Society - 7 Sept 2022

Zhang Ziyang, Morstein Johannes, Ecker Andrew K, Guiley Keelan Z, Shokat Kevan M

Abstract excerpt

KRAS mutations are one of the most common oncogenic drivers in human cancer. While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutants remains challenging. Here we report the discovery of covalent chemical ligands for the common oncogenic mutant K-Ras(G12R). These ligands bind in the Switch II pocket and irreversibly react with...

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Identifiers

PMID: 36001446
DOI: 10.1021/jacs.2c05377
PMCID: PMC9460778

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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