Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile
Covalent Modifiers
NOVEMBER 26, 2023
While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutants remains challenging. An X-ray crystal structure reveals an imidazolium condensation product formed between the α,β-diketoamide ligand and the ε- and η-nitrogens of arginine 12.
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