4 minute read
Sep. 28, 2022

An Arginine-Targeting Covalent Strategy for KRAS(G12R)

compound 3

KRAS G12R mutant-selective covalent inhibitor privileged arginine-reactive functional group from previously disclosed KRAS inhibitors J. Am. Chem. Soc. University of California San Francisco, San Francisco, CA

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Drug Hunter Team
Reviewer:  

“ Compound 3 ” (UCSF) is a covalent KRAS G12R inhibitor used as a proof-of-concept for covalent arginine modification. KRAS is the first oncoprotein to be identified and is a well-known cancer-driving protein. As one of the most frequently mutated proteins in pancreatic and colorectal cancers, residues that are frequently mutated are [...]

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