Journal
NATURE CHEMICAL BIOLOGY
Volume 18, Issue 6, Pages 578-579Publisher
NATURE PORTFOLIO
DOI: 10.1038/s41589-022-01000-y
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This study demonstrates that optimizing non-covalent interactions with a cryptic pocket can significantly enhance the potency for another hotspot mutation.
Despite well-established tumorigenic roles of KRAS mutants, targeting their smooth surfaces was a challenge, which was overcome through the development of G12C-specific covalent inhibitors. A new study shows that optimizing non-covalent interactions with a cryptic pocket produces remarkable potency for another hotspot mutation.
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