Hitting the hotspots

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.

Automated summary

This study demonstrates that optimizing non-covalent interactions with a cryptic pocket can significantly enhance the potency for another hotspot mutation.