Article

KRAS G12D can be targeted by potent salt-bridge forming inhibitors

2021-12-14

Abstract excerpt

KRAS mutation occurs in nearly 30% of human cancers, yet the most prevalent and oncogenic KRAS mutation (G12D) still lacks inhibitors. Herein, we explored the formation of a salt-bridge between KRAS’s Asp12 residue and a series of potent inhibitors. Our ITC results show that these inhibitors bind to and inhibit both GDP-bound and GTP-bound KRAS G12D, and our crystallographic studies revealed the structural basis o...

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Literature Corpus work: 286ef437-f26a-5036-916e-8a0bbfa1568c
DOI: 10.1101/2021.12.13.472365

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