Exploring the state- and allele-specific conformational landscapes of Ras: understanding their respective druggabilities.

Abstract excerpt

Recent advances in direct inhibition of Ras benefit from the protein's intrinsic dynamic nature that derives therapeutically vulnerable conformers bearing transiently formed cryptic pockets. Hotspot mutants of Ras are major tumor drivers and are hyperactivated in cells at variable levels, which may require allele-specific strategies for effective targeting. However, it remains unclear how the prevalent oncogenic...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to Alleles
• Share to Magnetic Resonance Spectroscopy