Tuesday, July 30, 2024

Direct RAS inhibitors turn 10

 Ostrem, J.M.L., Peters, U. & Shokat, K.M

 Nat Chem Biol (2024). 

https://doi.org/10.1038/s41589-024-01691-5

RAS proteins, central drivers of cancer, appeared ‘undruggable’ for almost 30 years. Here we provide a personal perspective on the effort leading to our initial report of KRASG12C inhibitors in 2013, and the decade of discoveries that followed.



Direct RAS inhibitors turn 10

A Tandem Bioorthogonal Retro-Cope and Cope Elimination for the Activation of Covalent Inhibitors with an Acrylamide or Vinylsulfonamide Warhead in Live Cells

Yan Huang, Miao Liu, Dongguang Fan, Fan Xu, Fushuang Xiang, Qingqiang Min, and Xingyue Ji Journal of the American Chemical Society 2026 DOI:...