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

Covalent Inhibitors of Monoacylglycerol Lipase Induce Conformational Changes and Proteasomal Degradation

Jordan A. Pham, Thanawat Thaingtamtanha, William McLeish, David Lefebvre, Spencer M. Uguccioni, Roxana Filip, Francesco Gentile, and John Pa...