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 Global Ligandability Map of Tryptoline Butynamide Stereoprobes Identifies Covalent Inhibitors of the Actin Maturation Protease ACTMAP

Yijun Xiong, Christopher J. Reinhardt, Tracey Nguyen, Melissa A. Hoffman, Gabriel M. Simon, Bruno Melillo, Benjamin F. Cravatt bioRxiv , 202...