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

Structure-Guided Optimization of 4-Chloro-Pyrazolopyridine Analogs for Covalent PREP Inhibition

Kalyani Thakur, Ian Fucci, Joshua Pandian, Kiall F. Suazo, Diana C. F. Monteiro, and Euna Yoo Journal of Medicinal Chemistry 2025 DOI: 10.1...