Reviving Ras

Activated Ras proteins are among the most notorious oncoproteins, but thus far they have proven undruggable. Now, teams at Roche's Genentech Inc. unit and at Vanderbilt University School of Medicine have independently used fragment-based drug discovery to identify a new small molecule binding site that blocks Ras activation.^1,2

The results could reinvigorate drug discovery efforts against the target. Remaining hurdles include developing more potent inhibitors and testing whether optimized molecules block mutant Ras-driven cancers...