Figure 1. Approaches to discover and develop pharmacologic inhibitors of mutant Ras.
Past and ongoing approaches to inhibitors of mutationally activated Ras include Ras-binding small molecules that disrupt a key function(s) of Ras, inhibition of the CAAX motif-targeted enzymes that promote Ras membrane association, inhibitors of effector signalling function, unbiased interfering RNA, genetic or chemical screens for synthetic lethal interactors and inhibitors of metabolism.