The critical role of Rac1 in cancer

Rac1 and its variants are proteins that function as central signaling nodes for diverse pathways that drive various cancer promoting processes including cell growth, migration, invasion, and angiogenesis. These proteins switch between the inactive guanosine diphosphate (or GDP-bound form) and the active guanosine triphosphate (or GTP-bound form). The active GTP form recruits downstream effector proteins to activate oncogenic pathways.

While GTPases in general have been elusive drug discovery targets, our proprietary methods have enabled us to discover promising inhibitors for these signaling proteins. We have developed an industry-leading suite of biochemical and cell-based assays designed for conducting research on Rho GTPases. These assays, together with computer-aided drug design, provide the foundation for a sustainable pipeline of first-in-class drugs to address unmet needs for cancer patients.