Covalent Chemical Inhibitors Of The Oncoprotein K-Ras (G12R)

Value Proposition

KRAS mutations are one of the most common oncogenic drivers in human cancer. While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutant remain challenging. One of such oncogenic mutants is K-Ras (G12R), with estimated >9000 cancer patients/year in the US who have this KRAS mutation (~17% of pancreatic cancer).

Technology Description

UCSF investigators have discovered covalent chemical ligands (small molecules) for the common oncogenic mutant K-Ras (G12R). Further development and testing of the covalent chemical ligands is underway.

Related Materials

• Zhang, Z., Morstein, J., Ecker, A. K., Guiley, K. Z., & Shokat, K. M. (2022). Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile. Journal of the American Chemical Society, 144(35), 15916–15921.

Patent Status

Additional Patents Pending