Description
Deltarasin inhibits PDEδ at the farnesyl binding pocket, preventing its association with K-Ras. Deltarasin displays anticancer chemotherapeutic activity, inhibiting cell proliferation in cellular and animal models of pancreatic ductal adenocarcinoma.
References
Zimmermann G, Schultz-Fademrecht C, Küchler P, et al. Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site. J Med Chem. 2014 Jun 26;57(12):5435-48. PMID: 24884780.
Zimmermann G, Papke B, Ismail S, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42. PMID: 23698361.