Identification of Inhibitors of the Lipid Kinase PI5P4Ka/B as Potential Anti-Cancer Agents

National Center For Advancing Translational Sciences

Investigators

Abstract

This previous collaborative team - composed of groups from Weill Cornell Medical College, Harvard Medical School and the Dana Farber Cancer Institute and NCATS - had uncovered novel inhibitors of the lipid kinase PI5P4Ka/ as potential anti-cancer agents indications. After an extensive SAR campaign against PI5P4Ka and b, Brooke Emerling at Sanford Burnham showed that a key dual PI5P4Ka/b inhibitor can kill p53 mutant cancer cells under condition where autophagy is upregulated. This has led to a CBC funded SAR campaign on the same series and other possible series that use structure based drug design to develop bioavailable dual inhibitors of PI5P4K alpha and beta in collaboration with SBP.