Identification of modulators of PI4K for cellular trafficking-related indications

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, the collaborative team tested hits, identified through high-throughput screening, in cell-based models of phosphatidylinositol 4-kinase 2-alpha (PI4K2a) activity. Molecular modeling studies were performed to design compounds with increased specificity relative to phosphoinositide 3-kinase (PI3K). Select chemotypes were advanced through medicinal chemistry efforts and activity was assessed using a cell-based BRET assay to measure phosphatidylinositol-4-phosphate (PI4P) generation on endosomes.