Gangling Liao, Wenjuan Ye, Tyler Heitmann, Glen Ernst, Michael DePasquale, Laiyi Xu, Michael Wormald, Xin Hu, Marc Ferrer, Robert K Harmel, Dorothea Fiedler, James Barrow, Huijun Wei
Inositol hexakisphosphate kinases (IP6Ks) catalyze pyrophosphorylation of inositol hexakisphosphate (IP6) into inositol 5-diphospho-1,2,3,4,6-pentakisphosphate (IP7), which is involved in numerous areas of cell physiology including glucose homeostasis, blood coagulation, and neurological development. Inhibition of IP6Ks may be effective for the treatment of Type II diabetes, obesity, metabolic complications, thrombosis, and psychiatric disorders. We performed a high-throughput screen (HTS) of 158 410 compounds for IP6K1 inhibitors using a previously developed ADP-Glo Max assay...
April 9, 2021: ACS Pharmacology & Translational Science