In vitro screen for inhibitors of the inositol kinases ITPK1 and PPIP5K

National Center For Advancing Translational Sciences

Investigators

Abstract

Recent publications have suggested that two members of the inositol kinase family, ITPK1 and PPIP5K, are implicated to play important roles in cancer. ITPK1 has been shown to be involved in cell migration, and PPIP5K has been identified as controlling cancer cell metabolism and tumor growth, in addition to general roles in cellular energy sensing. These observations suggest that both inositol kinases may be potential drug targets for cancer and other diseases. Yet to date, no inhibitors have been developed for these kinases. The discovery and development of small molecule inhibitors for ITPK1 and PPIP5K may lead to new insight into the pharmacophore space of these enzymes and improve rational inhibitor design. During this period, the collaborative team devised a research plan and began optimizing and miniaturizing high-throughput amenable assays to enable initial screening against these two targets.