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

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Project highlights: executed the screen and identified chemical series of interest. Performed medicinal chemistry optimization and validation of the compounds in orthogonal assays such as radiolabeled ATP assays. Determined the mechanism of action of the chemical series as ATP-competitive. Determined the effect of the compounds on cell viability in a variety of cancer cell lines. During this period, the NCGC has fostered and maintained over 180 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to over 100 high-throughput screens and nearly 60 medicinal chemistry campaigns, providing our collaborators and the general research community a wealth of publications and promising small molecule leads. In addition, the NCGC has undertaken a number of informatic challenges to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.