This federal Project Grant award from the National Cancer Institute (CFDA 93.395 - Cancer Treatment Research) to Purdue University provides $572,254 over a nearly 3-year period (2/1/2025 - 1/31/2028) to identify the first selective small molecule inhibitors of the phospholipase C gamma (PLCγ1 and PLCγ2) enzymes. The research aims to develop an HTS-amenable biochemical assay using novel fluorescent substrates and screen a 200,000 compound library to find potent, specific inhibitors of these enzymes, which have been implicated in driving oncogenesis. Confirmed hit compounds will undergo further validation and structure-activity relationship studies to determine a path for developing them into useful chemical probes or potential therapeutic leads. The overarching goal is to provide new targeted therapeutic options for a variety of cancer types where PLCγ dysfunction is a driver.
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