Novel FFA3 Antagonist Development for Type 2 Diabetes

Type of Award: accelerator
Award Number: A-004
Award Period: July 2018 - June 2019
Amount Awarded: $ 100,000.00
PI(s): Brian Layden, UIC;

Abstract: New approaches to treat type 2 diabetes (T2D) are needed. We have shown that the free fatty acid receptor-3 (FFA3) mediates insulin secretion, an important mechanism in the adaption of pancreatic beta (β) cells to insulin resistance. We also have shown that FFA3 signaling negatively mediates glucose stimulated insulin secretion (GSIS) using a variety of genetic and pharmacological methods, collectively suggesting that receptor antagonists will be useful as potential T2D therapeutics. In this proposal, we will carry out a high-throughput screen of a drug- like small molecule library to identify novel FFA3 antagonists. These hits will be thoroughly validated in a series of secondary assays to demonstrate their potential as FFA3-directed T2D agents amenable for further lead optimization. Future work will develop these hits into lead compounds that are suitable for pre-clinical and clinical studies.