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Free Fatty Acid Receptor (FFAR)

Free fatty acid receptor (FFAR) ligands act on G protein-coupled receptors (GPCRs) that sense fatty acids. FFAR1 and FFAR4, also called G protein-coupled receptors 40 and 120 (GPR40, GPR120), respond to medium- and long-chain fatty acids. FFAR2 and FFAR3 are GPCRs that instead bind short-chain fatty acids produced by gut bacteria. In 2003 GPR40 was shown to mediate fatty acid-stimulated insulin secretion from pancreatic beta cells. Two years later, GPR120 was linked to fatty acid-induced secretion of glucagon-like peptide 1 (GLP-1) in the gut. Fasiglifam, TUG-770 and LY2922470 are FFAR1 agonists, and GW-1100 is an FFAR1 antagonist. TUG-891 is an FFAR4 agonist, whereas GW9508 acts on both FFAR1 and FFAR4.

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