Abstract
In the past decade, a strategy to deorphanize G protein-coupled receptors (GPCRs) has identified a series of receptors for free fatty acids (FFAs) that play significant roles in nutrition regulation. In this free fatty acid receptor family, FFAR1 (GPR40) and FFAR4 (GPR120) are activated by medium- and long-chain FFAs. FFAR1 regulates insulin secretion in pancreatic β-cells, whereas FFAR4 promotes the secretion of glucagon-like peptide-1 (GLP-1) in the intestine and also act as the lipid sensor in the adipose tissue to sense dietary fat and control energy balance. In this chapter, we discuss recent advances in the identification of ligands and the pharmacological characterization of FFAR1 and FFAR4, and we present a summary of the current understanding of their physiological roles and potential as drug targets.
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