Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 100, Issue 9, Pages 3594-3601Publisher
WILEY
DOI: 10.1002/jps.22639
Keywords
receptors; metabolism; gastrointestinal; lipids; hormones
Funding
- Ministry of Education, Science, and Culture of Japan
- Grants-in-Aid for Scientific Research [23890019] Funding Source: KAKEN
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Free fatty acids (FFAs) are not only essential nutritional components, but they also act as signaling molecules in various physiological processes. Recently, a G-protein-coupled receptor deorphanizing strategy has successfully identified a family of receptors that are activated by FFAs. FFA receptors (FFARs) are proposed to play critical roles in a variety of physiological and pathophysiological processes, especially in metabolic disorders. Among the FFARs, FFAR1 (GPR40) and GPR120 are activated by medium-and long-chain FFAs. FFAR1 facilitates glucose-stimulated insulin secretion from pancreatic beta-cells, whereas GPR120 regulates the secretion of glucagon-like peptide-1 in the intestine, as well as insulin sensitivity in macrophages. Because these receptors are potential therapeutic targets for metabolic disorders such as type 2 diabetes, selective ligands have been developed. In this review, we discuss recent advances in the identification of ligands, structure activity relationships, and pharmacological characterization of FFAR1 and GPR120, and we present a summary of recent progress in understanding their physiological roles and their potential as drug targets. (C) 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3594-3601, 2011
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