title: [Free Fatty Acid Receptor Family: A New Therapeutic Target for Metabolic Diseases].
abstract: Free fatty acids (FFAs) are not only essential nutritional components but they also act as signaling molecules in various physiological processes. A strategy to deorphanize G-protein-coupled receptors (GPCRs) identified a series of receptors for FFAs that play significant roles in nutrition regulation. In this free fatty acid receptor family, FFAR1 (GPR40) and FFAR4 (GPR120) are activated by 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 acts as a lipid sensor in adipose tissue to sense dietary fat and control energy balance. In this review, we discuss recent advances in the pharmacological characterization of FFAR1 and FFAR4, and we present a summary of current understandings of their physiological roles and their potential as drug targets.
authors.affiliation: Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Science, Kyoto University; 46-29 Yoshida-Shimo-Adachi-cho, Sakyo-ku, Kyoto 606-8501; 2) Inistitute for Integrated Medical Scinces, Tokyo Women's Medical University; 8-1 Kawada-cho, Shinjuku-ku, Tokyo 162-8666, Japan.
authors.forename: Akira
authors.initials: A
authors.lastname: Hirasawa
mesh_terms: D000273:Adipose Tissue / Q000378:metabolism; D004041:Dietary Fats / Q000378:metabolism; D055808:Drug Discovery / Q000639:trends*; D004734:Energy Metabolism / Q000235:genetics; D005230:Fatty Acids, Nonesterified / Q000378:metabolism*; D052216:Glucagon-Like Peptide 1 / Q000378:metabolism; D006801:Humans; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000378:metabolism; D007413:Intestinal Mucosa / Q000378:metabolism; D050356:Lipid Metabolism; D009747:Nutritional Physiological Phenomena / Q000235:genetics; D043562:Receptors, G-Protein-Coupled / Q000502:physiology*
chemical_list: D004041:Dietary Fats; C473034:FFAR1 protein, human; C519853:FFAR4 protein, human; D005230:Fatty Acids, Nonesterified; D007328:Insulin; D043562:Receptors, G-Protein-Coupled; D052216:Glucagon-Like Peptide 1