Free Fatty Acid Receptors and Their Physiological Role in Metabolic Regulation

  • HIRASAWA Akira
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University
  • HARA Takafumi
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University
  • ICHIMURA Atsuhiko
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University
  • TSUJIMOTO Gozoh
    Department of Genomic Drug Discovery Science, Graduate School of Pharmaceutical Sciences, Kyoto University

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Other Title
  • 消化管脂肪酸受容体とその生理作用
  • ショウカカン シボウサン ジュヨウタイ ト ソノ セイリ サヨウ

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Abstract

  Free fatty acids (FFAs) are not only essential nutrient components, but they also function as signaling molecules in various physiological processes. In the progression of genomic analysis, many orphan G-protein coupled receptors (GPCRs) are found. Recently, GPCRs deorphanizing strategy successfully identified multiple receptors for FFAs. In these FFA receptors (FFARs), GPR40 (FFAR1) and GPR120 are activated by medium- to long- chain FFAs. GPR40 is expressed mainly in pancreatic β-cell and mediates insulin secretion, whereas GPR120 is expressed abundantly in the intestine and regulates the secretion of cholecystokinin (CCK) and glucagons-like peptide-1 (GLP-1), it promotes insulin secretion. Due to these biological activity, GPR40 and GPR120 are potential drug target for type 2 diabetes and selective ligands have been developed. In this review, we provide recent development in the field and discuss their physiological roles and their potential as drug targets.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 131 (12), 1683-1689, 2011-12-01

    The Pharmaceutical Society of Japan

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