Free Fatty Acid Receptors and Drug Discovery

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Author(s)

    • ADACHI Tetsuya
    • Department of Genomic Drug Discovery Science, Kyoto University Graduate School of Pharmaceutical Sciences
    • TSUJIMOTO Gozoh
    • Department of Genomic Drug Discovery Science, Kyoto University Graduate School of Pharmaceutical Sciences

Abstract

Utilizing the human genome database, the recently developed G-protein-coupled receptor (GPCR) deorphanizing strategy successfully identified multiple receptors of free fatty acids (FFAs) and is proposed to play a critical role in a variety of physiologic homeostasis mechanisms. GPR40 and GPR120 are activated by medium- and long-chain FFAs, whereas GPR41 and GPR43 are activated by short-chain FFAs. GPR40, which is preferentially expressed in pancreatic β-cells, mediates insulin secretion. On the other hand, GPR120, which is abundantly expressed in the intestine, functions as a receptor for unsaturated long-chain FFAs and promotes the secretion of glucagon-like peptide-1 (GLP-1). In this review, we summarize the identification, structure, and pharmacology of the receptors and speculate on the respective physiologic roles that FFA receptor family members may play.

Journal

  • Biological and Pharmaceutical Bulletin

    Biological and Pharmaceutical Bulletin 31(10), 1847-1851, 2008-10-01

    The Pharmaceutical Society of Japan

References:  41

Cited by:  4

Codes

  • NII Article ID (NAID)
    110006936320
  • NII NACSIS-CAT ID (NCID)
    AA10885497
  • Text Lang
    ENG
  • Article Type
    Journal Article
  • ISSN
    09186158
  • NDL Article ID
    9655255
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-V41
  • Data Source
    CJP  CJPref  NDL  NII-ELS  J-STAGE 
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