Free fatty acid receptors act as nutrient sensors to regulate energy homeostasis

被引:148
|
作者
Ichimura, Atsuhiko [1 ]
Hirasawa, Akira [1 ]
Hara, Takafumi [1 ]
Tsujimoto, Gozoh [1 ]
机构
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Dept Genom Drug Discovery Sci, Sakyo Ku, Kyoto 6068501, Japan
关键词
G-protein-coupled receptor; Free fatty acid; Insulin; FFAR1; FFAR2; FFAR3; GPR120; PROTEIN-COUPLED-RECEPTOR; STIMULATED INSULIN-SECRETION; PANCREATIC BETA-CELLS; CHOLECYSTOKININ SECRETION; GPR40; FFAR1; RAT; ACTIVATION; AGONISTS; GPR120; IDENTIFICATION;
D O I
10.1016/j.prostaglandins.2009.05.003
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Free fatty acids (FFAs) have been demonstrated to act as ligands of several G-protein-coupled receptors (GPCRs) (FFAR1, FFAR2, FFAR3, GPR84, and GPR120). These fatty acid receptors are proposed to play critical roles in a variety of types of physiological homeostasis. FFAR1 and GPR120 are activated by medium- and long-chain FFAs. GPR84 is activated by medium-chain, but not long-chain, FFAs. In contrast, FFAR2 and FFAR3 are activated by short-chain FFAs. FFAR1 is expressed mainly in pancreatic beta-cells and mediates insulin secretion, whereas GPR120 is expressed abundantly in the intestine and promotes the secretion of glucagon-like peptide-1 (GLP-1). FFAR3 is expressed in enteroendocrine cells and regulates host energy balance through effects that are dependent upon the gut microbiota. In this review, we summarize the identification, structure, and pharmacology of these receptors and present an essential overview of the current understanding of their physiological roles. (C) 2009 Elsevier Inc. All rights reserved.
引用
收藏
页码:82 / 88
页数:7
相关论文
共 50 条
  • [21] Free Fatty Acid Receptors 2 and 3 as Microbial Metabolite Sensors to Shape Host Health: Pharmacophysiological View
    Mishra, Sidharth P.
    Karunakar, Prashantha
    Taraphder, Subhash
    Yadav, Hariom
    BIOMEDICINES, 2020, 8 (06)
  • [22] Free Fatty Acid (FFA) and Hydroxy Carboxylic Acid (HCA) Receptors
    Offermanns, Stefan
    ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 54, 2014, 54 : 407 - 434
  • [23] Hypothalamic roles of mTOR complex I: integration of nutrient and hormone signals to regulate energy homeostasis
    Hu, Fang
    Xu, Yong
    Liu, Feng
    AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM, 2016, 310 (11): : E994 - E1002
  • [24] Free Fatty Acid Receptors 1 (FFAR1) and 4 (FFAR4) Regulate Fatty Acid-Stimulated AMPK Activation and Neurotensin Secretion
    Li, Jing
    Song, Jun
    Weiss, Heidi L.
    Townsend, Courtney M.
    Evers, B. Mark
    GASTROENTEROLOGY, 2016, 150 (04) : S521 - S521
  • [25] How Arrestins and GRKs Regulate the Function of Long Chain Fatty Acid Receptors
    Alharbi, Abdulrahman G.
    Tobin, Andrew B.
    Milligan, Graeme
    INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2022, 23 (20)
  • [26] Free Fatty Acid Receptors-possible markers in melanoma?
    Kleemann, J.
    Haerle, K.
    Steinhorst, K.
    Hrgovic, I.
    Ter-Nedden, J.
    Kaufmann, R.
    Kippenberger, S.
    Meissner, M.
    EXPERIMENTAL DERMATOLOGY, 2016, 25 (03) : E14 - E14
  • [27] Free Fatty Acid Receptors and Their Physiological Role in Metabolic Regulation
    Hirasawa, Akira
    Hara, Takafumi
    Ichimura, Atsuhiko
    Tsujimoto, Gozoh
    YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 2011, 131 (12): : 1683 - 1689
  • [28] Allosteric Activation of Free Fatty Acid Receptors 2 and 3
    Lamodiere, Elisabeth
    Tautermann, Christofer S.
    Bakker, Remko A.
    DIABETES, 2011, 60 : A440 - A440
  • [29] Free fatty acid receptors and their pathophysiological role in metabolic disorder
    Hirasawa, Akira
    Tsujimoto, Gozoh
    JOURNAL OF PHARMACOLOGICAL SCIENCES, 2009, 109 : 40P - 40P
  • [30] Free fatty acid receptors as therapeutic targets for the treatment of diabetes
    Ichimura, Atsuhiko
    Hasegawa, Sae
    Kasubuchi, Mayu
    Kimura, Ikuo
    FRONTIERS IN PHARMACOLOGY, 2014, 5