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Published online before print December 1, 2008

0031-6997/08/6004-405-417$7.00
Pharmacol Rev 60:405-417, 2008

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IUPHAR Nomenclature Report

International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1, -2, and -3: Pharmacology and Pathophysiological Functions

Leigh A. Stoddart, Nicola J. Smith and Graeme Milligan

Molecular Pharmacology Group, Neuroscience and Molecular Pharmacology, Faculty of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom

Abstract
I. Introduction
II. Cloning of cDNA for Free Fatty Acid Receptors 1, 2, and 3
III. Free Fatty Acid Receptor Structure
IV. Deorphanization of Free Fatty Acid Receptors and Modes of Signal Transduction
    A. Free Fatty Acid Receptor 1
    B. Free Fatty Acid Receptors 2 and 3
V. Tissue Distribution of Free Fatty Acid Receptors
    A. Tissue Distribution of Free Fatty Acid Receptor 1
    B. Tissue Distribution of Free Fatty Acid Receptor 2
    C. Tissue Distribution of Free Fatty Acid Receptor 3
VI. Free Fatty Acid Receptor 1 Synthetic Agonists and Antagonists
VII. Molecular Basis of Free Fatty Acid Receptor 1 Activation
VIII. Physiological Roles of Free Fatty Acid Receptors
    A. Pancreatic Role of Free Fatty Acid Receptor 1
    B. Other Potential Roles of Free Fatty Acid Receptor 1
    C. Potential Roles of Free Fatty Acid Receptors 2 and 3
IX. Conclusions
Identification of G protein-coupled receptors that are activated by free fatty acids has led to considerable interest in their pharmacology and function because of the wide range of normal physiology and disease states in which fatty acids have been implicated. Free fatty acid receptor (FFA) 1 is activated by medium- to long-chain fatty acids and is expressed in the insulin-producing β-cells of the pancreas. Activation of FFA1 has been proposed to mediate fatty acid augmentation of glucose-stimulated insulin secretion although it is unclear whether the known long-term detrimental effects of β-cell exposure to high levels of fatty acids are also mediated through this receptor. The related receptors FFA2 and FFA3 are both activated by short-chain fatty acids although they have key differences in the signaling pathways they activate and tissue expression pattern. The aim of this review is to provide a comprehensive overview of the current understanding of the pharmacology and physiological role of these fatty acid receptors.

Address correspondence to: Dr. Leigh A. Stoddart, Lab 253, Wolfson Building, University of Glasgow, University Avenue, Glasgow G12 8QQ, Scotland, UK. E-mail: l.stoddart.1{at}research.gla.ac.uk




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