title: Physiology and therapeutics of the free fatty acid receptor GPR40.
abstract: The G protein-coupled receptor 40 (GPR40) was deorphanized in 2003 as a receptor of medium- and long-chain free fatty acids (FFAs), now also called FFA receptor 1 (FFAR1). Studies have shown that GPR40 not only directly mediates FFA amplification of glucose-stimulated insulin secretion but also indirectly enhances insulin secretion by stimulating incretin release. Therefore, GPR40 has attracted considerable attention as a therapeutic drug target of type 2 diabetes mellitus, and numerous GPR40 ligands have been developed and investigated for their antidiabetic actions. Recently, one of these ligands, TAK-875, has been successfully tested in phase II clinical trials with reduced risk of hypoglycemia. This chapter will summarize studies on GPR40, including its molecular cloning and tissue distribution, physiology, pharmacology, and pathophysiology.
authors.affiliation: Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama, USA.
authors.forename: Hui
authors.initials: H
authors.lastname: Huang
authors.affiliation: Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama, USA; Department of Basic Veterinary Medicine, College of Veterinary Medicine, Huazhong Agricultural University, Wuhan, Hubei, China.
authors.forename: Meng-Hong
authors.initials: MH
authors.lastname: Dai
authors.affiliation: Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, Alabama, USA.
authors.forename: Ya-Xiong
authors.initials: YX
authors.lastname: Tao
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D005230:Fatty Acids, Nonesterified / Q000378:metabolism*; D020869:Gene Expression Profiling; D006801:Humans; D008969:Molecular Sequence Data; D058990:Molecular Targeted Therapy; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D005230:Fatty Acids, Nonesterified; D043562:Receptors, G-Protein-Coupled
keywords: FFA; GPCR; GPR40; T2DM