GPR40: a therapeutic target for mediating insulin secretion (review)

Int J Mol Med. 2012 Dec;30(6):1261-6. doi: 10.3892/ijmm.2012.1142. Epub 2012 Sep 26.

Abstract

G-protein-coupled receptor 40 (GPR40), known as free fatty acid receptor 1, is mainly expressed in pancreatic β-cells and activated by medium- and long-chain fatty acids. Increasing evidence indicates that the activation of GPR40 in cells causes insulin secretion, and GPR40 has become an attractive therapeutic target for type 2 diabetes. Recently, certain novel GPR40 agonists have been identified that regulate glucose-stimulated insulin secretion, leading to the development of new drugs for the treatment of type 2 diabetes. In this review, we focus on progress in the physiological role of GPR40 and potential drugs targeting GPR40 over the past decade.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Benzofurans / pharmacology
  • Berberine / pharmacology
  • Clinical Trials, Phase II as Topic
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Fatty Acids, Nonesterified / physiology
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Insulin / metabolism*
  • Insulin Secretion
  • Ligands
  • Molecular Targeted Therapy
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / physiology*
  • Sulfones / pharmacology

Substances

  • Benzofurans
  • FFAR1 protein, human
  • Fatty Acids, Nonesterified
  • Hypoglycemic Agents
  • Insulin
  • Ligands
  • Receptors, G-Protein-Coupled
  • Sulfones
  • TAK-875
  • Berberine