Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases

Trends Pharmacol Sci. 2011 Sep;32(9):543-50. doi: 10.1016/ Epub 2011 Jun 12.


The past decade has seen great progress in the understanding of the molecular pharmacology, physiological function and therapeutic potential of G-protein-coupled receptors (GPCRs). Free fatty acids (FFAs) have been demonstrated to act as ligands of several GPCRs including GPR40, GPR43, GPR84, GPR119 and GPR120. We have recently shown that GPR120 acts as a physiological receptor of ω3 fatty acids in macrophages and adipocytes, which mediate potent anti-inflammatory and insulin sensitizing effects. The important role GPR120 plays in the control of inflammation raises the possibility that targeting this receptor could have therapeutic potential in many inflammatory diseases including obesity and type 2 diabetes. In this review paper, we discuss lipid-sensing GPCRs and highlight potential outcomes of targeting such receptors in ameliorating disease.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / physiopathology
  • Drug Delivery Systems
  • Fatty Acids, Nonesterified / metabolism
  • Humans
  • Inflammation / drug therapy
  • Inflammation / physiopathology*
  • Insulin Resistance*
  • Ligands
  • Obesity / drug therapy
  • Obesity / physiopathology
  • Receptors, G-Protein-Coupled / metabolism*


  • FFAR4 protein, human
  • Fatty Acids, Nonesterified
  • Ligands
  • Receptors, G-Protein-Coupled