Peroxisome proliferator-activated receptor delta (PPARdelta), a novel target site for drug discovery in metabolic syndrome

Pharmacol Res. 2006 Jun;53(6):501-7. doi: 10.1016/j.phrs.2006.03.019. Epub 2006 Mar 29.


The development of new treatments for metabolic syndrome is urgent project for decreasing the prevalence of coronary heart disease and diabetes mellitus in the advanced countries. Peroxisome proliferator-activated receptor (PPAR)alpha and gamma agonists have shed light on the treatment of hypertriglyceridemia and type 2 diabetes mellitus, respectively. Among PPARs, analysis of the PPARdelta functions is lagging behind because specific PPARdelta agonists have not been developed. The appearance of new PPARdelta agonists is brightening the prospects for elucidating the physiological role of PPARdelta. PPARdelta is a new target for the treatment of metabolic syndrome. In particular, the fact that fatty acid oxidation and energy dissipation in skeletal muscle and adipose tissue by PPARdelta agonists lead to improved lipid profile, reduced adiposity and insulin sensitivity is a breakthrough. It seems that treatment of PPARdelta agonists operate similarly to the caloric restriction and prolonged exercise. We suggest that the physiological role of PPARdelta may be an indicator for switching from glucose metabolism to fatty acid metabolism. To receive new benefits of PPARdelta agonists against metabolic syndrome by increasing fatty acid consumption in skeletal muscle and adipose tissue, we need to unveil more details on the functions of PPARdelta itself and its agonists in the future.

Publication types

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

MeSH terms

  • Adipocytes / cytology
  • Adipocytes / metabolism
  • Animals
  • Atherosclerosis / prevention & control
  • Cell Differentiation
  • Drug Design*
  • Fatty Acids / metabolism
  • Humans
  • Lipoproteins / metabolism
  • Metabolic Syndrome / drug therapy*
  • Mice
  • Muscle, Skeletal / metabolism
  • Myocytes, Cardiac / drug effects
  • Oxidation-Reduction
  • PPAR delta / agonists*
  • PPAR delta / physiology


  • Fatty Acids
  • Lipoproteins
  • PPAR delta