PPARs: therapeutic targets for metabolic disease

Trends Pharmacol Sci. 2005 May;26(5):244-51. doi: 10.1016/j.tips.2005.03.003.


The three peroxisome-proliferator-activated receptor (PPAR) subtypes, PPAR-gamma, PPAR-alpha and PPAR-delta, are nuclear receptors that have been the focus of extensive research during the past decade. These receptors function as lipid sensors that coordinately regulate the expression of large gene arrays and, thereby, modulate important metabolic events. They are also the targets of drugs that are effective in the treatment of metabolic disorders (type 2 diabetes mellitus and atherosclerosis) that afflict industrialized societies at epidemic levels. Ongoing research indicates that modulation of PPAR activity might be an effective therapy for additional maladies associated with the metabolic syndrome, including obesity. Novel PPAR ligands are now being developed that possess broader efficacies and improved tolerability compared with currently available therapeutic agents.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Ligands
  • Lipid Metabolism
  • Metabolic Diseases / drug therapy*
  • Metabolic Diseases / metabolism
  • Peroxisome Proliferator-Activated Receptors / genetics
  • Peroxisome Proliferator-Activated Receptors / metabolism*


  • Ligands
  • Peroxisome Proliferator-Activated Receptors