PPAR-gamma agonists: therapeutic role in diabetes, inflammation and cancer

Trends Pharmacol Sci. 2000 Dec;21(12):469-74. doi: 10.1016/s0165-6147(00)01559-5.


The recent development of a novel class of insulin-sensitizing drugs, the thiazolidinediones (TZDs), represents a significant advance in antidiabetic therapy. One key mechanism by which these drugs exert their effects is by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma), a member of the nuclear receptor family. Evidence supporting this mechanism of action of the TZDs will be reviewed in this article. Recent data suggests that PPAR-gamma agonists might also have therapeutic potential in the treatment of inflammatory diseases and certain cancers.

Publication types

  • Review

MeSH terms

  • Animals
  • DNA-Binding Proteins / agonists
  • DNA-Binding Proteins / chemistry
  • DNA-Binding Proteins / therapeutic use*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Humans
  • Inflammation / drug therapy
  • Ligands
  • Neoplasms / drug therapy
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Thiazoles / chemistry
  • Thiazoles / therapeutic use*
  • Thiazolidinediones*
  • Transcription Factors / agonists*
  • Transcription Factors / chemistry


  • DNA-Binding Proteins
  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Thiazoles
  • Thiazolidinediones
  • Transcription Factors
  • 2,4-thiazolidinedione