Antineoplastic effects of peroxisome proliferator-activated receptor gamma agonists

Lancet Oncol. 2004 Jul;5(7):419-29. doi: 10.1016/S1470-2045(04)01509-8.


Peroxisome proliferator-activated receptors (PPAR) are members of a superfamily of nuclear hormone receptors. Activation of PPAR isoforms elicits both antineoplastic and anti-inflammatory effects in several types of mammalian cells. PPARs are ligand-activated transcription factors and have a subfamily of three different isoforms: PPAR alpha, PPAR gamma, and PPAR beta/delta. All isoforms heterodimerise with the 9-cis-retinoic acid receptor RXR, and play an important part in the regulation of several metabolic pathways, including lipid biosynthesis and glucose metabolism. Endogenous ligands of PPAR gamma include long-chain polyunsaturated fatty acids, eicosanoid derivates, and oxidised lipids. Newly developed synthetic ligands include thiazolidinediones-a group of potent PPAR gamma agonists and antidiabetic agents. Here, we review PPAR gamma-induced antineoplastic signalling pathways, and summarise the antineoplastic effects of PPAR gamma agonists in different cancer cell lines, animal models, and clinical trials.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Clinical Trials as Topic
  • Humans
  • Models, Animal
  • Neoplasms / drug therapy*
  • Receptors, Cytoplasmic and Nuclear / agonists
  • Receptors, Cytoplasmic and Nuclear / therapeutic use
  • Signal Transduction / physiology
  • Transcription Factors / agonists
  • Transcription Factors / pharmacology*
  • Transcription Factors / therapeutic use


  • Antineoplastic Agents
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors