Central role of peroxisome proliferator-activated receptors in the actions of peroxisome proliferators

Annu Rev Pharmacol Toxicol. 2000;40:491-518. doi: 10.1146/annurev.pharmtox.40.1.491.


Peroxisome proliferators (PPs) are a large class of structurally dissimilar chemicals that have diverse effects in rodents and humans. Most, if not all, of the diverse effects of PPs are mediated by three members of the nuclear receptor superfamily called peroxisome proliferator-activated receptors (PPARs). In this review, we define the molecular mechanisms of PPs, including PPAR binding specificity, alteration of gene expression through binding to DNA response elements, and cross talk with other signaling pathways. We discuss the roles of PPARs in growth promotion in rodent hepatocarcinogenesis and potential therapeutic effects, including suppression of cancer growth and inflammation.

Publication types

  • Review

MeSH terms

  • Animals
  • Humans
  • Inflammation / drug therapy
  • Liver Neoplasms / chemically induced
  • Peroxisome Proliferators / pharmacology*
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Receptors, Cytoplasmic and Nuclear / drug effects
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Response Elements
  • Signal Transduction
  • Structure-Activity Relationship
  • Transcription Factors / chemistry
  • Transcription Factors / drug effects
  • Transcription Factors / physiology*


  • Peroxisome Proliferators
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors