The toxicology of ligands for peroxisome proliferator-activated receptors (PPAR)

Marjorie A. Peraza, Andrew D. Burdick, Holly E. Marin, Frank J. Gonzalez, Jeffrey M. Peters

Research output: Contribution to journalReview articlepeer-review

210 Scopus citations

Abstract

Peroxisome proliferator-activated receptors (PPARs) are ligand activated transcription factors that modulate target gene expression in response to endogenous and exogenous ligands. Ligands for the PPARs have been widely developed for the treatment of various diseases including dyslipidemias and diabetes. While targeting selective receptor activation is an established therapeutic approach for the treatment of various diseases, a variety of toxicities are known to occur in response to ligand administration. Whether PPAR ligands produce toxicity via a receptor-dependent and/or off-target-mediated mechanism(s) is not always known. Extrapolation of data derived from animal models and/or in vitro models, to humans, is also questionable. The different toxicities and mechanisms associated with administration of ligands for the three PPARs will be discussed, and important data gaps that could increase our current understanding of how PPAR ligands lead to toxicity will be highlighted.

Original languageEnglish (US)
Pages (from-to)269-295
Number of pages27
JournalToxicological Sciences
Volume90
Issue number2
DOIs
StatePublished - Apr 2006

All Science Journal Classification (ASJC) codes

  • Toxicology

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