PXR, car and drug metabolism

Timothy M. Willson, Steven A. Kliewer

Research output: Contribution to journalReview articlepeer-review

406 Scopus citations


Mechanisms that protect the body from a diverse array of harmful chemicals are also involved in drug metabolism, and can cause adverse drug-drug interactions. Two closely related orphan nuclear hormone receptors - the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) - have recently emerged as transcriptional regulators of cytochrome P450 expression that couple xenobiotic exposure to oxidative metabolism. In this review, we provide an examination of the roles of PXR and CAR as xenobiotic sensors, and discuss the application of this knowledge to toxicological screening in drug discovery.

Original languageEnglish (US)
Pages (from-to)259-266
Number of pages8
JournalNature Reviews Drug Discovery
Issue number4
StatePublished - Apr 2002

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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