PXR, car and drug metabolism

Timothy M. Willson, Steven A. Kliewer

Research output: Contribution to journalReview article

350 Scopus citations

Abstract

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
Volume1
Issue number4
DOIs
StatePublished - Apr 2002

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ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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