PXR, CAR and drug metabolism.

by: TM Willson, SA Kliewer

Nature reviews. Drug discovery, Vol. 1, No. 4. (April 2002), pp. 259-266.

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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.

@article{citeulike:2837343, 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.}, address = {GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. tmw20653@gsk.com}, author = {Willson, T. M. and Kliewer, S. A. }, citeulike-article-id = {2837343}, issn = {1474-1776}, journal = {Nature reviews. Drug discovery}, keywords = {induction, p450, pxr}, month = {April}, number = {4}, pages = {259--266}, posted-at = {2008-05-27 12:59:29}, priority = {2}, title = {PXR, CAR and drug metabolism.}, url = {http://view.ncbi.nlm.nih.gov/pubmed/12120277}, volume = {1}, year = {2002} }

RIS record

TY - JOUR ID - citeulike:2837343 L3 - citeulike-article-id:2837343 N2 - 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. IS - 4 JF - Nature reviews. Drug discovery SN - 1474-1776 AD - GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. tmw20653@gsk.com EP - 266 TI - PXR, CAR and drug metabolism. VL - 1 SP - 259 KW - induction KW - p450 KW - pxr AU - Willson, TM AU - Kliewer, SA PY - 2002/04// UR - http://view.ncbi.nlm.nih.gov/pubmed/12120277 ER -

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