Pxr, car and drug metabolism
Top Cited Papers
- 1 April 2002
- journal article
- review article
- Published by Springer Nature in Nature Reviews Drug Discovery
- Vol. 1 (4) , 259-266
- https://doi.org/10.1038/nrd753
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.Keywords
This publication has 90 references indexed in Scilit:
- Induction Profile of Rat Organic Anion Transporting Polypeptide 2 (oatp2) by Prototypical Drug-Metabolizing Enzyme Inducers That Activate Gene Expression through Ligand-Activated Transcription Factor PathwaysThe Journal of Pharmacology and Experimental Therapeutics, 2002
- High Throughput Screening: Early Successes Indicate a Promising FutureSLAS Discovery, 2001
- Clinical-Pharmacological Strategies to Assess Drug Interaction Potential During Drug DevelopmentDrug Safety, 2001
- Nuclear Receptor Response Elements Mediate Induction of Intestinal MDR1 by RifampinJournal of Biological Chemistry, 2001
- Ligand binding and nuclear receptor evolutionBioEssays, 2000
- Induction of Drug Metabolising EnzymesClinical Pharmacokinetics, 2000
- Pharmacogenomics of cytochrome P450 and other enzymes involved in biotransformation of xenobioticsDrug Development Research, 2000
- SXR, a novel steroid and xenobioticsensing nuclear receptorGenes & Development, 1998
- The Promoter of the Human 25-Hydroxyvitamin D31α-Hydroxylase Gene Confers Positive and Negative Responsiveness to PTH, Calcitonin, and 1α,25(OH)2D3Biochemical and Biophysical Research Communications, 1998
- P450 superfamily: update on new sequences, gene mapping, accession numbers and nomenclaturePharmacogenetics, 1996