Synthetic Drugs and Natural Products as Modulators of Constitutive Androstane Receptor (Car) and Pregnane X Receptor (PXR)
- 1 January 2006
- journal article
- research article
- Published by Taylor & Francis in Drug Metabolism Reviews
- Vol. 38 (1-2) , 51-73
- https://doi.org/10.1080/03602530600569828
Abstract
Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) are members of the nuclear receptor superfamily. These transcription factors are predominantly expressed in the liver, where they are activated by structurally diverse compounds, including many drugs and endogenous substances. CAR and PXR regulate the expression of a broad range of genes, which contribute to transcellular transport, bioactivation, and detoxification of numerous xenochemicals and endogenous substances. This article discusses the importance of these receptors for pharmacology and toxicology, emphasizing the role of individual drugs and natural products as agonists, indirect activators, inverse agonists, and antagonists of CAR and PXR.Keywords
This publication has 133 references indexed in Scilit:
- Chronic ethanol exposure downregulates hepatic expression of pregnane X receptor and P450 3A11 in female ICR miceToxicology, 2005
- Trabectedin (YondelisTM, formerly ET-743), a mass balance study in patients with advanced cancerInvestigational New Drugs, 2005
- CAR and PXR agonists stimulate hepatic bile acid and bilirubin detoxification and elimination pathways in mice†Hepatology, 2005
- Steroid and xenobiotic receptor (SXR), cytochrome P450 3A4 and multidrug resistance gene 1 in human adult and fetal tissuesMolecular and Cellular Endocrinology, 2005
- Cytoplasmic Localization of Pregnane X Receptor and Ligand-dependent Nuclear Translocation in Mouse LiverJournal of Biological Chemistry, 2004
- DESMETHOXYYANGONIN AND DIHYDROMETHYSTICIN ARE TWO MAJOR PHARMACOLOGICAL KAVALACTONES WITH MARKED ACTIVITY ON THE INDUCTION OF CYP3A23Drug Metabolism and Disposition, 2004
- Expression of Constitutive Androstane Receptor Splice Variants in Human Tissues and Their Functional ConsequencesThe Journal of Pharmacology and Experimental Therapeutics, 2004
- Avasimibe Induces CYP3A4 and Multiple Drug Resistance Protein 1 Gene Expression through Activation of the Pregnane X ReceptorThe Journal of Pharmacology and Experimental Therapeutics, 2003
- Role of the Hepatocyte Nuclear Factor 4α in Control of the Pregnane X Receptor During Fetal Liver DevelopmentHepatology, 2003
- Pathophysiological Factors Affecting CAR Gene ExpressionDrug Metabolism Reviews, 2003