Work

Drug-activated nuclear receptors CAR and PXR

Year: 2003

Type: article

Abstract: The metabolism and elimination of drugs is mainly mediated by cytochrome P450 (CYP) enzymes, aided by conjugative enzymes and transport proteins. An integral aspect of this elimination process is the induction of drug metabolism through activation of gene expression of metabolic and transport proteins. There is compelling evidence that induction is regulated by drug-activated nuclear receptors constitutive androstane receptor (CAR) and pregnane X receptor (PXR). This review outlines the basic properties of CAR and PXR, their ligands and target genes, and the mechanisms of the induction process. The implications of nuclear receptor-mediated induction for drug research are also discussed.

Source: Annals of Medicine

DOI: 10.1080/07853890310008224

Authors: Paavo Honkakoski, Tatsuya Sueyoshi, Masahiko Negishi

Institutions: University of Eastern Finland, National Institutes of Health, National Institute of Environmental Health Sciences

Language: English

Topic: Pharmacogenetics and Drug Metabolism

Subfield: Pharmacology

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: bronze

OpenAlex ID: W2040567225

FWCI: 14.42

Cites: 88

Cited by: 182

Related to: 10