Drug-activated nuclear receptors CAR and PXR

被引：142

作者：

Honkakoski, P

Sueyoshi, T

Negishi, M

机构：

[1] NIEHS, Pharmacogenet Sect, Reprod & Dev Toxicol Lab, Res Triangle Pk, NC 27709 USA

[2] Univ Kuopio, Dept Pharmaceut, FIN-70211 Kuopio, Finland

来源：

ANNALS OF MEDICINE | 2003年 / 35卷 / 03期

关键词：

CAR; cytochrome P450; drug metabolism; induction; intestine; liver; nuclear receptor; PXR; RXR;

D O I：

10.1080/07853890310008224

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

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.

引用

收藏

页码：172 / 182

页数：11

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