Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR)

被引：114

作者：

Chang, TKH

Waxman, DJ

机构：

[1] Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V6T 1Z3, Canada

[2] Boston Univ, Dept Biol, Div Cell & Mol Biol, Boston, MA 02215 USA

来源：

DRUG METABOLISM REVIEWS | 2006年 / 38卷 / 1-2期

关键词：

constitutive androstane receptor; cytochrome P450; drug-metabolizing enzyme; drug transporter; nuclear receptor; pregnane X receptor;

D O I：

10.1080/03602530600569828

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

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页码：51 / 73

页数：23

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