CYP2A6: a human coumarin 7-hydroxylase

被引：183

作者：

Pelkonen, O

Rautio, A

Raunio, H

Pasanen, M

机构：

[1] Univ Oulu, Dept Pharmacol & Toxicol, FIN-90401 Oulu, Finland

[2] Natl Agcy Med, Helsinki, Finland

来源：

TOXICOLOGY | 2000年 / 144卷 / 1-3期

关键词：

D O I：

10.1016/S0300-483X(99)00200-0

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Coumarin 7-hydroxylation is catalysed by a high-affinity CYP2A6 enzyme in human liver microsomes. CYP2A6 is the only enzyme catalysing this reaction and consequently the formation of 7-hydroxycoumarin can be used as 'an in vitro and in vivo probe' for CYP2A6. CYP2A6 is a major contributor to the oxidative metabolism of nicotine and cotinine, and it also contributes, to a larger or smaller extent, to the metabolism of a few pharmaceuticals (e.g. fadrozole), nitrosamines, other carcinogens (e.g. aflatoxin B1) and a number of coumarin-type alkaloids. CYP2A6 may be inducible by antiepileptic drugs and it is decreased in alcohol-induced severe liver cirrhosis. Several mutated or deleted CYP2AG alleles have been characterized. Although CYP2A6 represent up to 15% of human microsomes P450 proteins, it is still one of the less well characterised cytochrome P450 enzymes. (C) 2000 Elsevier Science Ireland Ltd. All rights reserved.

引用

页码：139 / 147

页数：9

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