Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen

被引：0

作者：

Jason K Yano

Mei-Hui Hsu

Keith J Griffin

C David Stout

Eric F Johnson

机构：

[1] Scripps Research Institute,Department of Molecular and Experimental Medicine

[2] Scripps Research Institute,Department of Molecular Biology

来源：

Nature Structural & Molecular Biology | 2005年 / 12卷

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摘要：

Human microsomal cytochrome P450 2A6 (CYP2A6) contributes extensively to nicotine detoxication but also activates tobacco-specific procarcinogens to mutagenic products. The CYP2A6 structure shows a compact, hydrophobic active site with one hydrogen bond donor, Asn297, that orients coumarin for regioselective oxidation. The inhibitor methoxsalen effectively fills the active site cavity without substantially perturbing the structure. The structure should aid the design of inhibitors to reduce smoking and tobacco-related cancers.

引用

页码：822 / 823

页数：1

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