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Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen
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Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen
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Journal Article
Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen
2005
Overview
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.
Publisher
Nature Publishing Group US,Nature Publishing Group
