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- Title
Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen.
- Authors
Yano, Jason K; Mei-Hui Hsu; Griffin, Keith J; Stout, C. David; Johnson, Eric F.
- Abstract
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.
- Subjects
CYTOCHROMES; HEMOPROTEINS; BIOLOGICAL pigments; COUMARINS; ANTICOAGULANTS; BENZOPYRANS
- Publication
Nature Structural & Molecular Biology, 2005, Vol 12, Issue 9, p822
- ISSN
1545-9993
- Publication type
Article
- DOI
10.1038/nsmb971