Author(s): Yano JK, Hsu MH, Griffin KJ, Stout CD, Johnson EF, Yano JK, Hsu MH, Griffin KJ, Stout CD, Johnson EF
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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.
This article was published in Nat Struct Mol Biol
and referenced in Journal of Drug Metabolism & Toxicology