1z11
Crystal Structure of Human Microsomal P450 2A6 with Methoxsalen Bound
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| , resolution 2.05Å | |||||||
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| Ligands: | , | ||||||
| Gene: | CYP2A6 (Homo sapiens) | ||||||
| Activity: | Unspecific monooxygenase, with EC number 1.14.14.1 | ||||||
| Related: | 1PQ2, 1R9O, 1TQN
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
OverviewOverview
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.
About this StructureAbout this Structure
1Z11 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen., Yano JK, Hsu MH, Griffin KJ, Stout CD, Johnson EF, Nat Struct Mol Biol. 2005 Sep;12(9):822-3. Epub 2005 Aug 7. PMID:16086027
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