1z11
From Proteopedia
(New page: 200px<br /> <applet load="1z11" size="450" color="white" frame="true" align="right" spinBox="true" caption="1z11, resolution 2.05Å" /> '''Crystal Structure o...) |
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- | [[Image:1z11.gif|left|200px]]<br /> | + | [[Image:1z11.gif|left|200px]]<br /><applet load="1z11" size="350" color="white" frame="true" align="right" spinBox="true" |
- | <applet load="1z11" size=" | + | |
caption="1z11, resolution 2.05Å" /> | caption="1z11, resolution 2.05Å" /> | ||
'''Crystal Structure of Human Microsomal P450 2A6 with Methoxsalen Bound'''<br /> | '''Crystal Structure of Human Microsomal P450 2A6 with Methoxsalen Bound'''<br /> | ||
==Overview== | ==Overview== | ||
- | Human microsomal cytochrome P450 2A6 (CYP2A6) contributes extensively to | + | 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 Structure== | ==About this Structure== | ||
- | 1Z11 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with HEM and 8MO as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Unspecific_monooxygenase Unspecific monooxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.14.1 1.14.14.1] Full crystallographic information is available from [http:// | + | 1Z11 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=HEM:'>HEM</scene> and <scene name='pdbligand=8MO:'>8MO</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Unspecific_monooxygenase Unspecific monooxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.14.1 1.14.14.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Z11 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Unspecific monooxygenase]] | [[Category: Unspecific monooxygenase]] | ||
- | [[Category: Griffin, K | + | [[Category: Griffin, K J.]] |
- | [[Category: Hsu, M | + | [[Category: Hsu, M H.]] |
- | [[Category: Johnson, E | + | [[Category: Johnson, E F.]] |
- | [[Category: Stout, C | + | [[Category: Stout, C D.]] |
- | [[Category: Yano, J | + | [[Category: Yano, J K.]] |
[[Category: 8MO]] | [[Category: 8MO]] | ||
[[Category: HEM]] | [[Category: HEM]] | ||
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[[Category: p450 2a6]] | [[Category: p450 2a6]] | ||
- | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:11:06 2008'' |
Revision as of 14:11, 21 February 2008
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Crystal Structure of Human Microsomal P450 2A6 with Methoxsalen Bound
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.
About this Structure
1Z11 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Unspecific monooxygenase, with EC number 1.14.14.1 Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Thu Feb 21 16:11:06 2008
Categories: Homo sapiens | Single protein | Unspecific monooxygenase | Griffin, K J. | Hsu, M H. | Johnson, E F. | Stout, C D. | Yano, J K. | 8MO | HEM | Coumarin 7-hydroxylase | Cyp2a6 | Drug metabolizing enzyme | Heme | Methoxsalen | Monooxygenase | Nicotine oxidase | Oxidoreductase | P450 | P450 2a6