1z10: Difference between revisions
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[[Image:1z10.gif|left|200px]] | [[Image:1z10.gif|left|200px]] | ||
'''Crystal Structure of Human Microsomal P450 2A6 with Coumarin Bound''' | {{Structure | ||
|PDB= 1z10 |SIZE=350|CAPTION= <scene name='initialview01'>1z10</scene>, resolution 1.90Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=COU:COUMARIN'>COU</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene> | |||
|ACTIVITY= [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] | |||
|GENE= CYP2A6 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |||
}} | |||
'''Crystal Structure of Human Microsomal P450 2A6 with Coumarin Bound''' | |||
==Overview== | ==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. | 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. | ||
==Disease== | |||
Known diseases associated with this structure: Coumarin resistance OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=122720 122720]], Lung cancer, resistance to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=122720 122720]], Nicotine addiction, protection from OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=122720 122720]] | |||
==About this Structure== | ==About this Structure== | ||
1Z10 is a [ | 1Z10 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Z10 OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/16086027 16086027] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| Line 32: | Line 44: | ||
[[Category: p450 2a6]] | [[Category: p450 2a6]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:29:59 2008'' | ||
Revision as of 16:29, 20 March 2008
| |||||||
| , resolution 1.90Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , and | ||||||
| Gene: | CYP2A6 (Homo sapiens) | ||||||
| Activity: | Unspecific monooxygenase, with EC number 1.14.14.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of Human Microsomal P450 2A6 with Coumarin Bound
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.
DiseaseDisease
Known diseases associated with this structure: Coumarin resistance OMIM:[122720], Lung cancer, resistance to OMIM:[122720], Nicotine addiction, protection from OMIM:[122720]
About this StructureAbout this Structure
1Z10 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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