1r9o

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[[Image:1r9o.gif|left|200px]]
[[Image:1r9o.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1r9o |SIZE=350|CAPTION= <scene name='initialview01'>1r9o</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1r9o", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=FLP:FLURBIPROFEN'>FLP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CYP2C9 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1r9o| PDB=1r9o | SCENE= }}
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|RELATEDENTRY=[[1n6b|1N6B]], [[1og5|1OG5]], [[1po5|1PO5]], [[1pq2|1PQ2]], [[1nr6|1NR6]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1r9o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r9o OCA], [http://www.ebi.ac.uk/pdbsum/1r9o PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1r9o RCSB]</span>
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}}
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'''Crystal Structure of P4502C9 with Flurbiprofen bound'''
'''Crystal Structure of P4502C9 with Flurbiprofen bound'''
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[[Category: Wester, M R.]]
[[Category: Wester, M R.]]
[[Category: Yano, J K.]]
[[Category: Yano, J K.]]
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[[Category: drug metabolizing enzyme]]
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[[Category: Drug metabolizing enzyme]]
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[[Category: heme]]
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[[Category: Heme]]
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[[Category: monooxygenase]]
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[[Category: Monooxygenase]]
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[[Category: oxidoreductase]]
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[[Category: Oxidoreductase]]
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[[Category: p450]]
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[[Category: P450]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:14:45 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:25:02 2008''
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Revision as of 04:14, 3 May 2008

Image:1r9o.gif

Template:STRUCTURE 1r9o

Crystal Structure of P4502C9 with Flurbiprofen bound


Overview

The structure of human P450 2C9 complexed with flurbiprofen was determined to 2.0 A by x-ray crystallography. In contrast to other structurally characterized P450 2C enzymes, 2C5, 2C8, and a 2C9 chimera, the native catalytic domain of P450 2C9 differs significantly in the conformation of the helix F to helix G region and exhibits an extra turn at the N terminus of helix A. In addition, a distinct conformation of the helix B to helix C region allows Arg-108 to hydrogen bond with Asp-293 and Asn-289 on helix I and to interact directly with the carboxylate of flurbiprofen. These interactions position the substrate for regioselective oxidation in a relatively large active site cavity and are likely to account for the high catalytic efficiency exhibited by P450 2C9 for the regioselective oxidation of several anionic non-steroidal anti-inflammatory drugs. The structure provides a basis for interpretation of a number of observations regarding the substrate selectivity of P450 2C9 and the observed effects of mutations on catalysis.

About this Structure

1R9O is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The structure of human cytochrome P450 2C9 complexed with flurbiprofen at 2.0-A resolution., Wester MR, Yano JK, Schoch GA, Yang C, Griffin KJ, Stout CD, Johnson EF, J Biol Chem. 2004 Aug 20;279(34):35630-7. Epub 2004 Jun 4. PMID:15181000 Page seeded by OCA on Sat May 3 07:14:45 2008

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OCA

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