1r9o

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[[Image:1r9o.gif|left|200px]]
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{{Seed}}
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[[Image:1r9o.png|left|200px]]
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{{STRUCTURE_1r9o| PDB=1r9o | SCENE= }}
{{STRUCTURE_1r9o| PDB=1r9o | SCENE= }}
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'''Crystal Structure of P4502C9 with Flurbiprofen bound'''
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===Crystal Structure of P4502C9 with Flurbiprofen bound===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 15181000 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15181000}}
==About this Structure==
==About this Structure==
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[[Category: Oxidoreductase]]
[[Category: Oxidoreductase]]
[[Category: P450]]
[[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 Mon Jul 28 12:41:08 2008''

Revision as of 09:41, 28 July 2008

Image:1r9o.png

Template:STRUCTURE 1r9o

Crystal Structure of P4502C9 with Flurbiprofen bound

Template:ABSTRACT PUBMED 15181000

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

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