1w0f: Difference between revisions

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{{STRUCTURE_1w0f|  PDB=1w0f  |  SCENE=  }}  
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'''CRYSTAL STRUCTURE OF HUMAN CYTOCHROME P450 3A4'''
===CRYSTAL STRUCTURE OF HUMAN CYTOCHROME P450 3A4===




==Overview==
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Cytochromes P450 (P450s) metabolize a wide range of endogenous compounds and xenobiotics, such as pollutants, environmental compounds, and drug molecules. The microsomal, membrane-associated, P450 isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, and CYP1A2 are responsible for the oxidative metabolism of more than 90% of marketed drugs. Cytochrome P450 3A4 (CYP3A4) metabolizes more drug molecules than all other isoforms combined. Here we report three crystal structures of CYP3A4: unliganded, bound to the inhibitor metyrapone, and bound to the substrate progesterone. The structures revealed a surprisingly small active site, with little conformational change associated with the binding of either compound. An unexpected peripheral binding site is identified, located above a phenylalanine cluster, which may be involved in the initial recognition of substrates or allosteric effectors.
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==About this Structure==
==About this Structure==
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[[Category: Nifedipine oxidase]]
[[Category: Nifedipine oxidase]]
[[Category: Oxidoreductase]]
[[Category: Oxidoreductase]]
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Revision as of 20:12, 27 July 2008

File:1w0f.png

Template:STRUCTURE 1w0f

CRYSTAL STRUCTURE OF HUMAN CYTOCHROME P450 3A4CRYSTAL STRUCTURE OF HUMAN CYTOCHROME P450 3A4

Template:ABSTRACT PUBMED 15256616

About this StructureAbout this Structure

1W0F is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone., Williams PA, Cosme J, Vinkovic DM, Ward A, Angove HC, Day PJ, Vonrhein C, Tickle IJ, Jhoti H, Science. 2004 Jul 30;305(5684):683-6. Epub 2004 Jul 15. PMID:15256616

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