1tqn
From Proteopedia
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| - | [[Image:1tqn.gif|left|200px]] | + | [[Image:1tqn.gif|left|200px]] |
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| - | '''Crystal Structure of Human Microsomal P450 3A4''' | + | {{Structure |
| + | |PDB= 1tqn |SIZE=350|CAPTION= <scene name='initialview01'>1tqn</scene>, resolution 2.05Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=HEM:PROTOPORPHYRIN IX CONTAINING FE'>HEM</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= CYP3A4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''Crystal Structure of Human Microsomal P450 3A4''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1TQN is a [ | + | 1TQN 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=1TQN OCA]. |
==Reference== | ==Reference== | ||
| - | The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution., Yano JK, Wester MR, Schoch GA, Griffin KJ, Stout CD, Johnson EF, J Biol Chem. 2004 Sep 10;279(37):38091-4. Epub 2004 Jul 16. PMID:[http:// | + | The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution., Yano JK, Wester MR, Schoch GA, Griffin KJ, Stout CD, Johnson EF, J Biol Chem. 2004 Sep 10;279(37):38091-4. Epub 2004 Jul 16. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15258162 15258162] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: p450]] | [[Category: p450]] | ||
| - | ''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 14:21:53 2008'' |
Revision as of 12:21, 20 March 2008
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| , resolution 2.05Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | CYP3A4 (Homo sapiens) | ||||||
| Activity: | Unspecific monooxygenase, with EC number 1.14.14.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of Human Microsomal P450 3A4
Overview
The structure of P450 3A4 was determined by x-ray crystallography to 2.05-A resolution. P450 3A4 catalyzes the metabolic clearance of a large number of clinically used drugs, and a number of adverse drug-drug interactions reflect the inhibition or induction of the enzyme. P450 3A4 exhibits a relatively large substrate-binding cavity that is consistent with its capacity to oxidize bulky substrates such as cyclosporin, statins, taxanes, and macrolide antibiotics. Family 3A P450s also exhibit unusual kinetic characteristics that suggest simultaneous occupancy by smaller substrates. Although the active site volume is similar to that of P450 2C8 (PDB code: 1PQ2), the shape of the active site cavity differs considerably due to differences in the folding and packing of portions of the protein that form the cavity. Compared with P450 2C8, the active site cavity of 3A4 is much larger near the heme iron. The lower constraints on the motions of small substrates near the site of oxygen activation may diminish the efficiency of substrate oxidation, which may, in turn, be improved by space restrictions imposed by the presence of a second substrate molecule. The structure of P450 3A4 should facilitate a better understanding of the substrate selectivity of the enzyme.
About this Structure
1TQN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution., Yano JK, Wester MR, Schoch GA, Griffin KJ, Stout CD, Johnson EF, J Biol Chem. 2004 Sep 10;279(37):38091-4. Epub 2004 Jul 16. PMID:15258162
Page seeded by OCA on Thu Mar 20 14:21:53 2008
