1qxy
From Proteopedia
(New page: 200px<br /><applet load="1qxy" size="450" color="white" frame="true" align="right" spinBox="true" caption="1qxy, resolution 1.04Å" /> '''Crystal structure of...) |
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| - | [[Image:1qxy.gif|left|200px]]<br /><applet load="1qxy" size=" | + | [[Image:1qxy.gif|left|200px]]<br /><applet load="1qxy" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1qxy, resolution 1.04Å" /> | caption="1qxy, resolution 1.04Å" /> | ||
'''Crystal structure of S. aureus methionine aminopeptidase in complex with a ketoheterocycle 618'''<br /> | '''Crystal structure of S. aureus methionine aminopeptidase in complex with a ketoheterocycle 618'''<br /> | ||
==Overview== | ==Overview== | ||
| - | High-resolution crystal structures of Staphylococcus aureus methionine | + | High-resolution crystal structures of Staphylococcus aureus methionine aminopeptidase I in complex with various keto heterocycles and aminoketones were determined, and the intermolecular ligand interactions with the enzyme are reported. The compounds are effective inhibitors of the S. aureus enzyme because of the formation of an uncleavable tetrahedral intermediate upon binding. The electron densities unequivocally show the enzyme-catalyzed transition-state analogue mimicking that for amide bond hydrolysis of substrates. |
==About this Structure== | ==About this Structure== | ||
| - | 1QXY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with CO, ACT and M2C as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Methionyl_aminopeptidase Methionyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.18 3.4.11.18] Full crystallographic information is available from [http:// | + | 1QXY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with <scene name='pdbligand=CO:'>CO</scene>, <scene name='pdbligand=ACT:'>ACT</scene> and <scene name='pdbligand=M2C:'>M2C</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Methionyl_aminopeptidase Methionyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.18 3.4.11.18] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QXY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Staphylococcus aureus]] | [[Category: Staphylococcus aureus]] | ||
| - | [[Category: Arcy, A | + | [[Category: Arcy, A D.]] |
| - | [[Category: Dale, G | + | [[Category: Dale, G E.]] |
[[Category: Douangamath, A.]] | [[Category: Douangamath, A.]] | ||
[[Category: Oefner, C.]] | [[Category: Oefner, C.]] | ||
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[[Category: pita bread fold]] | [[Category: pita bread fold]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:44:53 2008'' |
Revision as of 12:44, 21 February 2008
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Crystal structure of S. aureus methionine aminopeptidase in complex with a ketoheterocycle 618
Overview
High-resolution crystal structures of Staphylococcus aureus methionine aminopeptidase I in complex with various keto heterocycles and aminoketones were determined, and the intermolecular ligand interactions with the enzyme are reported. The compounds are effective inhibitors of the S. aureus enzyme because of the formation of an uncleavable tetrahedral intermediate upon binding. The electron densities unequivocally show the enzyme-catalyzed transition-state analogue mimicking that for amide bond hydrolysis of substrates.
About this Structure
1QXY is a Single protein structure of sequence from Staphylococcus aureus with , and as ligands. Active as Methionyl aminopeptidase, with EC number 3.4.11.18 Full crystallographic information is available from OCA.
Reference
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate., Douangamath A, Dale GE, D'Arcy A, Almstetter M, Eckl R, Frutos-Hoener A, Henkel B, Illgen K, Nerdinger S, Schulz H, Mac Sweeney A, Thormann M, Treml A, Pierau S, Wadman S, Oefner C, J Med Chem. 2004 Mar 11;47(6):1325-8. PMID:14998322
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