1ebv

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[[Image:1ebv.jpg|left|200px]]
[[Image:1ebv.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1ebv |SIZE=350|CAPTION= <scene name='initialview01'>1ebv</scene>, resolution 3.2&Aring;
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The line below this paragraph, containing "STRUCTURE_1ebv", 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=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=OAS:O-ACETYLSERINE'>OAS</scene>, <scene name='pdbligand=SCL:ACETIC+ACID+SALICYLOYL-AMINO-ESTER'>SCL</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/Prostaglandin-endoperoxide_synthase Prostaglandin-endoperoxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1ebv| PDB=1ebv | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ebv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ebv OCA], [http://www.ebi.ac.uk/pdbsum/1ebv PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ebv RCSB]</span>
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}}
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'''OVINE PGHS-1 COMPLEXED WITH SALICYL HYDROXAMIC ACID'''
'''OVINE PGHS-1 COMPLEXED WITH SALICYL HYDROXAMIC ACID'''
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[[Category: Loll, P J.]]
[[Category: Loll, P J.]]
[[Category: Sharkey, C T.]]
[[Category: Sharkey, C T.]]
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[[Category: monotopic membrane protein]]
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[[Category: Monotopic membrane protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:55:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:59:32 2008''
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Revision as of 11:55, 2 May 2008

Image:1ebv.jpg

Template:STRUCTURE 1ebv

OVINE PGHS-1 COMPLEXED WITH SALICYL HYDROXAMIC ACID


Overview

Aspirin is unique among clinically used nonsteroidal antiinflammatory drugs in that it irreversibly inactivates prostaglandin (PG) H2 synthase (PGHS) via acetylation of an active-site serine residue. We report the synthesis and characterization of a novel acetylating agent, O-acetylsalicylhydroxamic acid (AcSHA), which inhibits PGE2 synthesis in vivo and blocks the cyclooxygenase activity of PGHS in vitro. AcSHA requires the presence of the active-site residue Ser-529 to be active against human PGHS-1; the S529A mutant is resistant to inactivation by the inhibitor. Analysis of PGHS inactivation by AcSHA, coupled with the X-ray crystal structure of the complex of ovine PGHS-1 with AcSHA, confirms that the inhibitor elicits its effects via acetylation of Ser-529 in the cyclooxygenase active site. The crystal structure reveals an intact inhibitor molecule bound in the enzyme's cyclooxygenase active-site channel, hydrogen bonding with Arg-119 of the enzyme. The structure-activity profile of AcSHA can be rationalized in terms of the crystal structure of the enzyme-ligand complex. AcSHA may prove useful as a lead compound to facilitate the development of new acetylating inhibitors.

About this Structure

1EBV is a Single protein structure of sequence from Ovis aries. Full crystallographic information is available from OCA.

Reference

O-acetylsalicylhydroxamic acid, a novel acetylating inhibitor of prostaglandin H2 synthase: structural and functional characterization of enzyme-inhibitor interactions., Loll PJ, Sharkey CT, O'Connor SJ, Dooley CM, O'Brien E, Devocelle M, Nolan KB, Selinsky BS, Fitzgerald DJ, Mol Pharmacol. 2001 Dec;60(6):1407-13. PMID:11723249 Page seeded by OCA on Fri May 2 14:55:01 2008

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