11gs

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[[Image:11gs.gif|left|200px]]
[[Image:11gs.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 11gs |SIZE=350|CAPTION= <scene name='initialview01'>11gs</scene>, resolution 2.3&Aring;
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The line below this paragraph, containing "STRUCTURE_11gs", 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=EAA:ETHACRYNIC+ACID'>EAA</scene>, <scene name='pdbligand=GTT:GLUTATHIONE'>GTT</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</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/Glutathione_transferase Glutathione transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.18 2.5.1.18] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= GSTP1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_11gs| PDB=11gs | 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=11gs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=11gs OCA], [http://www.ebi.ac.uk/pdbsum/11gs PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=11gs RCSB]</span>
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}}
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'''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)'''
'''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)'''
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[[Category: Oakley, A J.]]
[[Category: Oakley, A J.]]
[[Category: Parker, M W.]]
[[Category: Parker, M W.]]
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[[Category: ethacrynic acid]]
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[[Category: Ethacrynic acid]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 09:27:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:27:10 2008''
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Revision as of 06:27, 2 May 2008

Image:11gs.gif

Template:STRUCTURE 11gs

GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)


Overview

The diuretic drug ethacrynic acid, an inhibitor of pi class glutathione S-transferase, has been tested in clinical trials as an adjuvant in chemotherapy. We recently solved the crystal structure of this enzyme in complex with ethacrynic acid and its glutathione conjugate. Here we present a new structure of the ethacrynic-glutathione conjugate complex. In this structure the ethacrynic moiety of the complex is shown to bind in a completely different orientation to that previously observed. Thus there are at least two binding modes possible, an observation of great importance to the design of second generation inhibitors of the enzyme.

About this Structure

11GS is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The glutathione conjugate of ethacrynic acid can bind to human pi class glutathione transferase P1-1 in two different modes., Oakley AJ, Lo Bello M, Mazzetti AP, Federici G, Parker MW, FEBS Lett. 1997 Dec 8;419(1):32-6. PMID:9426214 Page seeded by OCA on Fri May 2 09:27:17 2008

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