11gs
From Proteopedia
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| - | [[Image:11gs.gif|left|200px]] | + | [[Image:11gs.gif|left|200px]] |
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| - | '''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)''' | + | {{Structure |
| + | |PDB= 11gs |SIZE=350|CAPTION= <scene name='initialview01'>11gs</scene>, resolution 2.3Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=GTT:GLUTATHIONE'>GTT</scene>, <scene name='pdbligand=EAA:ETHACRYNIC+ACID'>EAA</scene> and <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC ACID'>MES</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= GSTP1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 11GS is a [ | + | 11GS 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=11GS OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/9426214 9426214] |
[[Category: Glutathione transferase]] | [[Category: Glutathione transferase]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''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 09:48:51 2008'' |
Revision as of 07:48, 20 March 2008
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| , resolution 2.3Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , and | ||||||
| Gene: | GSTP1 (Homo sapiens) | ||||||
| Activity: | Glutathione transferase, with EC number 2.5.1.18 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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
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