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11gs
From Proteopedia
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(New page: 200px<br /> <applet load="11gs" size="450" color="white" frame="true" align="right" spinBox="true" caption="11gs, resolution 2.3Å" /> '''GLUTATHIONE S-TRANSF...)
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Revision as of 13:46, 12 November 2007
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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 with GTT, EAA and MES as ligands. Active as Glutathione transferase, with EC number 2.5.1.18 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 Mon Nov 12 15:52:45 2007
