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11gs

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(New page: 200px<br /> <applet load="11gs" size="450" color="white" frame="true" align="right" spinBox="true" caption="11gs, resolution 2.3&Aring;" /> '''GLUTATHIONE S-TRANSF...)
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<applet load="11gs" size="450" color="white" frame="true" align="right" spinBox="true"
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'''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)'''<br />
'''GLUTATHIONE S-TRANSFERASE COMPLEXED WITH ETHACRYNIC ACID-GLUTATHIONE CONJUGATE (FORM II)'''<br />
==Overview==
==Overview==
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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.
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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==
==About this Structure==
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11GS is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with GTT, EAA and MES as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=11GS OCA].
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11GS is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=GTT:'>GTT</scene>, <scene name='pdbligand=EAA:'>EAA</scene> and <scene name='pdbligand=MES:'>MES</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=11GS OCA].
==Reference==
==Reference==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Bello, M.Lo.]]
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[[Category: Bello, M Lo.]]
[[Category: Federici, G.]]
[[Category: Federici, G.]]
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[[Category: Mazzetti, A.P.]]
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[[Category: Mazzetti, A P.]]
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[[Category: Oakley, A.J.]]
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[[Category: Oakley, A J.]]
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[[Category: Parker, M.W.]]
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[[Category: Parker, M W.]]
[[Category: EAA]]
[[Category: EAA]]
[[Category: GTT]]
[[Category: GTT]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 15:52:45 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 11:37:44 2008''

Revision as of 09:37, 21 February 2008

Image:11gs.gif

11gs, resolution 2.3Å

Drag the structure with the mouse to rotate

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 , and 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 Thu Feb 21 11:37:44 2008

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