4acs

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[[Image:4acs.png|left|200px]]
 
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==Crystal structure of mutant GST A2-2 with enhanced catalytic efficiency with azathioprine==
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The line below this paragraph, containing "STRUCTURE_4acs", creates the "Structure Box" on the page.
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<StructureSection load='4acs' size='340' side='right'caption='[[4acs]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[4acs]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ACS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ACS FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GSH:GLUTATHIONE'>GSH</scene></td></tr>
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{{STRUCTURE_4acs| PDB=4acs | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4acs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4acs OCA], [https://pdbe.org/4acs PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4acs RCSB], [https://www.ebi.ac.uk/pdbsum/4acs PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4acs ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/GSTA2_HUMAN GSTA2_HUMAN] Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Glutathione transferase (GST) A2-2 is the most efficient human enzyme in the biotransformation of the prodrug azathioprine (Aza). The activation of Aza has therapeutic potential for possible use of GSTs in targeted enzyme-prodrug treatment of diseases. Based on the assumed catalytic mechanism and computational docking of Aza to the active site of the enzyme, active-site residues were selected for construction of focused mutant libraries, which were thereafter screened for Aza activity. Mutants with elevated Aza activity were identified, DNA sequenced, and the proteins purified. The two most active mutants showed up to 70-fold higher catalytic efficiency than the parental GST A2-2. The structure of the most active triple mutant (L107G/L108D/F222H) enzyme was determined by X-ray crystallography demonstrating significant changes in the topography of the active site facilitating productive binding of Aza as a substrate.
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===Crystal structure of mutant GST A2-2 with enhanced catalytic efficiency with azathioprine===
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Structure-Based Redesign of GST A2-2 for Enhanced Catalytic Efficiency with Azathioprine.,Zhang W, Moden O, Tars K, Mannervik B Chem Biol. 2012 Mar 23;19(3):414-21. PMID:22444596<ref>PMID:22444596</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4acs" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_22444596}}, adds the Publication Abstract to the page
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*[[Glutathione S-transferase 3D structures|Glutathione S-transferase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 22444596 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_22444596}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[4acs]] is a 4 chain structure with 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=4ACS OCA].
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==Reference==
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<ref group="xtra">PMID:022444596</ref><references group="xtra"/>
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[[Category: Glutathione transferase]]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Mannervik, B.]]
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[[Category: Large Structures]]
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[[Category: Moden, O.]]
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[[Category: Mannervik B]]
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[[Category: Tars, K.]]
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[[Category: Moden O]]
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[[Category: Zhang, W.]]
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[[Category: Tars K]]
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[[Category: Oxidation-reduction]]
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[[Category: Zhang W]]
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[[Category: Transferase]]
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Current revision

Crystal structure of mutant GST A2-2 with enhanced catalytic efficiency with azathioprine

PDB ID 4acs

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