4kyh
From Proteopedia
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==Crystal structure of mouse glyoxalase I complexed with zopolrestat== | ==Crystal structure of mouse glyoxalase I complexed with zopolrestat== | ||
| - | <StructureSection load='4kyh' size='340' side='right'caption='[[4kyh]]' scene=''> | + | <StructureSection load='4kyh' size='340' side='right'caption='[[4kyh]], [[Resolution|resolution]] 2.50Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4KYH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4KYH FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[4kyh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4KYH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4KYH FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4kyh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4kyh OCA], [https://pdbe.org/4kyh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4kyh RCSB], [https://www.ebi.ac.uk/pdbsum/4kyh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4kyh ProSAT]</span></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=ZST:3,4-DIHYDRO-4-OXO-3-((5-TRIFLUOROMETHYL-2-BENZOTHIAZOLYL)METHYL)-1-PHTHALAZINE+ACETIC+ACID'>ZST</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4kyh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4kyh OCA], [https://pdbe.org/4kyh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4kyh RCSB], [https://www.ebi.ac.uk/pdbsum/4kyh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4kyh ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/LGUL_MOUSE LGUL_MOUSE] Catalyzes the conversion of hemimercaptal, formed from methylglyoxal and glutathione, to S-lactoylglutathione. Involved in the regulation of TNF-induced transcriptional activity of NF-kappa-B (By similarity). | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Old drugs new tricks: Zopolrestat, an aldose reductase inhibitor developed by Pfizer for the treatment of diabetic complications, is a potent competition inhibitor of human glyoxalase I (GLOI) in vitro. Crystal structures of GLOI in complex with zopolrestat and indomethacin, a nonsteroidal anti-inflammatory drug and moderate inhibitor of GLOI, provide a structural basis for the development of novel GLOI inhibitors with excellent pharmacokinetics profiles. | ||
| + | |||
| + | Zopolrestat as a Human Glyoxalase I Inhibitor and Its Structural Basis.,Zhai J, Zhang H, Zhang L, Zhao Y, Chen S, Chen Y, Peng X, Li Q, Yuan M, Hu X ChemMedChem. 2013 Jul 15. doi: 10.1002/cmdc.201300243. PMID:23857942<ref>PMID:23857942</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 4kyh" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
*[[Glyoxalase 3D structures|Glyoxalase 3D structures]] | *[[Glyoxalase 3D structures|Glyoxalase 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| + | [[Category: Mus musculus]] | ||
[[Category: Chen S]] | [[Category: Chen S]] | ||
[[Category: Chen Y]] | [[Category: Chen Y]] | ||
Current revision
Crystal structure of mouse glyoxalase I complexed with zopolrestat
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Categories: Large Structures | Mus musculus | Chen S | Chen Y | Yuan M | Zhai J | Zhang H | Zhang L | Zhao Y
