4kyh

<StructureSection load='4kyh' size='340' side='right'caption='[[4kyh]], [[Resolution|resolution]] 2.50&Aring;' scene=''>

<table><tr><td colspan='2'>[[4kyh]] is a 2 chain structure. 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='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>

== 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).

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== 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&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>

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<div class="pdbe-citations 4kyh" style="background-color:#fffaf0;"></div>

== References ==

<references/>

[[Category: Lactoylglutathione lyase]]

[[Category: Chen, S]]

[[Category: Chen, Y]]

[[Category: Yuan, M]]

[[Category: Zhai, J]]

[[Category: Zhang, H]]

[[Category: Zhang, L]]

[[Category: Zhao, Y]]

[[Category: Lyase-lyase inhibitor complex]]