4kyh: Difference between revisions
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<StructureSection load='4kyh' size='340' side='right'caption='[[4kyh]], [[Resolution|resolution]] 2.50Å' scene=''> | <StructureSection load='4kyh' size='340' side='right'caption='[[4kyh]], [[Resolution|resolution]] 2.50Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4kyh]] is a 2 chain structure | <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"><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> | </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='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2za0|2za0]], [[4kyk|4kyk]]</ | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2za0|2za0]], [[4kyk|4kyk]]</div></td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Lactoylglutathione_lyase Lactoylglutathione lyase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.4.1.5 4.4.1.5] </span></td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[ | <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> | ||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Function == | == 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;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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[[Category: Lactoylglutathione lyase]] | [[Category: Lactoylglutathione lyase]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Chen, S]] | [[Category: Chen, S]] | ||
[[Category: Chen, Y]] | [[Category: Chen, Y]] |
Revision as of 08:03, 25 August 2022
Crystal structure of mouse glyoxalase I complexed with zopolrestatCrystal structure of mouse glyoxalase I complexed with zopolrestat
Structural highlights
Function[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). Publication Abstract from PubMedOld 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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