2xpk
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases== | |
| + | <StructureSection load='2xpk' size='340' side='right'caption='[[2xpk]], [[Resolution|resolution]] 2.40Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2xpk]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Clostridium_perfringens Clostridium perfringens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XPK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XPK FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=Z0M:N-[(5R,6R,7R,8S)-6,7-DIHYDROXY-5-(HYDROXYMETHYL)-2-(2-PHENYLETHYL)-5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRIDIN-8-YL]-3-SULFANYLPROPANAMIDE'>Z0M</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=2xpk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xpk OCA], [https://pdbe.org/2xpk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xpk RCSB], [https://www.ebi.ac.uk/pdbsum/2xpk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xpk ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/OGA_CLOP1 OGA_CLOP1] Biological function unknown. Capable of hydrolyzing the glycosidic link of O-GlcNAcylated proteins. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Posttranslational modification of metazoan nucleocytoplasmic proteins with N-acetylglucosamine (O-GlcNAc) is essential, dynamic, and inducible and can compete with protein phosphorylation in signal transduction. Inhibitors of O-GlcNAcase, the enzyme removing O-GlcNAc, are useful tools for studying the role of O-GlcNAc in a range of cellular processes. We report the discovery of nanomolar OGA inhibitors that are up to 900,000-fold selective over the related lysosomal hexosaminidases. When applied at nanomolar concentrations on live cells, these cell-penetrant molecules shift the O-GlcNAc equilibrium toward hyper-O-GlcNAcylation with EC values down to 3 nM and are thus invaluable tools for the study of O-GlcNAc cell biology. | ||
| - | + | Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases.,Dorfmueller HC, Borodkin VS, Schimpl M, Zheng X, Kime R, Read KD, van Aalten DM Chem Biol. 2010 Nov 24;17(11):1250-5. PMID:21095575<ref>PMID:21095575</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| + | <div class="pdbe-citations 2xpk" style="background-color:#fffaf0;"></div> | ||
| - | + | ==See Also== | |
| + | *[[Beta-Hexosaminidase|Beta-Hexosaminidase]] | ||
| + | *[[Beta-Hexosaminidase 3D structures|Beta-Hexosaminidase 3D structures]] | ||
| + | *[[O-GlcNAcase|O-GlcNAcase]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Clostridium perfringens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Borodkin VS]] | ||
| + | [[Category: Dorfmueller HC]] | ||
| + | [[Category: Kime R]] | ||
| + | [[Category: Read KD]] | ||
| + | [[Category: Schimpl M]] | ||
| + | [[Category: Zheng X]] | ||
| + | [[Category: Van Aalten DMF]] | ||
Current revision
Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases
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