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2xpk

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[[Image:2xpk.png|left|200px]]
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==CELL-PENETRANT, NANOMOLAR O-GLCNACASE INHIBITORS SELECTIVE AGAINST LYSOSOMAL HEXOSAMINIDASES==
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<StructureSection load='2xpk' size='340' side='right' caption='[[2xpk]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2xpk]] is a 2 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XPK FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2cbi|2cbi]], [[2vur|2vur]], [[2x0y|2x0y]], [[2j62|2j62]], [[2wb5|2wb5]], [[2jh2|2jh2]], [[2v5c|2v5c]], [[2cbj|2cbj]], [[2v5d|2v5d]]</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Beta-N-acetylhexosaminidase Beta-N-acetylhexosaminidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.52 3.2.1.52] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2xpk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xpk OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xpk RCSB], [http://www.ebi.ac.uk/pdbsum/2xpk PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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{{STRUCTURE_2xpk| PDB=2xpk | SCENE= }}
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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>
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===CELL-PENETRANT, NANOMOLAR O-GLCNACASE INHIBITORS SELECTIVE AGAINST LYSOSOMAL HEXOSAMINIDASES===
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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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{{ABSTRACT_PUBMED_21095575}}
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==About this Structure==
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[[2xpk]] is a 2 chain structure with sequence from [http://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].
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==See Also==
==See Also==
*[[Beta-Hexosaminidase|Beta-Hexosaminidase]]
*[[Beta-Hexosaminidase|Beta-Hexosaminidase]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:021095575</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Beta-N-acetylhexosaminidase]]
[[Category: Beta-N-acetylhexosaminidase]]
[[Category: Clostridium perfringens]]
[[Category: Clostridium perfringens]]

Revision as of 13:11, 22 October 2014

CELL-PENETRANT, NANOMOLAR O-GLCNACASE INHIBITORS SELECTIVE AGAINST LYSOSOMAL HEXOSAMINIDASES

2xpk, resolution 2.40Å

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