View source for 2xpk


==Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases==
<StructureSection load='2xpk' size='340' side='right'caption='[[2xpk]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2xpk]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/"bacillus_perfringens"_veillon_and_zuber_1898 "bacillus perfringens" veillon and zuber 1898]. 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://proteopedia.org/fgij/fg.htm?mol=2XPK FirstGlance]. <br>
</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='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>
<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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2xpk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xpk OCA], [http://pdbe.org/2xpk PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2xpk RCSB], [http://www.ebi.ac.uk/pdbsum/2xpk PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2xpk ProSAT]</span></td></tr>
</table>
== Function ==
[[http://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&reg;/PubMed&reg;, 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]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Bacillus perfringens veillon and zuber 1898]]
[[Category: Beta-N-acetylhexosaminidase]]
[[Category: Large Structures]]
[[Category: Aalten, D M.F van]]
[[Category: Borodkin, V S]]
[[Category: Dorfmueller, H C]]
[[Category: Kime, R]]
[[Category: Read, K D]]
[[Category: Schimpl, M]]
[[Category: Zheng, X]]
[[Category: Hydrolase]]
[[Category: Signalling]]