5abe: Difference between revisions
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''' | ==Structure of GH84 with ligand== | ||
<StructureSection load='5abe' size='340' side='right' caption='[[5abe]], [[Resolution|resolution]] 2.00Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5abe]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5ABE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5ABE FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=XQO:2-[(2S,3S,4R,5R)-5-(HYDROXYMETHYL)-3,4-BIS(OXIDANYL)-1-PENTYL-PYRROLIDIN-2-YL]-N-METHYL-ETHANAMIDE'>XQO</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5abf|5abf]], [[5abg|5abg]], [[5abh|5abh]]</td></tr> | |||
<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=5abe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5abe OCA], [http://pdbe.org/5abe PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5abe RCSB], [http://www.ebi.ac.uk/pdbsum/5abe PDBsum]</span></td></tr> | |||
</table> | |||
== Function == | |||
[[http://www.uniprot.org/uniprot/OGA_BACTN OGA_BACTN]] Biological function unknown. Capable of hydrolyzing the glycosidic link of O-GlcNAcylated proteins. | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Pyrrolidine-based iminocyclitols are a promising class of glycosidase inhibitors. Reported herein is a convenient epimerization strategy that provides direct access to a range of stereoisomeric iminocyclitol inhibitors of O-GlcNAcase (OGA), the enzyme responsible for catalyzing removal of O-GlcNAc from nucleocytoplasmic proteins. Structural details regarding the binding of these inhibitors to a bacterial homologue of OGA reveal the basis for potency. These compounds are orally available and permeate into rodent brain to increase O-GlcNAc, and should prove useful tools for studying the role of OGA in health and disease. | |||
A Convenient Approach to Stereoisomeric Iminocyclitols: Generation of Potent Brain-Permeable OGA Inhibitors.,Bergeron-Brlek M, Goodwin-Tindall J, Cekic N, Roth C, Zandberg WF, Shan X, Varghese V, Chan S, Davies GJ, Vocadlo DJ, Britton R Angew Chem Int Ed Engl. 2015 Nov 6. doi: 10.1002/anie.201507985. PMID:26545827<ref>PMID:26545827</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 5abe" style="background-color:#fffaf0;"></div> | |||
[[Category: | == References == | ||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Bergeron-Brlek, M]] | |||
[[Category: Britton, R]] | [[Category: Britton, R]] | ||
[[Category: Cekic, N]] | |||
[[Category: Chan, S]] | [[Category: Chan, S]] | ||
[[Category: Davies, G J]] | |||
[[Category: Goodwin-Tindall, J]] | |||
[[Category: Roth, C]] | |||
[[Category: Shan, X]] | |||
[[Category: Varghese, V]] | [[Category: Varghese, V]] | ||
[[Category: | [[Category: Vocadlo, D J]] | ||
[[Category: | [[Category: Zandberg, W F]] | ||
[[Category: | [[Category: Hydrolase]] | ||
[[Category: | [[Category: Inhibitor]] | ||
[[Category: | [[Category: Tim-barrel]] | ||
