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2ybt

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[[Image:2ybt.png|left|200px]]
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==CRYSTAL STRUCTURE OF HUMAN ACIDIC CHITINASE IN COMPLEX WITH BISDIONIN C==
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<StructureSection load='2ybt' size='340' side='right' caption='[[2ybt]], [[Resolution|resolution]] 2.22&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2ybt]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YBT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2YBT 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=DW0:1,1-PROPANE-1,3-DIYLBIS(3,7-DIMETHYL-3,7-DIHYDRO-1H-PURINE-2,6-DIONE)'>DW0</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2ybu|2ybu]]</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/Chitinase Chitinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.14 3.2.1.14] </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=2ybt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ybt OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2ybt RCSB], [http://www.ebi.ac.uk/pdbsum/2ybt 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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Acidic mammalian chitinase (AMCase) is produced in the lung during allergic inflammation and asthma, and inhibition of enzymatic activity has been considered as a therapeutic strategy. However, most chitinase inhibitors are nonselective, additionally inhibiting chitotriosidase activity. Here, we describe bisdionin F, a competitive AMCase inhibitor with 20-fold selectivity for AMCase over chitotriosidase, designed by utilizing the AMCase crystal structure and dicaffeine scaffold. In a murine model of allergic inflammation, bisdionin F-treatment attenuated chitinase activity and alleviated the primary features of allergic inflammation including eosinophilia. However, selective AMCase inhibition by bisdionin F also caused dramatic and unexpected neutrophilia in the lungs. This class of inhibitor will be a powerful tool to dissect the functions of mammalian chitinases in disease and represents a synthetically accessible scaffold to optimize inhibitory properties in terms of airway inflammation.
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{{STRUCTURE_2ybt| PDB=2ybt | SCENE= }}
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Analyzing Airway Inflammation with Chemical Biology: Dissection of Acidic Mammalian Chitinase Function with a Selective Drug-like Inhibitor.,Sutherland TE, Andersen OA, Betou M, Eggleston IM, Maizels RM, van Aalten D, Allen JE Chem Biol. 2011 May 27;18(5):569-79. PMID:21609838<ref>PMID:21609838</ref>
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===CRYSTAL STRUCTURE OF HUMAN ACIDIC CHITINASE IN COMPLEX WITH BISDIONIN C===
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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_21609838}}
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== References ==
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<references/>
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==About this Structure==
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__TOC__
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[[2ybt]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YBT OCA].
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</StructureSection>
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==See Also==
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*[[Chitinase|Chitinase]]
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==Reference==
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<ref group="xtra">PMID:021609838</ref><references group="xtra"/>
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[[Category: Chitinase]]
[[Category: Chitinase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]

Revision as of 11:54, 29 October 2014

CRYSTAL STRUCTURE OF HUMAN ACIDIC CHITINASE IN COMPLEX WITH BISDIONIN C

2ybt, resolution 2.22Å

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