4pj6: Difference between revisions
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''' | ==Crystal Structure of Human Insulin Regulated Aminopeptidase with Lysine in Active Site== | ||
<StructureSection load='4pj6' size='340' side='right' caption='[[4pj6]], [[Resolution|resolution]] 2.96Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4pj6]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4PJ6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4PJ6 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LYS:LYSINE'>LYS</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cystinyl_aminopeptidase Cystinyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.3 3.4.11.3] </span></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=4pj6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4pj6 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4pj6 RCSB], [http://www.ebi.ac.uk/pdbsum/4pj6 PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Insulin-regulated aminopeptidase (IRAP, or oxytocinase) is a membrane-bound zinc- metallopeptidase that cleaves neuroactive peptides in the brain and produces memory enhancing effects when inhibited. We have determined the crystal structure of human IRAP revealing a closed, four domain arrangement with a large, mostly buried cavity abutting the active site. The structure reveals that the GAMEN exopeptidase loop adopts a very different conformation from other aminopeptidases, thus explaining IRAP's unique specificity for cyclic peptides such as oxytocin and vasopressin. Computational docking of a series of IRAP-specific cognitive enhancers into the crystal structure provides a molecular basis for their structure-activity relationships and demonstrates that the structure will be a powerful tool in the development of new classes of cognitive enhancers for treating a variety of memory disorders such as Alzheimer's disease. This article is protected by copyright. All rights reserved. | |||
Crystal structure of human insulin-regulated aminopeptidase with specificity for cyclic peptides.,Hermans SJ, Ascher DB, Hancock NC, Holien JK, Michell BJ, Chai SY, Morton CJ, Parker MW Protein Sci. 2014 Nov 18. doi: 10.1002/pro.2604. PMID:25408552<ref>PMID:25408552</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Cystinyl aminopeptidase]] | |||
[[Category: Ascher, D B]] | |||
[[Category: Hancock, N C]] | |||
[[Category: Hermans, S J]] | |||
[[Category: Holien, J K]] | |||
[[Category: Michell, B]] | |||
[[Category: Morton, C J]] | |||
[[Category: Parker, M W]] | |||
[[Category: Aminopeptidase]] | |||
[[Category: Hydrolase]] | |||
[[Category: Metalloprotease]] | |||