2m77: Difference between revisions
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New page: '''Unreleased structure''' The entry 2m77 is ON HOLD Authors: Conibear, A.C., Bochen, A., Rosengren, K., Kessler, H., Craik, D.J. Description: [Asp2]RTD-1 |
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==[Asp2]RTD-1== | |||
<StructureSection load='2m77' size='340' side='right'caption='[[2m77]]' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2m77]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2M77 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2M77 FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2m77 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2m77 OCA], [https://pdbe.org/2m77 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2m77 RCSB], [https://www.ebi.ac.uk/pdbsum/2m77 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2m77 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Peptides have the specificity and size required to target the protein-protein interactions involved in many diseases. Some cyclic peptides have been utilised as scaffolds for peptide drugs because of their stability; however, other cyclic peptide scaffolds remain to be explored. theta-Defensins are cyclic peptides from mammals; they are characterised by a cyclic cystine ladder motif and have low haemolytic and cytotoxic activity. Here we demonstrate the potential of the cyclic cystine ladder as a scaffold for peptide drug design by introducing the integrin-binding Arg-Gly-Asp (RGD) motif into the theta-defensin RTD-1. The most active analogue had an IC50 of 18 nM for the alphav beta3 integrin as well as high serum stability, thus demonstrating that a desired bioactivity can be imparted to the cyclic cystine ladder. This study highlights how theta-defensins can provide a stable and conformationally restrained scaffold for bioactive epitopes in a beta-strand or turn conformation. Furthermore, the symmetry of the cyclic cystine ladder presents the opportunity to design peptides with dual bioactive epitopes to increase activity and specificity. | |||
The Cyclic Cystine Ladder of Theta-Defensins as a Stable, Bifunctional Scaffold: A Proof-of-Concept Study Using the Integrin-Binding RGD Motif.,Conibear AC, Bochen A, Rosengren KJ, Stupar P, Wang C, Kessler H, Craik DJ Chembiochem. 2014 Feb 10;15(3):451-9. doi: 10.1002/cbic.201300568. Epub 2014 Jan , 2. PMID:24382674<ref>PMID:24382674</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 2m77" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Large Structures]] | |||
[[Category: Bochen A]] | |||
[[Category: Conibear AC]] | |||
[[Category: Craik DJ]] | |||
[[Category: Kessler H]] | |||
[[Category: Rosengren K]] | |||
