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2m79
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==[Asp2,11]RTD-1== | |
| + | <StructureSection load='2m79' size='340' side='right'caption='[[2m79]]' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2m79]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2M79 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2M79 FirstGlance]. <br> | ||
| + | </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=2m79 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2m79 OCA], [https://pdbe.org/2m79 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2m79 RCSB], [https://www.ebi.ac.uk/pdbsum/2m79 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2m79 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 2m79" 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]] | ||
Current revision
[Asp2,11]RTD-1
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