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6y1q
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Cortistatin analog with improved immunoregulatory activity== | |
| + | <StructureSection load='6y1q' size='340' side='right'caption='[[6y1q]]' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6y1q]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6Y1Q OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6Y1Q FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DTR:D-TRYPTOPHAN'>DTR</scene>, <scene name='pdbligand=O6H:2,4,6-trimethyl-L-phenylalanine'>O6H</scene>, <scene name='pdbligand=OCA:OCTANOIC+ACID+(CAPRYLIC+ACID)'>OCA</scene></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=6y1q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6y1q OCA], [https://pdbe.org/6y1q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6y1q RCSB], [https://www.ebi.ac.uk/pdbsum/6y1q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6y1q ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Ulcerative colitis and Crohn's disease are forms of inflammatory bowel disease whose incidence and prevalence are increasing worldwide. These diseases lead to chronic inflammation of the gastrointestinal tract as a result of an abnormal response of the immune system. Recent studies positioned Cortistatin, which shows low stability in plasma, as a candidate for IBD treatment. Here, using NMR structural information, we design five Cortistatin analogues adopting selected native Cortistatin conformations in solution. One of them, A5, preserves the anti-inflammatory and immunomodulatory activities of Cortistatin in vitro and in mouse models of the disease. Additionally, A5 displays an increased half-life in serum and a unique receptor binding profile, thereby overcoming the limitations of the native Cortistatin as a therapeutic agent. This study provides an efficient approach to the rational design of Cortistatin analogues and opens up new possibilities for the treatment of patients that fail to respond to other therapies. | ||
| - | + | Structure-based design of a Cortistatin analogue with immunomodulatory activity in models of inflammatory bowel disease.,Rol A, Todorovski T, Martin-Malpartida P, Escola A, Gonzalez-Rey E, Aragon E, Verdaguer X, Valles-Miret M, Farrera-Sinfreu J, Puig E, Fernandez-Carneado J, Ponsati B, Delgado M, Riera A, Macias MJ Nat Commun. 2021 Mar 25;12(1):1869. doi: 10.1038/s41467-021-22076-5. PMID:33767180<ref>PMID:33767180</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 6y1q" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Synthetic construct]] | ||
| + | [[Category: Rol A]] | ||
Current revision
Cortistatin analog with improved immunoregulatory activity
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