8cjr
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 8cjr is ON HOLD Authors: Landon, C., Meudal, H. Description: JzTx-34 toxin peptide W25A mutant Category: Unreleased Structures [[Category: Meud...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==JzTx-34 toxin peptide W25A mutant== | |
| + | <StructureSection load='8cjr' size='340' side='right'caption='[[8cjr]]' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[8cjr]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Chilobrachys Chilobrachys]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8CJR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8CJR FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 10 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=8cjr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8cjr OCA], [https://pdbe.org/8cjr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8cjr RCSB], [https://www.ebi.ac.uk/pdbsum/8cjr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8cjr ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Na(v)1.1 is an important pharmacological target as this voltage-gated sodium channel is involved in neurological and cardiac syndromes. Channel activators are actively sought to try to compensate for haploinsufficiency in several of these pathologies. Herein we used a natural source of new peptide compounds active on ion channels and screened for drugs capable to inhibit channel inactivation as a way to compensate for decreased channel function. We discovered that JzTx-34 is highly active on Na(v)1.1 and subsequently performed a full structure-activity relationship investigation to identify its pharmacophore. These experiments will help interpret the mechanism of action of this and formerly identified peptides as well as the future identification of new peptides. We also reveal structural determinants that make natural ICK peptides active against Na(v)1.1 challenging to synthesize. Altogether, the knowledge gained by this study will help facilitate the discovery and development of new compounds active on this critical ion channel target. | ||
| - | + | Structure-function relationship of new peptides activating human Na(v)1.1.,Lopez L, De Waard S, Meudal H, Caumes C, Khakh K, Peigneur S, Oliveira-Mendes B, Lin S, De Waele J, Montnach J, Cestele S, Tessier A, Johnson JP, Mantegazza M, Tytgat J, Cohen C, Beroud R, Bosmans F, Landon C, De Waard M Biomed Pharmacother. 2023 Sep;165:115173. doi: 10.1016/j.biopha.2023.115173. Epub , 2023 Jul 13. PMID:37453200<ref>PMID:37453200</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 8cjr" style="background-color:#fffaf0;"></div> |
| - | [[Category: Landon | + | == References == |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Chilobrachys]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Landon C]] | ||
| + | [[Category: Meudal H]] | ||
Current revision
JzTx-34 toxin peptide W25A mutant
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