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6wqr
From Proteopedia
(Difference between revisions)
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==NMR solution structure of leech peptide HSTX-I== | ==NMR solution structure of leech peptide HSTX-I== | ||
| - | <StructureSection load='6wqr' size='340' side='right'caption='[[6wqr]]' scene=''> | + | <StructureSection load='6wqr' size='340' side='right'caption='[[6wqr]], [[NMR_Ensembles_of_Models | 21 NMR models]]' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full | + | <table><tr><td colspan='2'>[[6wqr]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6WQR OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6WQR FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6wqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wqr OCA], [http://pdbe.org/6wqr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6wqr RCSB], [http://www.ebi.ac.uk/pdbsum/6wqr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6wqr ProSAT]</span></td></tr> | + | </td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></td></tr> |
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6wqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wqr OCA], [http://pdbe.org/6wqr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6wqr RCSB], [http://www.ebi.ac.uk/pdbsum/6wqr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6wqr ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The role of voltage-gated sodium (NaV) channels in pain perception is indisputable. Of particular interest as targets for the development of pain therapeutics are the tetrodotoxin-resistant isoforms NaV1.8 and NaV1.9, based on animal as well as human genetic studies linking these ion channel subtypes to the pathogenesis of pain. However, only a limited number of inhibitors selectively targeting these channels have been reported. HSTX-I is a peptide toxin identified from saliva of the leech Haemadipsa sylvestris. The native 23-residue peptide, stabilised by two disulfide bonds, has been reported to inhibit rat NaV1.8 and mouse NaV1.9 with low micromolar activity, and may therefore represent a scaffold for development of novel modulators with activity at human tetrodotoxin-resistant NaV isoforms. We synthetically produced this hydrophobic peptide in high yield using a one-pot oxidation and single step purification and determined the three-dimensional solution structure of HSTX-I using NMR solution spectroscopy. However, in our hands, the synthetic HSTX-I displayed only very modest activity at human NaV1.8 and NaV1.9, and lacked analgesic efficacy in a murine model of inflammatory pain. | ||
| + | |||
| + | Pharmacological activity and NMR solution structure of the leech peptide HSTX-I.,McMahon KL, Tay B, Deuis JR, Tanaka BS, Peigneur S, Jin AH, Tytgat J, Waxman SG, Dib-Hajj SD, Vetter I, Schroeder CI Biochem Pharmacol. 2020 Jun 7:114082. doi: 10.1016/j.bcp.2020.114082. PMID:32524995<ref>PMID:32524995</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6wqr" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: McMahon | + | [[Category: McMahon, K L]] |
| - | [[Category: Schroeder | + | [[Category: Schroeder, C I]] |
| + | [[Category: Antiparallel beta-sheet]] | ||
| + | [[Category: Disulfide-rich]] | ||
| + | [[Category: Hydrophobic]] | ||
| + | [[Category: Toxin]] | ||
Revision as of 20:50, 28 October 2020
NMR solution structure of leech peptide HSTX-I
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