5do6
From Proteopedia
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| - | ''' | + | ==Crystal structure of Dendroaspis polylepis venom mambalgin-1 T23A mutant== |
| + | <StructureSection load='5do6' size='340' side='right' caption='[[5do6]], [[Resolution|resolution]] 1.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5do6]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DO6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DO6 FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=PGO:S-1,2-PROPANEDIOL'>PGO</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2mjy|2mjy]], [[2mfa|2mfa]]</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5do6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5do6 OCA], [http://pdbe.org/5do6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5do6 RCSB], [http://www.ebi.ac.uk/pdbsum/5do6 PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Mambalgins are peptides isolated from mamba venom that specifically inhibit a set of acid-sensing ion channels (ASICs) to relieve pain. We show here the first full stepwise solid-phase peptide synthesis of mambalgin-1 and confirm the biological activity of the synthetic toxin both in vitro and in vivo. We also report the determination of its 3D crystal structure showing differences with previously described NMR structures. Finally, the functional domain by which the toxin inhibits ASIC1a channels was identified in its loop II and more precisely in the face containing Phe27, Leu32 and Leu34 residues. Moreover, proximity between Leu32 in mambalgin-1 and Phe350 in rASIC1a was proposed from double-mutant cycle analysis. These data give information on the structure and on the pharmacophore for ASIC channel inhibition by mambalgins that could have therapeutic value against pain and probably other neurological disorders. | ||
| - | + | Mambalgin-1 pain-relieving peptide: stepwise solid-phase synthesis, crystal structure and functional domain for acid-sensing ion channel 1a inhibition.,Mourier G, Salinas M, Kessler P, Stura EA, Leblanc M, Tepshi L, Besson T, Diochot S, Baron A, Douguet D, Lingueglia E, Servent D J Biol Chem. 2015 Dec 17. pii: jbc.M115.702373. PMID:26680001<ref>PMID:26680001</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 5do6" style="background-color:#fffaf0;"></div> | |
| - | + | == References == | |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Gilles, M]] | [[Category: Gilles, M]] | ||
[[Category: Kessler, P]] | [[Category: Kessler, P]] | ||
| + | [[Category: Servent, D]] | ||
| + | [[Category: Stura, E A]] | ||
[[Category: Tepshi, L]] | [[Category: Tepshi, L]] | ||
| - | [[Category: | + | [[Category: Acid sensing ion channel]] |
| - | [[Category: | + | [[Category: Elapid venom polypeptide]] |
| + | [[Category: Pain suppression drug]] | ||
| + | [[Category: Toxin]] | ||
Revision as of 19:28, 30 December 2015
Crystal structure of Dendroaspis polylepis venom mambalgin-1 T23A mutant
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