7knn

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'''Unreleased structure'''
 
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The entry 7knn is ON HOLD until Paper Publication
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==Solution structure of the alpha-conotoxin analogue [2-8]-alkyne Vc1.1==
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<StructureSection load='7knn' size='340' side='right'caption='[[7knn]]' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[7knn]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Conus_victoriae Conus victoriae]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7KNN OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7KNN FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ABA:ALPHA-AMINOBUTYRIC+ACID'>ABA</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7knn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7knn OCA], [https://pdbe.org/7knn PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7knn RCSB], [https://www.ebi.ac.uk/pdbsum/7knn PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7knn ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/CA1A_CONVC CA1A_CONVC] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This synthetic peptide (produced without hydroxyproline, nor 4-carboxyglutamate) is a neuronal nAChR antagonist that acts as a powerful analgesic. It blocks nAChRs composed of alpha-3 or -5/beta-2 (IC(50)=7.2 uM), alpha-3/beta-2 (IC(50)=7.3 uM), alpha-3/beta-4 (IC(50)=4.2 uM), alpha-3 or -5/beta-4 (IC(50)<30 uM), alpha-4/beta-2 (IC(50)<30 uM), alpha-4/beta-4 (IC(50)<30 uM) and alpha/beta/gamma/delta (IC(50)<30 uM) subunits.<ref>PMID:12779345</ref> <ref>PMID:15770155</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Several Conus-derived venom peptides are promising lead compounds for the management of neuropathic pain, with alpha-conotoxins being of particular interest. Modification of the interlocked disulfide framework of alpha-conotoxin Vc1.1 has been achieved using on-resin alkyne metathesis. Although introduction of a metabolically stable alkyne motif significantly disrupts backbone topography, the structural modification generates a potent and selective GABAB receptor agonist that inhibits Cav2.2 channels and exhibits dose-dependent reversal of mechanical allodynia in a behavioral rat model of neuropathic pain. The findings herein support the hypothesis that analgesia can be achieved via activation of GABABRs expressed in dorsal root ganglion (DRG) sensory neurons.
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Authors: MacRaild, C.A., Robinson, S.D., Chhabra, S., Norton, R.S.
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Alkyne-Bridged alpha-Conotoxin Vc1.1 Potently Reverses Mechanical Allodynia in Neuropathic Pain Models.,Belgi A, Burnley JV, MacRaild CA, Chhabra S, Elnahriry KA, Robinson SD, Gooding SG, Tae HS, Bartels P, Sadeghi M, Zhao FY, Wei H, Spanswick D, Adams DJ, Norton RS, Robinson AJ J Med Chem. 2021 Mar 25;64(6):3222-3233. doi: 10.1021/acs.jmedchem.0c02151. Epub , 2021 Mar 16. PMID:33724033<ref>PMID:33724033</ref>
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Description: Solution structure of the alpha-conotoxin analogue [2-8]-alkyne Vc1.1
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Macraild, C.A]]
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<div class="pdbe-citations 7knn" style="background-color:#fffaf0;"></div>
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[[Category: Chhabra, S]]
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== References ==
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[[Category: Robinson, S.D]]
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<references/>
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[[Category: Norton, R.S]]
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__TOC__
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</StructureSection>
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[[Category: Conus victoriae]]
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[[Category: Large Structures]]
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[[Category: Chhabra S]]
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[[Category: MacRaild CA]]
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[[Category: Norton RS]]
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[[Category: Robinson SD]]

Current revision

Solution structure of the alpha-conotoxin analogue [2-8]-alkyne Vc1.1

PDB ID 7knn

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