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5tcz

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'''Unreleased structure'''
 
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The entry 5tcz is ON HOLD until Paper Publication
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==NMR solution structure of engineered Protoxin-II analog==
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<StructureSection load='5tcz' size='340' side='right'caption='[[5tcz]]' scene=''>
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Authors: Gibbs, A.C., Wickenden, A.D.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5tcz]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Thrixopelma_pruriens Thrixopelma pruriens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TCZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5TCZ FirstGlance]. <br>
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Description: NMR solution structure of engineered Protoxin-II analog
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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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[[Category: Unreleased Structures]]
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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=5tcz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tcz OCA], [https://pdbe.org/5tcz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5tcz RCSB], [https://www.ebi.ac.uk/pdbsum/5tcz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5tcz ProSAT]</span></td></tr>
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[[Category: Gibbs, A.C]]
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</table>
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[[Category: Wickenden, A.D]]
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== Function ==
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[https://www.uniprot.org/uniprot/TXPR2_THRPR TXPR2_THRPR] Blocks both tetrodotoxin-sensitive and tetrodotoxin-resistant human voltage-gated sodium channels by shifting the voltage dependence of channel activation to more positive potentials. Inhibits Nav1.2/SCN2A, Nav1.3/SCN3A, Nav1.5/SCN5A, Nav1.6/SCN8A, Nav1.7/SCN9A, Nav1.8/SCN10A. Is significantly more potent against Nav1.7/SCN9A than the other Nav channel subtypes. Has no significant effect on Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.5/KCNA5, and Kv2.1/KCNB1 channels. Also inhibits Cav1.2/CACNA1C and Cav3.1/CACNA1G channels with an IC(50) around 100 nM. Does not bind to the pharmacologically defined Nav channel sites 3 or 4. Neutralization of gating charges in the voltage sensor (S4) of domain II of Nav1.2/SCN2A prevents the effect of the toxin on gating current. Thus, it has been suggested that the toxin acts by trapping the voltage sensor of Nav channel domain II in the resting state, impeding outward gating movement of the IIS4 transmembrane segment of the channel. Binds to phospholipids.<ref>PMID:12475222</ref> <ref>PMID:17087985</ref> <ref>PMID:17339321</ref> <ref>PMID:18156314</ref> <ref>PMID:18657562</ref> <ref>PMID:18728100</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
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[[Category: Thrixopelma pruriens]]
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[[Category: Gibbs AC]]
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[[Category: Wickenden AD]]

Current revision

NMR solution structure of engineered Protoxin-II analog

PDB ID 5tcz

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