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5t3m

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'''Unreleased structure'''
 
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The entry 5t3m is ON HOLD until Aug 25 2018
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==Solution structure of a triple mutant of HwTx-IV - a potent blocker of Nav1.7==
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<StructureSection load='5t3m' size='340' side='right' caption='[[5t3m]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''>
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Authors: Rahnama, S., Sharma, G., Mobli, M.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5t3m]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5T3M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5T3M FirstGlance]. <br>
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Description: Solution structure of a triple mutant of HwTx-IV -a potent blocker of Nav1.7
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</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=5t3m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5t3m OCA], [http://pdbe.org/5t3m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5t3m RCSB], [http://www.ebi.ac.uk/pdbsum/5t3m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5t3m ProSAT]</span></td></tr>
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[[Category: Unreleased Structures]]
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/TXH4_HAPSC TXH4_HAPSC]] This lethal neurotoxin acts selectively on tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels (Nav), with an IC(50) of 30 nM in rat DRG neurons. Preferentially inhibits neuronal voltage-gated sodium channel subtype hNav1.7/SCN9A (IC(50) is 26 nM), rNav1.2/SCN2A (IC(50) is 150 nM), and rNav1.3/SCN3A (IC(50) is 338 nM), compared with muscle subtypes rNav1.4/SCN4A and hNav1.5/SCN5A (IC(50) is > 10 uM). Inhibits activation of sodium channel by trapping the voltage sensor of domain II of the site 4 in the inward, closed configuration.<ref>PMID:12228241</ref> <ref>PMID:18628201</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: Mobli, M]]
[[Category: Rahnama, S]]
[[Category: Rahnama, S]]
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[[Category: Mobli, M]]
 
[[Category: Sharma, G]]
[[Category: Sharma, G]]
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[[Category: Toxin]]

Revision as of 09:41, 13 September 2017

Solution structure of a triple mutant of HwTx-IV - a potent blocker of Nav1.7

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