5t3m: Difference between revisions
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==Solution structure of a triple mutant of HwTx-IV - a potent blocker of Nav1.7== | |||
<StructureSection load='5t3m' size='340' side='right' caption='[[5t3m]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''> | |||
== Structural highlights == | |||
<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> | |||
</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> | |||
[[Category: | </table> | ||
== Function == | |||
[[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> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Mobli, M]] | |||
[[Category: Rahnama, S]] | [[Category: Rahnama, S]] | ||
[[Category: Sharma, G]] | [[Category: Sharma, G]] | ||
[[Category: Toxin]] | |||