2m50: Difference between revisions
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{{STRUCTURE_2m50| PDB=2m50 | SCENE= }} | |||
===Analysis of the structural and molecular basis of voltage-sensitive sodium channel inhibition by the spider toxin, Huwentoxin-IV (-TRTX-Hh2a).=== | |||
==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> | |||
==About this Structure== | |||
[[2m50]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Haplopelma_schmidti Haplopelma schmidti]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2M50 OCA]. | |||
==Reference== | |||
<references group="xtra"/><references/> | |||
[[Category: Haplopelma schmidti]] | |||
[[Category: Flinspach, M.]] | |||
[[Category: Gibbs, A.]] | |||
[[Category: Minassian, N.]] | |||
[[Category: Wickenden, A.]] | |||
[[Category: Toxin]] | |||
[[Category: Venom toxin]] | |||
Revision as of 07:16, 20 June 2013
Analysis of the structural and molecular basis of voltage-sensitive sodium channel inhibition by the spider toxin, Huwentoxin-IV (-TRTX-Hh2a).
Function
[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.[1] [2]
About this Structure
2m50 is a 1 chain structure with sequence from Haplopelma schmidti. Full experimental information is available from OCA.
Reference
- ↑ Peng K, Shu Q, Liu Z, Liang S. Function and solution structure of huwentoxin-IV, a potent neuronal tetrodotoxin (TTX)-sensitive sodium channel antagonist from Chinese bird spider Selenocosmia huwena. J Biol Chem. 2002 Dec 6;277(49):47564-71. Epub 2002 Sep 11. PMID:12228241 doi:10.1074/jbc.M204063200
- ↑ Xiao Y, Bingham JP, Zhu W, Moczydlowski E, Liang S, Cummins TR. Tarantula huwentoxin-IV inhibits neuronal sodium channels by binding to receptor site 4 and trapping the domain ii voltage sensor in the closed configuration. J Biol Chem. 2008 Oct 3;283(40):27300-13. doi: 10.1074/jbc.M708447200. Epub 2008 , Jul 14. PMID:18628201 doi:10.1074/jbc.M708447200
