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- Middleton,R.E. etal.(2002) Biochemistry 41,14734.
- Hall,E.O. etal.(2010) FASEBJ. 24, 608.14.
- AlomoneLabsProTx-II-BiotininhibitsNaV1.7channelsexpressedin Xenopus oocytes.A.Timecourseof ProTx-II-Biotin (#STP-100-B)inhibitionofNaV1.7channelscurrent.Membranepotentialwasheldat-100mV,currentwaselicitedbya100msvoltagestepto0mVevery10sec,andwassignificantlyinhibitedby200nMProTx-II-Biotin(bar), appliedfor4.5min.B.SuperimposedtracesofNaV1.7currentuponapplicationofcontrolandof200nMProTx-II-Biotin(asindicated),takenfromtherecordingshowninA.AlomoneLabsProTx-II-Biotinspecificallybindsavidin.SDS-PAGEresolvedpurified ProTx-II-Biotin (#STP-100-B)specificallybindsperoxidase-conjugatedavidin,showingadose-dependentECLsignalat~4kDa,absentforthesameamountofunlabeled ProTx-II (#STP-100).
- 1.Middleton,R.E. etal.(2002) Biochemistry 41, 14734.
- 2.Smith,J.J. etal.(2005) J.Biol.Chem. 280, 11127.
- 3.Smith,J.J. etal. (2007) J.Biol.Chem. 282, 12687.
ProTx-IIisapeptidyltoxinoriginallyproducedinThrixopelmapruriens,thePeruviangreenvelvettarantula.Itwasidentifiedasavoltage-gatedNa+channel(NaV)blockerwhichinhibitsbothtetrodotoxin-sensitiveandtetrodotoxin-resistantchannels1.
BindingofProTx-IItoanextracellulardomainofNaVchannel,probablytoahydrophobicsite3,inhibitscurrentbyshiftingthechannelactivationtomorepositivepotentials1-2.
ProTx-IIInhibitsNaV1.2,NaV1.3,NaV1.5,NaV1.6,NaV1.7,andNaV1.8.ItisasignificantlymorepotentinhibitoragainstNaV1.7thantheotherNaVchannelsubtypes1.
ProTx-IIwasalsofoundasaneffectivemodulatorwhichshiftsthevoltagedependenceactivityofT-typeCa2+channel1.
ProTx-II-Biotin(#STP-100-B) isahighlypure,synthetic,andbiologicallyactiveconjugatedpeptidetoxin.
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