Huwentoxin-XVIisa39aminoacidspeptidethatwasdiscoveredfromthevenomoftheChinesetarantulaOrnithoctonushuwena.Huwentoxin-XVIwasshowntobeapotentblockerofHVAN-typecalciumchannelswithanIC50valueof60nMinratDRG.Theblockingeffectappearstobesimilartothatofω-conotoxin-GVIAandω-conotoxin-MVIIA.Neverthelss,Huwentoxin-XVIdiffersfromGVIAandMVIIAthankstoitsgreaterreversibilityanditshigherselectivityforN-typeoverP/QtypethanMVIIA.
Productcode:N/A.Category:Highvoltage-gatedCa2+channels.Tags:Cav2.2,N-type.
AAsequence: Cys1-Ile-Gly-Glu-Gly-Val-Pro-Cys8-Asp-Glu-Asn-Asp-Pro-Arg-Cys15-Cys16-Ser-Gly-Leu-Val-Cys21-Leu-Lys-Pro-Thr-Leu-His-Gly-Ile-Trp-Tyr-Lys-Ser-Tyr-Tyr-Cys36-Tyr-Lys-Lys-OH
Disulfidebonds: Cys1-Cys16,Cys8-Cys21andCys15-Cys36
Length(aa):39
Formula: C196H292N50O56S6
Appearance:Whitelyophilizedsolid
MolecularWeight:4437.2Da
CASnumber:Notavailable
Source:Synthetic
Purityrate:>98%
Forresearchuseonly
N-typecalciumchannelsplayimportantrolesinthecontrolofneurotransmissionreleaseandtransmissionofpainsignalstothecentralnervoussystem.Theirselectiveinhibitorsarebelievedtobepotentialdrugsfortreatingchronicpain.Inthisstudy,anovelneurotoxinnamedHuwentoxin-XVI(HWTX-XVI)specificforN-typecalciumchannelswaspurifiedandcharacterizedfromthevenomofChinesetarantulaOrnithoctonushuwena.HWTX-XVIiscomposedof39aminoacidresiduesincludingsixcysteinesthatconstitutethreedisulfidebridges.HWTX-XVIcouldalmostcompletelyblockthetwitchresponseofratvasdeferenstolow-frequencyelectricalstimulation.ElectrophysiologicalassayindicatedthatHWTX-XVIspecificallyinhibitedN-typecalciumchannelsinratdorsalrootganglioncells(IC50∼60 nM).TheinhibitoryeffectofHWTX-XVIonN-typecalciumchannelcurrentswasdose-dependentandsimilartothatofCTx-GVIAandCTx-MVIIA.However,thethreepeptidesexhibitedmarkedlydifferentdegreesofreversibilityafterblock.Thetoxinhadnoeffectonvoltage-gatedT-typecalciumchannels,potassiumchannelsorsodiumchannels.IntraperitonealinjectionofthetoxinHWTX-XVItoratselicitedsignificantanalgesicresponsestoformalin-inducedinflammationpain.Toxintreatmentalsochangedwithdrawallatencyinhotplatetests.Intriguingly,wefoundthatintramuscularinjectionofthetoxinreducedmechanicalallodyniainducedbyincisionalinjuryinVonFreytest.Thus,ourfindingssuggestthattheanalgesicpotencyofHWTX-XVIanditsgreaterreversibilitycouldcontributetothedesignofanovelpotentialanalgesicagentwithhighpotencyandlowsideeffects
DengM.,etal.(2014)Huwentoxin-XVI,ananalgesic,highlyreversiblemammalianN-typecalciumchannelantagonistfromChinesetarantulaOrnithoctonushuwena.Neuropharmacol.
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Smartox Biotechnology 是全球唯一一家专门生产动物毒液多肽毒素，用于细胞离子通道功能研究的生物医药公司。多肽毒素在生物制药领域具有重要的使用价值。Smartox Biotechnology 于 2009 年由来自 Grenoble 神经科学研究所 (Grenoble Institute of Neuroscience) 的 Michel de waard 博士创立, Smartox Biotechnology 专门研究动物毒液，制作合成多种毒液中的多肽成分（常称为毒素）。 De Waard 博士研究离子通道与毒素多肽的关系，尤其是鉴定、开发毒素多肽作为治疗性分子或细胞穿透肽 (cell penetrating peptides, CPP) 。其研究团队在毒液分离，药理性活性肽鉴定、富半胱氨酸肽定性、制作和优化等方面具有独特、丰富的经验。 2010 年， Smartox Biotechnolgy 被法国研究部 (Ministry of Research) 授予“新兴企业 OSEO 奖 (OSEO prize for emerging businesses) ”。
