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Smartox/GsAF-1 blocks voltage-gated sodium channels/12GSF001-00500/0.5mg
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产品说明
GsAF-1(alsotermedβ-theraphotoxin-Gr1b,GsAF-I)wasoriginallyisolatedfromthevenomofGrammostolaroseaspider.GsAF-Ipeptidetoxinisreportedtoblockthefollowingvoltage-gatedsodiumchannelisoforms:Nav1.1,Nav1.2,Nav1.3,Nav1.4,Nav1.6andNav1.7withrespectiveIC50valuesof 0.4,0.6,1.3,0.3,1.2and0.04µM.Inaddition,thetoxinblocksthehERG1isoformwithanIC50valueof4.8µM.Description:Productcode:N/A.Category:Sodiumchannels.Tags:nav,tetrodotoxin,ttx.AAsequence:Tyr-Cys2-Gln-Lys-Trp-Leu-Trp-Thr-Cys9-Asp-Ser-Glu-Arg-Lys-Cys15-Cys16-Glu-Asp-Met-Val-Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Arg-Leu-NH2Disulfidebonds:Cys2-Cys16,Cys9-Cys21,andCys15-Cys25Length(aa):29Formula:C160H245N47O41S7MolecularWeight: 3707.48DaAppearance:WhitelyophilizedsolidSolubility:aqueousbufferCASnumber:notavailableSource:SyntheticPurityrate:>98%Reference:TargetPromiscuityandHeterogeneousEffectsofTarantulaVenomPeptidesAffectingNa+andK+IonChannelsVenom-derivedpeptidemodulatorsofionchannelgatingareregardedasessentialtoolsforunderstandingthemolecularmotionsthatoccurduringtheopeningandclosingofionchannels.Inthisstudy,wepresentthecharacterizationoffivespidertoxinson12humanvoltage-gatedionchannels,followingobservationsaboutthetargetpromiscuityofsomespidertoxinsandtheongoingrevisionoftheir“canonical”gating-modifyingmodeofaction.Thepeptideswerepurified denovo fromthevenomof Grammostolarosea tarantulas,andtheirsequenceswereconfirmedbyEdmandegradationandmassspectrometryanalysis.Theireffectsonseventetrodotoxin-sensitiveNa+ channels,thethreehuman ether-à-go-go (hERG)-relatedK+ channels,andtwohuman Shaker-relatedK+ channelswereextensivelycharacterizedbyelectrophysiologicaltechniques.AllthepeptidesinhibitedionconductionthroughalltheNa+channelstested,althoughwithdistinctivepatterns.ThepeptidesalsoaffectedthethreepharmaceuticallyrelevanthERGisoformsdifferently.Athigherconcentrations,allpeptidesalsomodifiedthegatingoftheNa+ channelsbyshiftingtheactivationtomorepositivepotentials,whereasmorecomplexeffectswererecordedonhERGchannels.Noeffectswereevidentonthetwo Shaker-relatedK+ channelsatconcentrationswellabovetheIC50 valuefortheaffectedchannels.Giventhesequencediversityofthetestedpeptides,weproposethattarantulatoxinsshouldbeconsideredbothasmultimodeandtarget-promiscuousionchannelmodulators;bothfeaturesshouldnotbeignoredwhenextractingmechaNISTicinterpretationsaboutionchannelgating.Ourobservationscouldalsoaidinfuturestructure-functionstudiesandmighthelpthedevelopmentofnovelionchannel-specificdrugs.ELISARedaelli,etal.(2010)TargetPromiscuityandHeterogeneousEffectsofTarantulaVenomPeptidesAffectingNa+andK+IonChannels.JBC.PMID:19955179
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) ”。
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