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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.
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-NH2
Disulfidebonds:Cys2-Cys16,Cys9-Cys21,andCys15-Cys25
Length(aa):29
Formula:C160H245N47O41S7
MolecularWeight: 3707.48Da
Appearance:Whitelyophilizedsolid
Solubility:aqueousbuffer
CASnumber:notavailable
Source:Synthetic
Purityrate:>98%
Venom-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
matriks/Shikari® (S-ATP) Anti-Pembrolizumab ELISA w/confirmation/PEM-QNS-KEY
intactgenomics/Methionine Auxotrophic LBA4404 | ig® | Intact Genomics/15x50μl/1076-15
goprolytix/Proteolytic Activation of Prothrombin/1 mg, 200 µg/BCT-DFP
novateinbio/Dynorphin A ( 13-17 ) Porcine Peptide/5mg/PE-54024_5mg
matriks/Shikari® (Q-ETA) Etanercept ELISA/ETA-FD-ENB
intactgenomics/Agrobacterium ElectroComponent Combo Pack | Intact Genomics/12x50µl/1290-24
Jackson/Peroxidase AffiniPure Goat Anti-Mouse IgG (H+L)/2.0 ml/115-035-003
Jackson/Peroxidase AffiniPure Goat Anti-Rabbit IgG (H+L)/2.0 ml/111-035-003
Qubit™ dsDNA BR Assay Kit Q32853现货
Invitrogen Q32855 Qubit™ RNA HS Assay Kit现货促销
LUCK-1G,D-Luciferin, Potassium Salt 钾盐现货
GoldBio/D-Luciferin, Sodium Salt (Proven and Published™)/LUCNA-1G/1 g