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Smartox/Blocker of Nav1.1 / 1.2 / 1.3 / 1.4 / 1.6 / 1.7/12GSF002-00100/0.1mg
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产品说明
GsAF-II (also termed Kappa-theraphotoxin-Gr2c, GsAF-2) was originally isolated from the venom of Grammostola rosea spider. GsAF-II peptide toxin has antinociceptive and antiarrhythmic effects in mammals. The peptide is reported to block the following voltage-gated sodium channels: Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6 and Nav1.7 with IC50 values of, respectively, 5.7, 12, 24, 4, 6.6 and 1.3 µM. This peptide also blocks hERG1 with an IC50 value of 4.7 µM.
Description:
Product code: N/A.
Category: Sodium channels.
Tags: nav, tetrodotoxin, ttx.
AA sequence: Tyr-Cys2-Gln-Lys-Trp-Met-Trp-Thr-Cys9-Asp-Glu-Glu-Arg-Lys-Cys15-Cys16-Glu-Gly-Leu-Val-Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Lys-Ile-Glu-Trp-OH
Disulfide bonds: Cys2-Cys16, Cys9-Cys21, and Cys15-Cys25)
Length (aa): 31
Formula: C176H261N47O45S7
Molecular Weight: 3979.78 Da
Appearance: White lyophilized solid
Solubility: aqueous buffer
CAS number: not available
Source: Synthetic
Purity rate: > 98%
Reference:Target Promiscuity and Heterogeneous Effects of Tarantula Venom Peptides Affecting Na+ and K+ Ion Channels Venom-derived peptide modulators of ion channel gating are regarded as essential tools for understanding the molecular motions that occur during the opening and closing of ion channels. In this study, we present the characterization of five spider toxins on 12 human voltage-gated ion channels, following observations about the target promiscuity of some spider toxins and the ongoing revision of their “canonical” gating-modifying mode of action. The peptides were purified de novo from the venom of Grammostola rosea tarantulas, and their sequences were confirmed by Edman degradation and mass spectrometry analysis. Their effects on seven tetrodotoxin-sensitive Na(+) channels, the three human ether-à-go-go (hERG)-related K(+) channels, and two human Shaker-related K(+) channels were extensively characterized by electrophysiological techniques. All thepeptides inhibited ion conduction through all the Na(+) channels tested, although with distinctive patterns. The peptides also affected the three pharmaceutically relevant hERG isoforms differently. At higher concentrations, all peptides also modified the gating of the Na(+) channels by shifting the activation to more positive potentials, whereas more complex effects were recorded on hERG channels. No effects were evident on the two Shaker-related K(+) channels at concentrations well above the IC(50) value for the affected channels. Given the sequence diversity of the testedpeptides, we propose that tarantula toxins should be considered both as multimode and target-promiscuous ion channel modulators; both features should not be ignored when extracting mechanistic interpretations about ion channel gating. Our observations could also aid in future structure-function studies and might help the development of novel ion channel-specific drugs.
Elisa Redaelli, et al. (2010) Target Promiscuity and Heterogeneous Effects of Tarantula Venom Peptides Affecting Na+ and K+ Ion Channels. 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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