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Biochemical and Electrophysiological Characterization of Two Sea Anemone Type 1 Potassium Toxins from a Geographically Distant Population of Bunodosoma caissarum

机译:地理分布的布氏多孢子虫中两种海葵1型钾毒素的生化和电生理特性

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摘要

Sea anemone (Cnidaria, Anthozoa) venom is an important source of bioactive compounds used as tools to study the pharmacology and structure-function of voltage-gated K+ channels (KV). These neurotoxins can be divided into four different types, according to their structure and mode of action. In this work, for the first time, two toxins were purified from the venom of Bunodosoma caissarum population from Saint Peter and Saint Paul Archipelago, Brazil. Sequence alignment and phylogenetic analysis reveals that BcsTx1 and BcsTx2 are the newest members of the sea anemone type 1 potassium channel toxins. Their functional characterization was performed by means of a wide electrophysiological screening on 12 different subtypes of KV channels (KV1.1–KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG and Shaker IR). BcsTx1 shows a high affinity for rKv1.2 over rKv1.6, hKv1.3, Shaker IR and rKv1.1, while Bcstx2 potently blocked rKv1.6 over hKv1.3, rKv1.1, Shaker IR and rKv1.2. Furthermore, we also report for the first time a venom composition and biological activity comparison between two geographically distant populations of sea anemones.
机译:海葵(Cnidaria,Anthozoa)毒液是生物活性化合物的重要来源,可作为研究电压门控K + 通道(KV)的药理学和结构功能的工具。根据它们的结构和作用方式,这些神经毒素可以分为四种不同的类型。在这项工作中,首次从巴西圣彼得和圣保罗群岛的布氏疟原虫种群的毒液中纯化了两种毒素。序列比对和系统发育分析表明,BcsTx1和BcsTx2是1型海葵钾通道毒素的最新成员。通过对12种不同的KV通道亚型(KV1.1–KV1.6; KV2.1; KV3.1; KV4.2; KV4.3; hERG和Shaker IR)进行广泛的电生理筛选,对它们进行功能表征。与rKv1.6,hKv1.3,Shaker IR和rKv1.1相比,BcsTx1对rKv1.2表现出高度亲和力,而Bcstx2在hKv1.3,rKv1.1,Shaker IR和rKv1.2上有效地阻断了rKv1.6。此外,我们还首次报告了两个地理上相距遥远的海葵种群之间的毒液组成和生物活性比较。

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