NEURONAL CALCIUM-CHANNEL ANTAGONISTS - DISCRIMINATION BETWEEN CALCIUM-CHANNEL SUBTYPES USING OMEGA-CONOTOXIN FROM CONUS-MAGUS VENOM
NEURONAL CALCIUM-CHANNEL ANTAGONISTS - DISCRIMINATION BETWEEN CALCIUM-CHANNEL SUBTYPES USING OMEGA-CONOTOXIN FROM CONUS-MAGUS VENOM
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DOI：
10.1021/bi00382a004
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发表时间：
1987-04-21
期刊：
影响因子：
2.9
通讯作者：
RIVIER, J
中科院分区：
文献类型：
--
作者：
OLIVERA, BM;CRUZ, LJ;RIVIER, J
从猎鱼锥螺的毒液中提取的欧米伽-芋螺毒素可能是目前最有用的脊椎动物神经元钙通道的配体。对其中的两种多肽毒素--魔芋螺毒素MVIIA和MVIIB进行了纯化。氨基酸序列与地理圆锥螺毒素有显著差异。实现了欧米茄-芋螺毒素MVIIA的全合成，并用碘化法制备了具有生物活性的放射性标记毒素。虽然在哺乳动物的脑中，欧米茄-芋螺毒素(GVIA)和魔芋螺毒素(MVIIA)似乎竞争相同的位置，但在两栖动物的脑中，欧米茄-芋螺毒素MVIIA的高亲和力结合具有较窄的特异性。在这个系统中，证明了两种ω-芋螺毒素的组合可以用于生化定义受体亚型，并提示这些亚型对应于神经元钙通道的亚型。
The .omega.-conotoxins from the venom of fish-hunting cone snails are probably the most useful of presently available ligands for neuronal Ca channels from vertebrates. Two of these peptide toxins, .omega.-conotoxins MVIIA and MVIIB from the venom of Conus magus, were purified. The amino acid sequences show significant differences from .omega.-conotoxins from Conus geographus. Total synthesis of .omega.-conotoxin MVIIA was achieved, and biologically active radiolabeled toxin was produced by iodination. Although .omega.-conotoxins from C. geographus (GVIA) and C. magus (MVIIA) appear to compete for the same sites in mammalian brain, in amphibian brain the high-affinity binding of .omega.-conotoxin MVIIA has narrower specificity. In this system, it is demonstrated that a combination of two .omega.-conotoxins can be used for biochemically defining receptor subtypes and suggested that these correspond to subtypes of neuronal Ca2+ channels.