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Application of Physiologically Active Substances Isolated from Natural Resources to Pharmacological Studies

机译:从自然资源中提取的生理活性物质在药理研究中的应用

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References(142) Cited-By(42) Numerous neurotoxins that alter Na+-channel function have been shown to be useful tools for characterizing Na+ channels. Polypeptide blockers of voltage-dependent K+ channels (dendrotoxins, etc.) and Ca2+ -activated K+ channels (apamine, etc.) have been studied extensively by numerous investigators. Peptide toxins, calciseptine and ω-conotoxins have been attracting much attention as inhibitors of L-type and N-type Ca2+ channels, respectively, while ω-conotoxins-MVIIC and ω-agatoxin IVA have been used as new types of Ca2+ -channel blockers. Ryanodine and bromoeudistomin D analogues have been extensively used to elucidate Ca2+ -release-channel functions and to purify its target protein. Polypeptide toxins (myotoxin α, etc.) and macrolides (FK 506, etc.) are useful Ca2+ releasers with a novel mechanism, while natural products such as thapsigargin and gingerol have been used as modulators of Ca2+ -pumping ATPase. Some modulators of the function of myosin (purealin, etc.) and actin (goniodomin A, etc.)have been demonstrated to be important chemical probes for understanding the physiological roles of the contractile proteins in structural changes and their interaction in muscle contraction. A large number of protein kinase inhibitors (staurosporine, etc.) and phosphatase inhibitors (okadaic acid, etc.)are widely used as first-choice reagents for studying protein phosphorylation. These natural products have become essential tools for studying the regulatory mechanism of cellular ion movements, muscle contraction and protein phosphorylation.
机译:参考文献(142)被引用的By(42)改变Na +通道功能的多种神经毒素已被证明是表征Na +通道的有用工具。众多研究者已经广泛研究了电压依赖性K +通道(树突毒素等)和Ca2 +激活的K +通道(阿帕明等)的多肽阻滞剂。作为L型和N型Ca2 +通道的抑制剂,肽毒素,钙环素和ω-芋螺毒素已引起了广泛的关注,而ω-芋螺毒素MVIIC和ω-毒素IVA已被用作新型的Ca2 +信道阻断剂。 Ryanodine和bromoeudistomin D类似物已被广泛用于阐明Ca2 +释放通道的功能并纯化其靶蛋白。多肽毒素(肌毒素α等)和大环内酯类(FK 506等)是具有新颖机制的有用的Ca2 +释放剂,而天然产物(如毒胡萝卜素和姜黄素)已被用作Ca2 +泵浦ATPase的调节剂。肌球蛋白(肌钙蛋白等)和肌动蛋白(促性腺激素A等)功能的某些调节剂已被证明是重要的化学探针,可用于了解收缩蛋白在结构变化中的生理作用及其在肌肉收缩中的相互作用。大量的蛋白激酶抑制剂(星形孢菌素等)和磷酸酶抑制剂(冈田酸等)被广泛用作研究蛋白磷酸化的首选试剂。这些天然产物已成为研究细胞离子运动,肌肉收缩和蛋白质磷酸化调控机制的重要工具。

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