[The role of peptidic toxins in the pharmacological approach of the diversity of calcium channels].

J L Morel, M Hugues
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Abstract

Peptidic toxins extracted from spider, marine snails or snakes venoms, have considerably helped the pharmacological characterization of calcium channels. They have successfully been used for calcium channels mapping. However, the actual situation remains unclear. Genetic investigations demonstrated the existence of a great number of types or sub-types of calcium channels. In recent year a large number of toxins have been purified. Many of these toxins have specific actions on calcium channels and have been used as powerful tools in pharmacological approaches of calcium channels. However the pharmacology of the calcium channels remains very limited, many of them are waiting for the discovery of pharmacological tools allowing their molecular approach in order to determinate their biological implications. In this paper we describe the different families of calcium channels and toxins that interact with these channels. We also recapitulate the "non defined" calcium channels i.e. calcium channel which does not correspond to a N, L, P/Q, R or T type channel and for which no effector are available. We report the discovery and characterization of mapacalcine, a toxin extracted for a marine sponge, as an example of an approach of an undefined calcium channels first characterized by electrophysiological techniques and for which a specific toxin has been purified allowing its pharmacological approach. We also state the possible role of calcium channel toxins in the domain of therapeutic applications.

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[肽毒素在钙通道多样性的药理学研究中的作用]。
从蜘蛛、海螺或蛇的毒液中提取的肽类毒素对钙通道的药理学表征有很大的帮助。它们已成功地用于钙通道的测绘。然而,实际情况仍不明朗。遗传学研究表明,钙通道存在大量类型或亚型。近年来,大量的毒素被提纯。其中许多毒素对钙通道具有特异性作用,已成为钙通道药理研究的有力工具。然而,钙通道的药理学研究仍然非常有限,他们中的许多人正在等待药理学工具的发现,允许他们的分子方法,以确定他们的生物学意义。在本文中,我们描述了钙通道的不同家族和与这些通道相互作用的毒素。我们还概述了“非定义”钙通道,即不对应于N、L、P/Q、R或T型通道的钙通道,并且没有可用的效应物。我们报告了mapacalcine的发现和表征,这是一种从海绵中提取的毒素,作为一种首先通过电生理技术表征的未定义钙通道方法的例子,并且已经纯化了一种特定的毒素,允许其药理学方法。我们还陈述了钙通道毒素在治疗应用领域的可能作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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