Martentoxin:一种大电导钙激活钾离子通道的独有配体(英文)  

Martentoxin:A unique ligand of BK channels

作　　者：陶杰[1] 施健[1] 刘志睿[1] 吉永华[1] 

机构地区：[1]上海大学神经药理学与毒理学实验室,上海200444

出　　处：《生理学报》2012年第4期355-364,共10页Acta Physiologica Sinica

基　　金：supported by the National Basic Research Development Program of China (No. 2010CB529806);National Natural Sciences Foundation of China (No. 30772554 and 31171064);Key Research Program of Science and Technology Commissions of Shanghai Municipality,China (No. 11JC1404300);Leading Academic Discipline Project of Shanghai Municipal Education Commission "Molecular Physiology" (No. J50108);the Innovation Foundation for Graduate Student,Shanghai University,China

摘　　要：大电导钙激活钾离子(BK)通道广泛分布于可兴奋细胞与非兴奋细胞中,行使着一系列重要的生理功能。以源于蝎粗毒的高亲和性毒素作为研究工具,使BK通道的药理学和结构性质正逐步被揭示。Martentoxin是一种分离提取自东亚短钳蝎(Buthus martensi Karsch)粗毒的短链多肽,由37个氨基酸残基构成。研究表明,其对BK通道的特异性远高于其它各类型的电压门控钾通道(Kv)。迄今为止,由于用以探明BK通道亚型结构与功能及相关病理的特异性药物工具仍然稀缺,因此阐明martentoxin与BK通道间的相互作用模式就显得至关重要了。鉴于此原因,本综述将针对martentoxin的药理性质和其与BK通道相互作用的分子机制做进一步阐明。The large-conductance calcium-activated potassium （BK） channels distributed in both excitable and non-excitable cells are key participants in a variety of physiological functions. By employing numerous high-affinity natural toxins originated from scorpion venoms the pharmacological and structural characteristics of these channels tend to be approached. A 37-residue short-chain peptide, named as martentoxin, arising from the venom of the East-Asian scorpion （Buthus martensi Karsch） has been investigated with a com- paratively higher preference for BK channels over other voltage-gated potassium （Kv） channels. Up to now, since the specific drug tool probing for clarifying structure-function of BK channel subtypes and related pathology remain scarce, it is of importance to illu- minate the underlying mechanism of molecular interaction between martentoxin and BK channels. As for it, the current review will address the recent progress on the studies of pharmacological characterizations and molecular determinants of martentoxin targeting on BK channels.

关 键 词：BK通道 martentoxin 钙离子敏感性 Β亚基 毒素-通道相互作用 

分 类 号：R338[医药卫生—人体生理学]