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与去甲肾上腺素能相关基因电压依赖性钾通道相互作用的毒素。

Toxins interacting with ether-à-go-go-related gene voltage-dependent potassium channels.

作者信息

Wanke Enzo, Restano-Cassulini Rita

机构信息

Dipartimento di Biotecnologie e Bioscienze, Università di Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.

出版信息

Toxicon. 2007 Feb;49(2):239-48. doi: 10.1016/j.toxicon.2006.09.025. Epub 2006 Oct 10.

DOI:10.1016/j.toxicon.2006.09.025
PMID:17097705
Abstract

The critical role that ether-à-go-go-related gene (erg) K(+) channels play in mating in Caenorhabditis elegans, neuronal seizures in Drosophila and cardiac action potential repolarization in humans has been well documented. Three erg genes (erg1, erg2 and erg3) have been identified and characterized. A structurally diverse number of compounds block these channels, but do not display specificity among the different channel isoforms. In this review we describe the blocking properties of several peptides, purified from scorpion, sea anemone and spider venoms, which are selective for certain members of the ERG family of channels. These peptides do not behave as classical pore blockers and appear to modify the gating properties of the channel. Genomic studies predict the existence of many other novel peptides with the potential of being more selective for ERG channels than those discussed here.

摘要

醚 - 去 - 去相关基因(erg)钾通道在秀丽隐杆线虫交配、果蝇神经元癫痫发作以及人类心脏动作电位复极化过程中所起的关键作用已有充分记载。已鉴定并表征了三个erg基因(erg1、erg2和erg3)。结构多样的多种化合物可阻断这些通道,但对不同的通道亚型不具有特异性。在本综述中,我们描述了从蝎子、海葵和蜘蛛毒液中纯化得到的几种肽的阻断特性,这些肽对ERG通道家族的某些成员具有选择性。这些肽并非传统的孔道阻断剂,似乎会改变通道的门控特性。基因组研究预测存在许多其他新型肽,它们对ERG通道的选择性可能比本文讨论的肽更高。

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