Grottesi Alessandro, Sansom Mark S P
Laboratory of Molecular Biophysics, Department of Biochemistry, University of Oxford, South Parks Road, Oxford OX1 3QU, UK.
FEBS Lett. 2003 Jan 30;535(1-3):29-33. doi: 10.1016/s0014-5793(02)03849-8.
Toxins that block voltage-gated potassium (Kv) channels provide a possible template for improved homology models of the Kv pore. In assessing the interactions of Kv channels and their toxins it is important to determine the dynamic flexibility of the toxins. Multiple 10 ns duration molecular dynamics simulations combined with essential dynamics analysis have been used to explore the flexibility of four different Kv channel-blocking toxins. Three toxins (Tc1, AgTx and ChTx) share a common fold. They also share a common pattern of conformational dynamics, as revealed by essential dynamics analysis of the simulation results. This suggests that some aspects of dynamic behaviour are conserved across a single protein fold class. In each of these three toxins, the residue exhibiting minimum flexibility corresponds to a conserved lysine residue that is suggested to interact with the filter domain of the channel. Thus, comparative simulations reveal functionally important conservation of molecular dynamics as well as protein fold across a family of related toxins.
阻断电压门控钾(Kv)通道的毒素为改进Kv孔的同源模型提供了一种可能的模板。在评估Kv通道与其毒素的相互作用时,确定毒素的动态灵活性很重要。已使用多个持续时间为10纳秒的分子动力学模拟结合主成分动力学分析来探究四种不同的Kv通道阻断毒素的灵活性。三种毒素(Tc1、AgTx和ChTx)具有共同的折叠结构。模拟结果的主成分动力学分析表明,它们还具有共同的构象动力学模式。这表明在单一蛋白质折叠类别中,动态行为的某些方面是保守的。在这三种毒素中的每一种中,表现出最小灵活性的残基对应于一个保守的赖氨酸残基,该残基被认为与通道的滤器结构域相互作用。因此,比较模拟揭示了相关毒素家族在分子动力学以及蛋白质折叠方面功能上重要的保守性。