Computational Biomolecular Dynamics Group, Max Planck Institute for Multidisciplinary Sciences , Göttingen, Germany.
Department of Medical Genetics and Molecular Biochemistry, Temple University Lewis Katz School of Medicine, Philadelphia, PA, USA.
J Gen Physiol. 2023 Aug 7;155(8). doi: 10.1085/jgp.202213166. Epub 2023 Jun 15.
K+ channel activity can be limited by C-type inactivation, which is likely initiated in part by dissociation of K+ ions from the selectivity filter and modulated by the side chains that surround it. While crystallographic and computational studies have linked inactivation to a "collapsed" selectivity filter conformation in the KcsA channel, the structural basis for selectivity filter gating in other K+ channels is less clear. Here, we combined electrophysiological recordings with molecular dynamics simulations, to study selectivity filter gating in the model potassium channel MthK and its V55E mutant (analogous to KcsA E71) in the pore-helix. We found that MthK V55E has a lower open probability than the WT channel, due to decreased stability of the open state, as well as a lower unitary conductance. Simulations account for both of these variables on the atomistic scale, showing that ion permeation in V55E is altered by two distinct orientations of the E55 side chain. In the "vertical" orientation, in which E55 forms a hydrogen bond with D64 (as in KcsA WT channels), the filter displays reduced conductance compared to MthK WT. In contrast, in the "horizontal" orientation, K+ conductance is closer to that of MthK WT; although selectivity filter stability is lowered, resulting in more frequent inactivation. Surprisingly, inactivation in MthK WT and V55E is associated with a widening of the selectivity filter, unlike what is observed for KcsA and reminisces recent structures of inactivated channels, suggesting a conserved inactivation pathway across the potassium channel family.
钾通道的活性可以受到 C 型失活的限制,这种失活可能部分由钾离子从选择性过滤器上解离引起,并受其周围侧链的调节。虽然晶体学和计算研究已经将失活与 KcsA 通道中选择性过滤器的“塌陷”构象联系起来,但其他钾通道中选择性过滤器门控的结构基础则不太清楚。在这里,我们将电生理记录与分子动力学模拟相结合,研究了模型钾通道 MthK 及其在孔环中的 V55E 突变体(类似于 KcsA E71)的选择性过滤器门控。我们发现,MthK V55E 的开放概率低于野生型通道,这是由于开放状态的稳定性降低以及单位电导降低所致。模拟从原子尺度解释了这两个变量,表明 V55E 中的离子渗透受到 E55 侧链的两种不同取向的影响。在“垂直”取向中,E55 与 D64 形成氢键(与 KcsA WT 通道中的情况相同),与 MthK WT 相比,过滤器的电导率降低。相比之下,在“水平”取向中,K+电导更接近 MthK WT;尽管选择性过滤器的稳定性降低,导致失活更频繁。令人惊讶的是,与 KcsA 不同,MthK WT 和 V55E 的失活与选择性过滤器的加宽有关,这与最近失活通道的结构相似,表明钾通道家族中存在保守的失活途径。