Department of Anesthesiology, Weill Cornell Medical College, New York, New York, USA.
Nat Struct Mol Biol. 2013 Feb;20(2):159-66. doi: 10.1038/nsmb.2473. Epub 2012 Dec 23.
Understanding how ion channels open and close their pores is crucial for comprehending their physiological roles. We used intracellular quaternary ammonium blockers, electrophysiology and X-ray crystallography to locate the voltage-dependent gate in MthK potassium channels from Methanobacterium thermoautotrophicum. Blockers bind in an aqueous cavity between two putative gates: an intracellular gate and the selectivity filter. Thus, these blockers directly probe gate location--an intracellular gate will prevent binding when closed, whereas a selectivity filter gate will always allow binding. Kinetic analysis of tetrabutylammonium block of single MthK channels combined with X-ray crystallographic analysis of the pore with tetrabutyl antimony unequivocally determined that the voltage-dependent gate, like the C-type inactivation gate in eukaryotic channels, is located at the selectivity filter. State-dependent binding kinetics suggest that MthK inactivation leads to conformational changes within the cavity and intracellular pore entrance.
了解离子通道如何打开和关闭其孔道对于理解它们的生理作用至关重要。我们使用细胞内的季铵盐阻断剂、电生理学和 X 射线晶体学来定位产甲烷菌 Methanobacterium thermoautotrophicum 中的 MthK 钾通道的电压门控。阻断剂结合在两个假定的门之间的含水腔中:一个是细胞内门,另一个是选择性过滤器。因此,这些阻断剂直接探测门的位置——当关闭时,细胞内门会阻止结合,而选择性过滤器门总是允许结合。对单 MthK 通道的四丁基铵阻断的动力学分析结合四丁基锑对孔道的 X 射线晶体学分析,明确确定了电压门控,就像真核通道中的 C 型失活门一样,位于选择性过滤器。状态依赖的结合动力学表明,MthK 的失活导致腔内和细胞内孔入口的构象变化。