Cuello L G, Romero J G, Cortes D M, Perozo E
Department of Molecular Physiology and Biological Physics, University of Virginia Health Sciences Center, Charlottesville.
Biochemistry. 1998 Mar 10;37(10):3229-36. doi: 10.1021/bi972997x.
Because of its size, high levels of expression, and unusual detergent stability, the small K+ channel from Streptomyces lividans (SKC1) is considered to be an ideal candidate for detailed structural analysis. In this paper, we have used planar lipid bilayers and radiotracer uptake experiments to study purified and reconstituted SKC1, in an attempt to develop a bulk assay for its functional characterization. In channels reconstituted into liposomes with external pH 3.5 and intravesicular pH 7.5, a time-dependent SKC1-catalyzed 86Rb+ uptake was observed. This cationic influx was blocked by Ba2+ ions with a Ki (external) of 0.4 mM and was shown to have the following selectivity sequence: K+ > Rb+ > NH4+ >> Na+ > Li+. In experiments with external pH 7.5 or in liposomes containing no channels, no 86Rb+ uptake was detected. When SKC1 was incorporated into planar lipid bilayers, we failed to observe significant single-channel activity at neutral pH but detected frequent multiple-channel openings a pH < 5.0. These results indicate that under these experimental conditions SKC1 behaves as a pH-gated K+ channel in which protonation of one or more residues promotes channel opening. At acidic pH and symmetrical 200 mM KCl solutions, SKC1 showed numerous brief openings with a main single-channel conductance of 135 pS and a subconductance state of 70 pS. Channel open probability showed a slight voltage dependence, with higher activities observed at negative potentials, a fact which may suggest that the protonation site lies within the transmembrane electrical field. Attempts to determine the pKa of channel activation were obscured by intrinsic limitations of the 86Rb+ flux assay. However, it appears to be lower than pH 4.0. Limited proteolysis experiments demonstrated that SKC1 reconstitutes vectorially, almost exclusively in the right-side-out configuration, indicating that the protonation site responsible for channel opening is located at the extracellular face of the channel. These results point toward a potentially novel gating mechanism for SKC1 and open the possibility of using transmembrane-driven radiotracer influx experiments as a reliable bulk functional assay for reconstituted SKC1.
由于其大小、高表达水平以及对去污剂的异常稳定性,来自天蓝色链霉菌的小钾离子通道(SKC1)被认为是进行详细结构分析的理想候选对象。在本文中,我们使用平面脂质双层和放射性示踪剂摄取实验来研究纯化和重组的SKC1,试图开发一种用于其功能表征的大量检测方法。在重构到外部pH为3.5且囊泡内pH为7.5的脂质体中的通道中,观察到了时间依赖性的SKC1催化的86Rb+摄取。这种阳离子内流被Ba2+离子阻断,其外部Ki为0.4 mM,并显示出以下选择性序列:K+ > Rb+ > NH4+ >> Na+ > Li+。在外部pH为7.5的实验中或在不含通道的脂质体中,未检测到86Rb+摄取。当SKC1整合到平面脂质双层中时,我们在中性pH下未观察到明显的单通道活性,但在pH < 5.0时检测到频繁的多通道开放。这些结果表明,在这些实验条件下,SKC1表现为一种pH门控钾离子通道,其中一个或多个残基的质子化促进通道开放。在酸性pH和对称的200 mM KCl溶液中,SKC1显示出许多短暂的开放,主要单通道电导为135 pS,亚电导状态为70 pS。通道开放概率显示出轻微的电压依赖性,在负电位下观察到更高的活性,这一事实可能表明质子化位点位于跨膜电场内。试图确定通道激活的pKa被86Rb+通量测定的内在局限性所掩盖。然而,它似乎低于pH 4.0。有限的蛋白酶解实验表明,SKC1以向量方式重构,几乎完全是外翻构型,表明负责通道开放的质子化位点位于通道的细胞外表面。这些结果指向SKC1一种潜在的新型门控机制,并开启了使用跨膜驱动的放射性示踪剂内流实验作为重组SKC1可靠的大量功能检测方法的可能性。