Shamgar Liora, Ma Lijuan, Schmitt Nicole, Haitin Yoni, Peretz Asher, Wiener Reuven, Hirsch Joel, Pongs Olaf, Attali Bernard
Department of Physiology & Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv 69978, Israel.
Circ Res. 2006 Apr 28;98(8):1055-63. doi: 10.1161/01.RES.0000218979.40770.69. Epub 2006 Mar 23.
The slow IKS K+ channel plays a major role in repolarizing the cardiac action potential and consists of the assembly of KCNQ1 and KCNE1 subunits. Mutations in either KCNQ1 or KCNE1 genes produce the long-QT syndrome, a life-threatening ventricular arrhythmia. Here, we show that long-QT mutations located in the KCNQ1 C terminus impair calmodulin (CaM) binding, which affects both channel gating and assembly. The mutations produce a voltage-dependent macroscopic inactivation and dramatically alter channel assembly. KCNE1 forms a ternary complex with wild-type KCNQ1 and Ca(2+)-CaM that prevents inactivation, facilitates channel assembly, and mediates a Ca(2+)-sensitive increase of IKS-current, with a considerable Ca(2+)-dependent left-shift of the voltage-dependence of activation. Coexpression of KCNQ1 or IKS channels with a Ca(2+)-insensitive CaM mutant markedly suppresses the currents and produces a right shift in the voltage-dependence of channel activation. KCNE1 association to KCNQ1 long-QT mutants significantly improves mutant channel expression and prevents macroscopic inactivation. However, the marked right shift in channel activation and the subsequent decrease in current amplitude cannot restore normal levels of IKS channel activity. Our data indicate that in healthy individuals, CaM binding to KCNQ1 is essential for correct channel folding and assembly and for conferring Ca(2+)-sensitive IKS-current stimulation, which increases the cardiac repolarization reserve and hence prevents the risk of ventricular arrhythmias.
缓慢激活的 IKS 钾通道在心脏动作电位复极化过程中起主要作用,由 KCNQ1 和 KCNE1 亚基组装而成。KCNQ1 或 KCNE1 基因的突变会导致长 QT 综合征,这是一种危及生命的室性心律失常。在此,我们表明位于 KCNQ1 C 末端的长 QT 突变会损害钙调蛋白(CaM)结合,这会影响通道门控和组装。这些突变会产生电压依赖性宏观失活,并显著改变通道组装。KCNE1 与野生型 KCNQ1 和 Ca(2+)-CaM 形成三元复合物,可防止失活,促进通道组装,并介导 IKS 电流的 Ca(2+)-敏感增加,同时激活的电压依赖性有相当大的 Ca(2+)-依赖性左移。将 KCNQ1 或 IKS 通道与 Ca(2+)-不敏感的 CaM 突变体共表达会显著抑制电流,并使通道激活的电压依赖性右移。KCNE1 与 KCNQ1 长 QT 突变体的结合可显著改善突变体通道表达并防止宏观失活。然而,通道激活的明显右移以及随后电流幅度的降低无法恢复 IKS 通道活性的正常水平。我们的数据表明,在健康个体中,CaM 与 KCNQ1 的结合对于正确的通道折叠和组装以及赋予 Ca(2+)-敏感的 IKS 电流刺激至关重要,这增加了心脏复极化储备,从而预防室性心律失常的风险。