Romey G, Attali B, Chouabe C, Abitbol I, Guillemare E, Barhanin J, Lazdunski M
Institut de Pharmacologie Moléculaire et Cellulaire, CNRS, 660 route des Lucioles, Sophia Antipolis, 06560 Valbonne, France.
J Biol Chem. 1997 Jul 4;272(27):16713-6. doi: 10.1074/jbc.272.27.16713.
The very slowly activating delayed rectifier K+ channel IKs is essential for controlling the repolarization phase of cardiac action potentials and K+ homeostasis in the inner ear. The IKs channel is formed via the assembly of two transmembrane proteins, KvLQT1 and MinK. Mutations in KvLQT1 are associated with a long QT syndrome that causes syncope and sudden death and also with deafness. Here, we show a new mode of association between ion channel forming subunits in that the cytoplasmic C-terminal end of MinK interacts directly with the pore region of KvLQT1. This interaction reduces KvLQT1 channel conductance from 7.6 to 0.58 picosiemens. However, because MinK also reveals a large number of previously silent KvLQT1 channels (x 60), the overall effect is a large increase (x 4) in the macroscopic K+ current. Conformational changes associated with the KvLQT1/MinK association create very slow and complex activation kinetics without much alteration in the deactivation process. Changes induced by MinK have an essential regulatory role in the development of this K+ channel activity upon repetitive electrical stimulation with a particular interest in tachycardia.
激活极其缓慢的延迟整流钾离子通道IKs对于控制心脏动作电位的复极化阶段以及内耳中的钾离子稳态至关重要。IKs通道由两种跨膜蛋白KvLQT1和MinK组装而成。KvLQT1中的突变与导致晕厥和猝死的长QT综合征有关,也与耳聋有关。在此,我们展示了离子通道形成亚基之间一种新的关联模式,即MinK的胞质C末端直接与KvLQT1的孔区域相互作用。这种相互作用将KvLQT1通道电导从7.6皮西门子降低至0.58皮西门子。然而,由于MinK还揭示了大量之前沉默的KvLQT1通道(增加60倍),总体效果是宏观钾电流大幅增加(增加4倍)。与KvLQT1/MinK关联相关的构象变化产生了非常缓慢且复杂的激活动力学,而失活过程没有太大改变。MinK诱导的变化在重复电刺激时对这种钾通道活性的发展具有重要的调节作用,尤其在心动过速方面。