Sakura H, Ammälä C, Smith P A, Gribble F M, Ashcroft F M
University Laboratory of Physiology, Oxford, UK.
FEBS Lett. 1995 Dec 27;377(3):338-44. doi: 10.1016/0014-5793(95)01369-5.
A cDNA clone encoding an inwardly-rectifying potassium channel subunit (Kir6.2) was isolated from an insulinoma cDNA library. The mRNA is strongly expressed in brain, skeletal muscle, cardiac muscle and in insulinoma cells, weakly expressed in lung and kidney and not detectable in spleen, liver or testis. Heterologous expression of Kir6.2 in HEK293 cells was only observed when the cDNA was cotransfected with that of the sulphonylurea receptor (SUR). Whole-cell Kir6.2/SUR currents were K(+)-selective, time-independent and showed weak inward rectification. They were blocked by external barium (5 mM), tolbutamide (Kd = 4.5 microM) or quinine (20 microM) and by 5 mM intracellular ATP. The single-channel conductance was 73 pS. Single-channel activity was voltage-independent and was blocked by 1 mM intracellular ATP or 0.5 mM tolbutamide. We conclude that the Kir6.2/SUR channel complex comprises the ATP-sensitive K-channel.
从胰岛素瘤cDNA文库中分离出一个编码内向整流钾通道亚基(Kir6.2)的cDNA克隆。该mRNA在脑、骨骼肌、心肌和胰岛素瘤细胞中强烈表达,在肺和肾中弱表达,在脾、肝或睾丸中未检测到。只有当该cDNA与磺脲类受体(SUR)的cDNA共转染时,才在HEK293细胞中观察到Kir6.2的异源表达。全细胞Kir6.2/SUR电流具有K(+)选择性、不依赖时间,并表现出弱内向整流。它们被细胞外钡(5 mM)、甲苯磺丁脲(Kd = 4.5 microM)或奎宁(20 microM)以及5 mM细胞内ATP阻断。单通道电导为73 pS。单通道活性不依赖电压,并被1 mM细胞内ATP或0.5 mM甲苯磺丁脲阻断。我们得出结论,Kir6.2/SUR通道复合物构成了ATP敏感性钾通道。