Bond C T, Ammälä C, Ashfield R, Blair T A, Gribble F, Khan R N, Lee K, Proks P, Rowe I C, Sakura H
Vollum Institute, Oregon Health Sciences University, Portland 97201, USA.
FEBS Lett. 1995 Jun 19;367(1):61-6. doi: 10.1016/0014-5793(95)00497-w.
A cDNA clone encoding an inwardly-rectifying K-channel (BIR1) was isolated from insulinoma cells. The predicted amino acid sequence shares 72% identity with the cardiac ATP-sensitive K-channel rcKATP (KATP-1;[6]). The mRNA is expressed in the brain and insulinoma cells. Heterologous expression in Xenopus oocytes produced currents which were K(+)-selective, time-independent and showed inward rectification. The currents were blocked by external barium and caesium, but insensitive to tolbutamide and diazoxide. In inside-out patches, channel activity was not blocked by 1 mM internal ATP. The sequence homology with KATP-1 suggests that BIR1 is a subunit of a brain and beta-cell KATP channel. However, pharmacological differences and the lack of ATP-sensitivity, suggest that if, this is the case, heterologous subunits must exert strong modulatory influences on the native channel.
从胰岛素瘤细胞中分离出一个编码内向整流钾通道(BIR1)的cDNA克隆。预测的氨基酸序列与心脏ATP敏感性钾通道rcKATP(KATP-1;[6])有72%的同源性。该mRNA在脑和胰岛素瘤细胞中表达。在非洲爪蟾卵母细胞中的异源表达产生了钾离子选择性、非时间依赖性且呈现内向整流的电流。这些电流被外部的钡和铯阻断,但对甲苯磺丁脲和二氮嗪不敏感。在内外膜片配置中,通道活性不被1 mM的内部ATP阻断。与KATP-1的序列同源性表明BIR1是脑和β细胞KATP通道的一个亚基。然而,药理学差异以及缺乏ATP敏感性表明,如果是这种情况,异源亚基必定对天然通道施加了强大的调节影响。