Oishi K, Zheng B, White J F, Vogler W R, Kuo J F
Department of Pharmacology, Emory University School of Medicine, Atlanta, Georgia 30322.
Biochem Biophys Res Commun. 1988 Dec 30;157(3):1000-6. doi: 10.1016/s0006-291x(88)80973-2.
The anticancer ether lipid analogs ET-18-OCH3 and BM 41.440 inhibited Na, K-ATPase in the purified rat brain membrane fragments, with a potency comparable to that of their inhibition of protein kinase C. They also inhibited Na,K-ATPase in the crude membrane fraction of HL60 cells. Kinetic analysis indicated that the lipids had a mode of action different from that of ouabain, a classic inhibitor of the ATPase. The lipids also blocked 22Na uptake in the inside-out membrane vesicles of human erythrocytes. It is suggested that Na,K-ATPase might represent an additional site with which certain protein kinase C inhibitors can interact to alter cellular activities.
抗癌醚脂类似物ET - 18 - OCH3和BM 41.440在纯化的大鼠脑膜片段中抑制钠钾ATP酶，其效力与其对蛋白激酶C的抑制作用相当。它们还抑制HL60细胞粗膜组分中的钠钾ATP酶。动力学分析表明，这些脂质的作用方式不同于哇巴因（一种ATP酶的经典抑制剂）。这些脂质还阻断人红细胞内翻膜囊泡对22Na的摄取。有人提出，钠钾ATP酶可能是某些蛋白激酶C抑制剂与之相互作用以改变细胞活性的另一个位点。
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