Livne A A, Sardet C, Pouyssegur J
C.N.R.S., Centre de Biochimie, Université de Nice, France.
FEBS Lett. 1991 Jun 24;284(2):219-22. doi: 10.1016/0014-5793(91)80689-z.
alpha-Thrombin, phorbol esters (PMA) and 1,2-diacylglycerol (DAG), three activators of the amiloride-sensitive Na+/H+ exchange in human platelets, rapidly increase the intracellular pH and the level of phosphorylation of the Na+/H+ exchange protein (NHE1). This stimulatory effect is suppressed by staurosporine, a potent kinase inhibitor, and increased by okadaic acid, a potent inhibitor of phosphatase 1 and 2A. The modulations of NHE1 phosphorylation by these factors correlate well with their effects on platelet pH. Thus, we conclude that in platelets (i) Na+/H+ exchange is mediated by NHE1, and (ii) platelet activating agents stimulate NHE1 via the modulation of the kinase/phosphatase equilibrium.
α-凝血酶、佛波酯（PMA）和1,2-二酰甘油（DAG）是人类血小板中对氨氯地平敏感的Na⁺/H⁺交换的三种激活剂，它们可迅速提高细胞内pH值以及Na⁺/H⁺交换蛋白（NHE1）的磷酸化水平。这种刺激作用被强效激酶抑制剂星形孢菌素抑制，并被蛋白磷酸酶1和2A的强效抑制剂冈田酸增强。这些因素对NHE1磷酸化的调节与其对血小板pH值的影响密切相关。因此，我们得出结论，在血小板中：（i）Na⁺/H⁺交换由NHE1介导；（ii）血小板激活剂通过调节激酶/磷酸酶平衡来刺激NHE1。
