Dluzewski A R, Garcia C R
Medical Research Council, Muscle and Cell Motility Unit, King's College, London, United Kingdom.
Experientia. 1996 Jun 15;52(6):621-3. doi: 10.1007/BF01969742.
We have examined the effects of seven protein kinase inhibitors (staurosporine, genistein, methyl 2,5-dihydroxycinnamate, tyrphostins B44 and B46, lavendustin A and R03) on the erythrocytic cycle of the malaria parasite, Plasmodium falciparum. One (staurosporine) strongly inhibits serine/threonine kinases, but the remainder all exhibit a strong preference for tyrosine kinases. We have been able to discriminate between effects on invasion and on intraerythrocytic development. All reagents impeded development of intraerythrocytic parasites, though at widely differing concentrations, from the sub-micromolar to the millimolar. Several inhibitors, including staurosporine, also reduced invasion. The phosphatase inhibitor, okadaic acid, had a strong inhibitory effect both on invasion and development. The regulation of malaria development by phosphorylation or dephosphorylation reactions at several points in the blood-stage cycle is implied.
我们研究了七种蛋白激酶抑制剂（星形孢菌素、染料木黄酮、2,5-二羟基肉桂酸甲酯、 tyrphostins B44和B46、薰衣草素A和R03）对疟原虫恶性疟原虫红细胞周期的影响。其中一种（星形孢菌素）强烈抑制丝氨酸/苏氨酸激酶，但其余的都对酪氨酸激酶有强烈的偏好。我们能够区分对入侵和红细胞内发育的影响。所有试剂都阻碍了红细胞内寄生虫的发育，尽管浓度差异很大，从亚微摩尔到毫摩尔。几种抑制剂，包括星形孢菌素，也减少了入侵。磷酸酶抑制剂冈田酸对入侵和发育都有很强的抑制作用。这意味着在血液阶段周期的几个点上，通过磷酸化或去磷酸化反应对疟疾发育进行调节。
