Ward G E, Fujioka H, Aikawa M, Miller L H
Laboratory of Malaria Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892.
Exp Parasitol. 1994 Nov;79(3):480-7. doi: 10.1006/expr.1994.1109.
Staurosporine, a protein kinase inhibitor, inhibits the invasion of rhesus by Plasmodium knowlesi merozoites with an IC50 of 250 nM. The drug exerts its effects primarily on the merozoite, with little or no effect on the erythrocyte. Okadaic acid, an inhibitor of protein phosphatases, can partially abrogate the inhibitory effects of staurosporine. Staurosporine arrests invasion at a step which is ultrastructurally similar to the arrest caused by cytochalasins B and D: the merozoite attaches, apically reorients, and forms a junction with the erythrocyte, but it does not internalize. These results suggest that protein phosphorylation within the merozoite plays an important role in the internalization step of invasion.
星形孢菌素是一种蛋白激酶抑制剂，它能抑制诺氏疟原虫子孢子对恒河猴的入侵，其半数抑制浓度（IC50）为250纳摩尔。该药物主要作用于子孢子，对红细胞几乎没有影响。冈田酸是一种蛋白磷酸酶抑制剂，它能部分消除星形孢菌素的抑制作用。星形孢菌素在一个步骤中阻止入侵，该步骤在超微结构上类似于细胞松弛素B和D所导致的阻止过程：子孢子附着、顶端重新定向并与红细胞形成连接，但它不会内化。这些结果表明，子孢子内的蛋白质磷酸化在入侵的内化步骤中起重要作用。
