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目的观察1, 8-二羟蒽醌对重组人蛋白激酶CK2全酶的直接作用及其酶动力学机制,以寻找CK2的抑制剂。方法以重组人CK2全酶为分子靶点,检测不同浓度1, 8-二羟蒽醌对CK2活性的影响。CK2活性通过测定转移到CK2底物上的[γ32P]ATP的[32P]放射活度来检测。结果重组人CK2与天然CK2的性质完全一致。1, 8-二羟蒽醌对重组人CK2全酶具有较强的抑制作用,半数抑制浓度(IC50 )为23. 90μmol·L-1; 与ATP呈竞争性抑制CK2的活性, 抑制常数Ki值为16. 08μmol·L-1。结论1, 8 -二羟蒽醌是重组人蛋白激酶CK2的抑制剂。
Objective To investigate the direct effect of 1, 8-dihydroxyanthraquinone on recombinant human protein kinase CK2 holoenzyme and its enzyme kinetic mechanism in order to find an inhibitor of CK2. Methods Using recombinant human CK2 holoenzyme as a molecular target, the effects of different concentrations of 1,8-dihydroxyanthraquinone on CK2 activity were examined. CK2 activity was measured by measuring [32P] radioactivity of [y32P] ATP transferred to CK2 substrate. Results The properties of recombinant human CK2 and native CK2 were identical. 1, 8-dihydroxyanthraquinone on recombinant human CK2 holoenzyme has a strong inhibitory effect, the median inhibitory concentration (IC50) of 23. 90μmol·L-1; and ATP was competitive inhibition of CK2 activity, inhibition constant Ki Which is 16. 08μmol·L-1. Conclusion 1, 8 - dihydroxyanthraquinone is an inhibitor of recombinant human protein kinase CK2.