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目的:研究tyrphostin对酪蛋白激酶Ⅱ(CKⅡ)的作用.方法:依次采用DEAE纤维素和肝素Sepharose层析将大鼠肝CKⅡ进行了部分纯化,通过将去磷酸化的酪蛋白和[γ32P]ATP与CKⅡ保温的方法测定CKⅡ的活性.结果:AG34对CKⅡ有强烈的抑制作用IC5033μmol·L-1(27-41μmol·L-1),AG372(121μmol·L-1)和AG1112(150μmol·L-1)对CKⅡ有明显的抑制作用.AG34对CKⅡ的动力学研究表明:它与酪蛋白和ATP均呈非竞争性抑制作用.结论:AG34、AG372和AG1112是CKⅡ的抑制剂,AG34的抑制作用与酪蛋白和ATP均呈非竞争性.
Objective: To investigate the effect of tyrphostin on casein kinase Ⅱ (CKⅡ). Methods: The liver CKⅡ was partially purified by DEAEcellulose and heparinSepharose chromatography. The activity of CKⅡ was determined by incubation of dephosphorylated casein and [γ32P] ATP with CKⅡ. RESULTS: AG34 had a strong inhibitory effect on CKⅡ. IC5033μmol·L-1 (27-41μmol·L-1), AG372 (121μmol·L-1) and AG1112 (150μmol·L-1) significantly inhibited CKⅡ. Kinetic studies of CK34 by AG34 showed that it exhibited non-competitive inhibition with both casein and ATP. CONCLUSION: AG34, AG372 and AG1112 are inhibitors of CKⅡ, and the inhibitory effect of AG34 is noncompetitive with both casein and ATP.