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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.