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目的:研究Tyrphostins(AG123,AG1394,AG114,AG1109,AG555)对酪蛋白激酶Ⅱ(CKⅡ)活性的影响。方法:依次采用DEAE-纤维素和肝素-Sepharose层析将大鼠肝CKⅡ纯化了104倍,通过将去磷酸化的酪蛋白和[γ-~(32)P)ATP与CKⅡ保温的方法测定CKⅡ的活性。结果:AG213对CKⅡ有强烈的抑制作用(IC_(50)44.7μmol·L~(-1)[41.5μmol·L~(-1),47.9μmol·L~(-1)]),AG1394(144μmol·L~(-1))对CKⅡ的抑制率为89％。AG114和AG1109对CKⅡ也有明显的抑制作用,而AG555对CKⅡ的活性没有影响。结论:某些tyrphostins是CKⅡ抑制剂。
Objective: To study the effect of Tyrphostins (AG123, AG1394, AG114, AG1109 and AG555) on the activity of casein kinase Ⅱ (CKⅡ). METHODS: Rat hepatic CKⅡ was purified 104-fold by DEAE-cellulose and heparin-Sepharose chromatography in turn. CKⅡ (CKⅡ) was determined by incubation of dephosphorylated casein and [γ- (32) Activity. Results: AG213 had a strong inhibitory effect on CKⅡ (IC 50 (44.7μmol·L -1 [41.5μmol·L -1, 47.9μmol·L -1]), AG1394 (144μmol·L -1) · L ~ (-1)) inhibited CKⅡ by 89%. AG114 and AG1109 had obvious inhibitory effects on CKⅡ, while AG555 had no effect on the activity of CKⅡ. Conclusion: Some tyrphostins are CKⅡ inhibitors.