在体外，肼屈嗪可抑制蛋白激酶A和G，但KRN2391则无此作用。
Inhibition of protein kinases A and G by hydralazine but not KRN2391 in vitro.
作者信息
Sun G, Robinson P J
机构信息
Endocrine Unit, John Hunter Hospital, Newcastle, NSW, Australia.
出版信息
Zhongguo Yao Li Xue Bao. 1995 May;16(3):276-80.
AIM
To examine possible direct effects of the vasodilators hydralazine and KRN2391 on the activities of protein kinase A (PKA), protein kinase G (PKG), and protein kinase C (PKC).
METHODS
PKA, PKG and PKC were extracted from bovine lung, heart and rat brain and purified to homogeneity by chromatography. The effects of different reagents on these protein kinase activities were determined in vitro.
RESULTS
Hydralazine (0.03-10 mmol.L(-1)) inhibited the activities of both PKA and PKG with IC50 of 1.2 and 2.5 mmol.L(-1), respectively, but had little effect on PKC. KRN2391 (1-1000 mumol.L(-1) had no effects on PKA, PKG, or PKC. Using H-89 and GF109203X, inhibitors relatively selective to PKA and PKC respectively, as controls, we obtained inhibitions on PKG, PKA, and PKC similar to literature. However, a novel PKG inhibitor KT5823 failed to inhibit PKG or PKA.
CONCLUSION
Hydralazine alters the activity of PKG and PKA, which may have implications for the vasodilator activity.
目的
研究血管舒张剂肼屈嗪和KRN2391对蛋白激酶A（PKA）、蛋白激酶G（PKG）和蛋白激酶C（PKC）活性的可能直接影响。
方法
从牛肺、心脏和大鼠脑中提取PKA、PKG和PKC，并通过色谱法纯化至同质。在体外测定不同试剂对这些蛋白激酶活性的影响。
结果
肼屈嗪（0.03 - 10 mmol.L⁻¹）抑制PKA和PKG的活性，IC50分别为1.2和2.5 mmol.L⁻¹，但对PKC影响较小。KRN2391（1 - 1000 μmol.L⁻¹）对PKA、PKG或PKC均无影响。分别使用对PKA和PKC相对选择性的抑制剂H - 89和GF109203X作为对照，我们获得了与文献相似的对PKG、PKA和PKC的抑制作用。然而，一种新型PKG抑制剂KT5823未能抑制PKG或PKA。
结论
肼屈嗪改变PKG和PKA的活性，这可能与血管舒张剂活性有关。
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