The Ca++/calmodulin-dependent protein kinase II inhibitors KN62 and KN93, and their inactive analogues KN04 and KN92, inhibit nicotinic activation of tyrosine hydroxylase in bovine chromaffin cells
The Ca++/calmodulin-dependent protein kinase II inhibitors KN62 and KN93, and their inactive analogues KN04 and KN92, inhibit nicotinic activation of tyrosine hydroxylase in bovine chromaffin cells
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DOI：
10.1006/bbrc.1996.0536
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发表时间：
1996-04-05
影响因子：
3.1
通讯作者：
Thomson, KA
中科院分区：
文献类型：
--
作者：
Marley, PD;Thomson, KA
本文研究了Ca ~（++）/钙调素依赖性蛋白激酶Ⅱ（CAM-K-Ⅱ）在牛肾上腺嗜铬细胞酪氨酸羟化酶烟碱激活中的可能作用。在3-30 μ M的浓度范围内，KN 62，一种特异性CAM-K-II抑制剂，抑制基础酪氨酸羟化酶活性和尼古丁或K+去极化刺激的活性。KN 04是KN 62的结构类似物，不抑制CAM-K-II，对基础和尼古丁刺激的酪氨酸羟化酶活性产生相同的浓度依赖性抑制。另一种CAM-K-II抑制剂KN 93也抑制尼古丁和K+对酪氨酸羟化酶活性的刺激;然而，KN 93的无活性类似物KN 92模拟了这些作用。结果表明，KN 62和KN 93对尼古丁和K+刺激的酪氨酸羟化酶活性的抑制不是由于它们抑制CAM-K-II的能力。(C)出版社：Academic Press，Inc.
The possible role of Ca++/calmodulin-dependent protein kinase II (CAM-K-II) in the nicotinic activation of tyrosine hydroxylase in intact cultured bovine adrenal chromaffin cells has been investigated. Over the concentration range 3-30 mu M, KN62, a specific CAM-K-II inhibitor, inhibited basal tyrosine hydroxylase activity and the activity stimulated by nicotine or K+ depolarisation. KN04, a structural analogue of KN62 which does not inhibit CAM-K-II, produced an identical concentration-dependent inhibition of basal and nicotine-stimulated tyrosine hydroxylase activity. Another CAM-K-II inhibitor, KN93, also inhibited nicotine and K+ stimulation of tyrosine hydroxylase activity; however, an inactive analogue of KN93, KN92, mimicked these effect. The results suggest that the inhibition of nicotine- and K+-stimulated tyrosine hydroxylase activity by KN62 and KN93 is not due to their ability to inhibit CAM-K-II. (C) 1996 Academic Press, Inc.