Activation of calcium and phospholipid-dependent protein kinase by diacylglycerol, its possible relation to phosphatidylinositol turnover.
Activation of calcium and phospholipid-dependent protein kinase by diacylglycerol, its possible relation to phosphatidylinositol turnover.
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发表时间：
1980-03
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通讯作者：
A. Kishimoto;Y. Takai;T. Mori;U. Kikkawa;Y. Nishizuka
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作者：
A. Kishimoto;Y. Takai;T. Mori;U. Kikkawa;Y. Nishizuka
来自各种哺乳动物组织(Takai，Y.，Kishimoto，A.，Iwa a，Y.，Kawahara，Y.，Mori，T.和Nishizuka，Y(1979)J.Biol)的钙激活的、磷脂依赖的蛋白激酶。化学。254,3692-3695)被添加低于磷脂浓度5%(w/w)的二酰甘油极大地刺激。这种刺激是由于酶对磷脂的表观亲和力增加，以及伴随而来的对钙离子的Ka值从大约1×10(-4)M下降到微摩尔范围。在较宽的钙离子浓度范围内，甘油二酯单独对酶活性影响很小或没有影响。这种影响对至少在2位含有不饱和脂肪酸的二酰基甘油的影响最大。到目前为止所测试的活性二酰甘油包括双甘油酯、双甘油酯、香菜素、1-硬脂酰基-2-油酰二甘油酯和1-硬脂酰基-2-亚油酰二甘油酯。相比之下，含有饱和脂肪酸的二酰甘油，如双棕榈素和二硬脂素，效果要差得多。三酰基甘油和单酰基甘油是完全无效的，与脂肪酰基部分无关。胆固醇和游离脂肪酸也没有效果。基于这些观察，提出了蛋白激酶激活和磷脂酰肌醇转换之间可能的偶联，这可能是由各种细胞外信使引起的。
Ca2+-activated, phospholipid-dependent protein kinase from various mammalian tissues (Takai, Y., Kishimoto, A., Iwasa, Y., Kawahara, Y., Mori, T., and Nishizuka, Y (1979) J. Biol. Chem. 254, 3692-3695) was greatly stimulated by the addition of diacylglycerol at less than 5% (w/w) the concentration of phospholipid. This stimulation was due to an increase in the apparent affinity of enzyme for phospholipid and to a concomitant decrease in the Ka value for Ca2+ from about 1 x 10(-4) M to the micromolar range. Diacylglycerol alone showed little or no effect on enzymatic activity over a wide range of Ca2+ concentrations. This effect was greatest for diacylglycerol which contained unsaturated fatty acid at least at position 2. The active diacylglycerols so far tested included diolein, dilinolein, diarachidonin, 1-stearoyl-2-oleoyl diglyceride, and 1-stearoyl-2-linoleoyl diglyceride. In contrast, diacylglycerols containing saturated fatty acids such as dipalmitin and distearin were far less effective. Triacyl- and monoacylglycerols were totally ineffective, irrespective of the fatty acyl moieties. Cholesterol and free fatty acids were also ineffective. Based on these observations, a possible coupling is proposed between the protein kinase activation and phosphatidylinositol turnover which can be provoked by various extracellular messengers.