Brostrom C O, Corbin J D, King C A, Krebs E G
Proc Natl Acad Sci U S A. 1971 Oct;68(10):2444-7. doi: 10.1073/pnas.68.10.2444.
Two cAMP-dependent protein kinases purified from rabbit skeletal muscle were shown to bind the same amount of cAMP per unit of enzyme activity at several concentrations of this nucleotide. A preparation containing both of these kinases was separated into catalytic (C) and regulatory (R) subunit fractions in the presence of cAMP, the regulatory subunit being obtained as an R.cAMP complex. Addition of increasing amounts of the R.cAMP complex to the holoenzyme (RC) increased the concentration of cAMP required for half-maximal activity of the enzyme. cAMP was liberated from the R.cAMP complex in the presence of added catalytic subunit in a reaction that was facilitated by Mg(2+), ATP, and warming. These findings are presented in support of a model for activation of the protein kinase by cAMP. The possibility that excess regulatory subunit may serve as a sink for intracellular cAMP is also discussed. It is shown that cAMP bound to the R subunit is not a substrate for the cAMP phosphodiesterase.
从兔骨骼肌中纯化得到的两种环磷酸腺苷(cAMP)依赖性蛋白激酶,在该核苷酸的几种浓度下,每单位酶活性结合的cAMP量相同。在cAMP存在的情况下,将含有这两种激酶的制剂分离为催化(C)亚基和调节(R)亚基部分,调节亚基以R·cAMP复合物的形式获得。向全酶(RC)中添加越来越多的R·cAMP复合物,会增加酶达到最大活性一半时所需的cAMP浓度。在添加的催化亚基存在下,cAMP从R·cAMP复合物中释放出来,该反应在镁离子(Mg²⁺)、三磷酸腺苷(ATP)和升温的促进下进行。提出这些发现是为了支持cAMP激活蛋白激酶的模型。还讨论了过量调节亚基可能作为细胞内cAMP汇的可能性。结果表明,与R亚基结合的cAMP不是cAMP磷酸二酯酶的底物。