Lerch K, Muir L W, Fischer E H
Biochemistry. 1975 May 6;14(9):2015-23. doi: 10.1021/bi00680a032.
A protein phosphokinase (EC 2.7.1.1.37) was isolated from baker's yeast (Saccharomyces cerevisiae) after a 17,000-fold purification; the purified enzyme is homogeneous according to the criteria of gel electrophoresis and ultracentrifuge analysis. The enzyme has a high isoelectric point of ca. 9 and appears to exist as a monomer with a molecular weight of 42,000 plus or minus 1500. It is neither stimulated by cyclic 3',5'-AMP, -GMP, -CMP or -ump nor inhibited by the regulatory subunit of rabbit muscle protein kinase (Reimann, E. M., Walsh, D. A., and Krebs, E. G. (1971), J. Biol. Chem. 246, 1986). In the presence of divalent metal ions, preferably Mg-2+ or Mn-2+, the enzyme readily transfers the terminal phosphate group of ATP to phosvitin, alphaS1B- and beta a-casein and an NH2-terminal tryptic peptide derived from beta a-casein, but not to protamine, lysine, or arginine-rich histones or to yeast enzymes such as phosphorylase, phosphofructokinase, or pyruvate carboxylase; serine and polyserine were also inactive as phosphate acceptors. Km values of 0.17 mM for beta a-casein and 0.2 mMfor ATP were determined at 10 mM Mg-2+. The urified yeast protein kinase also catalyzes the reverse reaction, namely, the transfer of phosphate from fully phosphorylated beta a-casein or its NH2-terminal peptide to ADP resulting in the formation of ATP. AMP, GDP, UDP, and CDP did not serve as phosphate acceptors in this reaction. As observed by Rabinowitz and Lipmann (Rabinowitz, M., and Lipmann, F. (1960), J. Biol. Chem. 235, 1043) both reactions have different pHoptima with values of 7.5 for the forward reaction (phosphorylation of the proteins) and ca 5.2 for the formation of ATP; both are differently affected by salts. Phosphorylation of beta a-casein with [gamma-32-P]ATP followed by digestion of the labeled protein with trypsin indicated that all the radioactivity was exclusively introduced in an NH2-terminal peptide possessing the unique sequence: Glu-Ser(P)-Leu-Ser(P)-Ser(P)-Ser(P)-Glu-Glu...(Ribadeau-Dumas, B., Brignon, G., Grosclaude, F., and Mercier, J.-C. (1971), eur J. Biochem. 20, 264). By subjecting beta a-casein and its NH2-terminal peptide to the combined action of almond acid phosphatease and purified yeast protein kinase, it was determined that the phosphorylation and dephosphorylation reactions proceed randomly, i.e., all seryl phosphate residues are equally susceptible and that the rate of phosphorylation decreases drastically as the number of bound phosphate groups in the substrate diminishes.
一种蛋白磷酸激酶(EC 2.7.1.1.37)经17000倍纯化后从面包酵母(酿酒酵母)中分离出来;根据凝胶电泳和超速离心分析的标准,纯化后的酶是均一的。该酶的等电点约为9,较高,似乎以单体形式存在,分子量为42000±1500。它既不受环3',5'-AMP、-GMP、-CMP或-ump的刺激,也不受兔肌蛋白激酶调节亚基的抑制(雷曼,E.M.,沃尔什,D.A.,和克雷布斯,E.G.(1971年),《生物化学杂志》246,1986)。在二价金属离子存在下,最好是Mg-2+或Mn-2+,该酶能轻易地将ATP的末端磷酸基团转移到卵黄高磷蛋白、αS1B-和βa-酪蛋白以及βa-酪蛋白衍生的NH2-末端胰蛋白酶肽段上,但不能转移到鱼精蛋白、赖氨酸或富含精氨酸的组蛋白上,也不能转移到酵母酶如磷酸化酶、磷酸果糖激酶或丙酮酸羧化酶上;丝氨酸和聚丝氨酸作为磷酸受体也无活性。在10 mM Mg-2+条件下,βa-酪蛋白的Km值为0.17 mM,ATP的Km值为0.2 mM。纯化的酵母蛋白激酶也催化逆反应,即从完全磷酸化的βa-酪蛋白或其NH2-末端肽段向ADP转移磷酸,从而形成ATP。AMP、GDP、UDP和CDP在该反应中不作为磷酸受体。正如拉比诺维茨和利普曼所观察到的(拉比诺维茨,M.,和利普曼,F.(1960年),《生物化学杂志》235,1043),这两个反应具有不同的最适pH值,正向反应(蛋白质的磷酸化)的值为7.5,ATP形成的最适pH值约为5.2;两者受盐的影响也不同。用[γ-32-P]ATP对βa-酪蛋白进行磷酸化,然后用胰蛋白酶消化标记的蛋白质,结果表明所有放射性都仅引入到具有独特序列Glu-Ser(P)-Leu-Ser(P)-Ser(P)-Ser(P)-Glu-Glu...的NH2-末端肽段中(里巴多-迪马,B.,布里尼翁,G.,格罗斯克洛德,F.,和梅西埃,J.-C.(1971年),《欧洲生物化学杂志》20,264)。通过使βa-酪蛋白及其NH2-末端肽段受到杏仁酸磷酸酶和纯化的酵母蛋白激酶的联合作用,确定磷酸化和去磷酸化反应随机进行,即所有丝氨酸磷酸残基同样敏感,并且随着底物中结合的磷酸基团数量减少,磷酸化速率急剧下降。