Williams D C
Biochem J. 1984 Feb 1;217(3):675-83. doi: 10.1042/bj2170675.
Phenylhydrazine treatment induced hydroxymethylbilane synthase activity (EC 4.3.1.8) in rat spleen, erythrocytes and liver by 40-fold, 7.5-fold and 6-fold respectively. Five multiple forms of the enzyme were resolved by DEAE-cellulose chromatography. In the presence of phenylmethanesulphonyl fluoride only three forms, two major and one minor, were resolved by the fractionation, suggesting that two of the original forms arose by proteolytic modification. Heat treatment (70 degrees C) in the presence of proteinase inhibitor converted one of the major forms into the other major form. Product isomer analysis suggested that this heat-labile form represented an enzyme-substrate covalent intermediate and not a hydroxymethylbilane synthase-uroporphyrinogen III synthase complex. Identical elution profiles and kinetic properties of the enzymes from rat spleen and erythrocytes suggested that the enzyme isolated from spleen was possibly from stored erythrocytes. Sephadex G-75 chromatography of the heat-stable DEAE-cellulose-purified form yielded pure enzyme as judged by sodium dodecyl sulphate/polyacrylamide-gel electrophoresis. The Mr was found to be 43000 +/- 1500. Initial-velocity studies on all enzyme forms showed a hyperbolic dependence of velocity on substrate concentration, demonstrating the existence of a displacement-type mechanism. For the heat-stable form Vmax, varied with pH as a typical bell-shaped curve, indicating that two ionizable groups with pK values of 7.4 and 8.8 are important for catalysis. Km decreased with decreasing pH on the acid side of the pH optimum, suggesting the absence of ionization of a group with pK 7.4 in free enzyme or substrate.
苯肼处理使大鼠脾脏、红细胞和肝脏中的羟甲基胆色素原合酶活性(EC 4.3.1.8)分别提高了40倍、7.5倍和6倍。通过DEAE-纤维素色谱法分离出该酶的五种多种形式。在苯甲磺酰氟存在的情况下,通过分级分离仅分离出三种形式,两种主要形式和一种次要形式,这表明原始形式中的两种是通过蛋白水解修饰产生的。在蛋白酶抑制剂存在下进行热处理(70℃)将一种主要形式转化为另一种主要形式。产物异构体分析表明,这种热不稳定形式代表一种酶-底物共价中间体,而不是羟甲基胆色素原合酶-尿卟啉原III合酶复合物。来自大鼠脾脏和红细胞的酶具有相同的洗脱曲线和动力学性质,这表明从脾脏分离出的酶可能来自储存的红细胞。通过十二烷基硫酸钠/聚丙烯酰胺凝胶电泳判断,热稳定的DEAE-纤维素纯化形式的葡聚糖G-75色谱法产生了纯酶。发现其Mr为43000±1500。对所有酶形式的初速度研究表明,速度对底物浓度呈双曲线依赖性,表明存在置换型机制。对于热稳定形式,Vmax随pH呈典型的钟形曲线变化,表明两个pK值分别为7.4和8.8的可电离基团对催化作用很重要。在最适pH的酸性一侧,Km随pH降低而降低,这表明游离酶或底物中不存在pK为7.4的基团的电离。