Hendrix H, Lindhout T, Mertens K, Engels W, Hemker H C
J Biol Chem. 1983 Mar 25;258(6):3637-44.
The activation of human prothrombin by the bacterial protein staphylocoagulase proceeds via the formation of a very stable equimolar complex. Unmasking of the active center in the prothrombin moiety of the complex is not caused by limited proteolysis. The kinetics of activation of human prothrombin by staphylocoagulase has been studied. The second order rate constant at pH 7.5, 37 degrees C, is 3.3 X 10(6) M-1 S-1. This reaction rate is close to reported diffusion-controlled rates of protein-protein interaction. The dissociation constant of the complex was too low to be measurable. From the kinetic data it is assumed that the first order rate constant for dissociation is orders of magnitude less than 10(-5) S-1. However, dissociation of the complex did occur in the presence of sodium dodecyl sulfate. Equimolar amounts of staphylocoagulase protect human thrombin, but not human factor Xa and bovine thrombin, against inactivation by antithrombin III. From these findings we postulate that tertiary structural changes in the thrombin region of prothrombin caused by a highly specific interaction between staphylocoagulase and that region unmask the active site.
细菌蛋白葡萄球菌凝固酶激活人凝血酶原的过程是通过形成一种非常稳定的等摩尔复合物来进行的。复合物中凝血酶原部分活性中心的暴露不是由有限的蛋白水解引起的。已经研究了葡萄球菌凝固酶激活人凝血酶原的动力学。在pH 7.5、37℃时的二级速率常数为3.3×10⁶ M⁻¹ s⁻¹。该反应速率接近报道的蛋白质-蛋白质相互作用的扩散控制速率。复合物的解离常数太低以至于无法测量。根据动力学数据推测,解离的一级速率常数比10⁻⁵ s⁻¹小几个数量级。然而,在十二烷基硫酸钠存在的情况下复合物确实发生了解离。等摩尔量的葡萄球菌凝固酶可保护人凝血酶,但不能保护人因子Xa和牛凝血酶不被抗凝血酶III灭活。根据这些发现我们推测,葡萄球菌凝固酶与凝血酶原的该区域之间高度特异性的相互作用导致凝血酶原的凝血酶区域发生三级结构变化,从而暴露了活性位点。