Maksimenko A V, Torchilin V P
Thromb Res. 1985 May 1;38(3):289-95. doi: 10.1016/0049-3848(85)90157-4.
The attachment of urokinase to fibrinogen via a "spacer" of aliphatic diamine increases the affinity of the modified enzyme to the fibrin clot. This provides increased (2.5-fold higher than for native urokinase) fibrinolytic activity of the modified urokinase. Modification of the enzyme does not affect its kinetic parameters, but increases its stability. It is shown that 1,12-dodecamethylenediamine is an optimal linking agent. Fibrinogen modified with diamines does not lose the ability to be co-polymerized in the three-dimensional fibrin clot under the action of thrombin and acquires increased stability towards proteolytic degradation. Use of fibrinogen as a carrier for thrombolytic drugs can increase their affinity to the injured site and enhance the local targeted action of therapeutic agent.
通过脂肪族二胺“间隔物”将尿激酶与纤维蛋白原连接,可增加修饰酶对纤维蛋白凝块的亲和力。这使得修饰后的尿激酶的纤溶活性提高(比天然尿激酶高2.5倍)。酶的修饰不影响其动力学参数,但增加了其稳定性。结果表明,1,12 - 十二亚甲基二胺是最佳连接剂。用二胺修饰的纤维蛋白原在凝血酶作用下不会丧失在三维纤维蛋白凝块中共聚的能力,并且对蛋白水解降解的稳定性增强。将纤维蛋白原用作溶栓药物的载体可增加其对损伤部位的亲和力,并增强治疗剂的局部靶向作用。