Maksimenko A V, Tishvhenko E G, Petrov A D, Orekhova N M, Ragimov S E
Biull Eksp Biol Med. 1988 Sep;106(9):322-4.
Urokinase was covalently bounded with modified thrombin. Thrombin was modified by carbodiimide and 1, 12-dodecamethylenediamine. In this conjugate thrombin is not catalytically active and does not induce platelets aggregation. The catalytic properties of modified urokinase do not essentially differ from native enzyme but its thermostability increases. The modified urokinase thrombolytic effect is at least 10-fold higher than the native one. In femoral arteries of experimental thrombosis the conjugate urokinase-thrombin brings about total thrombolytic effect as early as 1.5 hours after injection (2500 IU per 1 kg of the animals weight). The causes of the observed effect were discussed.
尿激酶与修饰的凝血酶共价结合。凝血酶用碳二亚胺和1,12 - 十二亚甲基二胺进行修饰。在这种共轭物中，凝血酶没有催化活性，也不诱导血小板聚集。修饰的尿激酶的催化特性与天然酶基本没有差异，但其热稳定性增加。修饰的尿激酶的溶栓效果比天然尿激酶至少高10倍。在实验性血栓形成的股动脉中，尿激酶 - 凝血酶共轭物在注射后1.5小时（每1千克动物体重2500国际单位）就可产生完全的溶栓效果。文中讨论了观察到这种效果的原因。
