Prolonged plasma clot lysis induced by acyl-derivatives of urokinase in vitro |
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Authors: | Roza B Aisina Liliya I Moukhametova Ekaterina F Firsova Sergei D Varfolomeyev |
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Institution: | 1. Department of Chemical Enzymology, Faculty of Chemistry, Lomonosov Moscow State University, 119899, Moscow, Russia
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Abstract: | Two acyl-derivatives of urokinase, p-trimethylam inocinnamoyl-urokinase (TMAC-Uk) and p-guanidinobenzoyl-urokinase (GB-Uk), reactivating with different rates (k reac were 6×10?4/s and 6×10?5/s, respectively) were prepared. In comparison with free urokinase, acyl-activators were more stable in human plasma, and their stability increased with the decrease in the reactivation rate. Plasma clotlysis induced by all three agents was time- and dose-dependent, but acyl-activators caused a more prolonged fibrinolysis and lengthened lag-phase than free urokinase. Slowly reactivating GB-Uk induced the most long-lasting clotlysis, whereas free urokinase was more effective for the first 3 h. A combination of GB-Uk with low dose urokinase promoted the long-lasting clotlysis with the shortened lag-phase. |
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