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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Aisina, R.B., Moukhametova, L.I., Firsova, E.F. et al. Prolonged plasma clot lysis induced by acyl-derivatives of urokinase in vitro. Appl Biochem Biotechnol 88, 137–143 (2000). https://doi.org/10.1385/ABAB:88:1-3:137
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DOI: https://doi.org/10.1385/ABAB:88:1-3:137