Prourokinase(scu-PA),a thrombolytic agent,was inserted between Gly118 and Ile119 with foreign anti-thrombosis functional motif(Lys-Gly-Asp-Trp-motif)to construct a multi-functional chimeric molecule.The molecular mode...Prourokinase(scu-PA),a thrombolytic agent,was inserted between Gly118 and Ile119 with foreign anti-thrombosis functional motif(Lys-Gly-Asp-Trp-motif)to construct a multi-functional chimeric molecule.The molecular model of a chimera was simulated and pre-dicted.The recombinant chimeric protein was expressed by the baculovirus-insect cell expression system and puri-fied by affinity chromatography.The physico-chemical characteristics of the chimeric molecule were assayed.The thrombolytic activity was determined to be 90000 IU/mg of fibrinolytic special activity by the fibrin-plate method.The anti-thrombosis activities were also assayed with IC50 of 9.6 μM by an inhibition test of ADP-induced platelet aggregation.展开更多
Stroke is usually treated by systemic thrombolytic therapy if the patient presents within an appropriate time window. There is also widespread interest in the development of thrombolytic agents that can be used in cas...Stroke is usually treated by systemic thrombolytic therapy if the patient presents within an appropriate time window. There is also widespread interest in the development of thrombolytic agents that can be used in cases of delayed presentation. Current agents that can be used in cases of delayed presentation of nerve damage by thrombus. Current systemic thrombolytic therapy is associated with adverse effects such as fibrinogenolysis and bleeding. In an attempt to increase the efficacy, safety, and specificity of thrombolytic therapy, a number of targeted thrombolytic agents have been studied in recent years. This review focuses on the concepts underlying targeted thrombolytic therapy and describes recent drug developments in this field.展开更多
基金This work was supported by the National Natural Science Foundation of China(Grant No.30540071).
文摘Prourokinase(scu-PA),a thrombolytic agent,was inserted between Gly118 and Ile119 with foreign anti-thrombosis functional motif(Lys-Gly-Asp-Trp-motif)to construct a multi-functional chimeric molecule.The molecular model of a chimera was simulated and pre-dicted.The recombinant chimeric protein was expressed by the baculovirus-insect cell expression system and puri-fied by affinity chromatography.The physico-chemical characteristics of the chimeric molecule were assayed.The thrombolytic activity was determined to be 90000 IU/mg of fibrinolytic special activity by the fibrin-plate method.The anti-thrombosis activities were also assayed with IC50 of 9.6 μM by an inhibition test of ADP-induced platelet aggregation.
基金supported by the National Natural Science Foundation of China,No.81271692
文摘Stroke is usually treated by systemic thrombolytic therapy if the patient presents within an appropriate time window. There is also widespread interest in the development of thrombolytic agents that can be used in cases of delayed presentation. Current agents that can be used in cases of delayed presentation of nerve damage by thrombus. Current systemic thrombolytic therapy is associated with adverse effects such as fibrinogenolysis and bleeding. In an attempt to increase the efficacy, safety, and specificity of thrombolytic therapy, a number of targeted thrombolytic agents have been studied in recent years. This review focuses on the concepts underlying targeted thrombolytic therapy and describes recent drug developments in this field.
