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Macromolecular Ensembles of Internal and External Fibrinolysis: the Resources for Enhancement of Thrombolysis Efficacy

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Abstract:

The results of the search for new plasminogen activators for thrombolytic therapy have been reviewed with analysis of slowdown in this process. The reserves of increasing the effectiveness of thrombolysis are considered and the mechanisms underlying the interactions between plasminogen and its activators with fibrin are described. The domain composition of the fibrinolytic agents and the functional role of their structural elements in fibrinolytic interactions are discussed. The action of fibrin-specific and fibrinnonspecific plasminogen activators in fibrinolysis has been evaluated. The necessity of the investigation of the regularities of internal and external fibrinolysis has been substantiated. The internal fibrinolysis became the resource for enhancement of thrombolysis efficacy. The approaches to the use of internal fibrinolysis to increase the effectiveness of enzyme therapy (monotherapy with plasminogen or new-made plasminogen activator as well as polytherapy with combination of different plasminogen activators /thrombolysis trigger plus third-generaton plasminogen activator of prolonged action/) have been outlined and the relationship between this research and the current tendencies in the improvement of clinical thrombolysis (dose reduction, adjacent therapy, etc.) has been discussed.

Keywords: Plasminogen activators; enzyme therapy; fibrin; fibrinolysis; plasminogen; thromboses

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986706777441977

Affiliations: Institute of Experimental Cardiology, Russian Cardiology Research-and-Production Complex, 3rd Cherepkovskaya str., 15A, Moscow 121552, Russia.

Publication date: June 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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