Serine-proteases as plasminogen activators in terms of fibrinolysis

• Published in: Journal of pharmacy and pharmacology 2012-08, Vol.64 (8), p.1025-1039
• Main Authors: Flemmig, Martin, Melzig, Matthias F.
• Format: Article
• Language: English
• Subjects: Animals; Blood Coagulation - drug effects; fibrinolysis; Fibrinolysis - drug effects; Fibrinolytic Agents - pharmacology; Fibrinolytic Agents - therapeutic use; Humans; plasmin; plasminogen activator; Plasminogen Activators - pharmacology; Plasminogen Activators - therapeutic use; serine protease; Serine Proteases - pharmacology; Serine Proteases - therapeutic use; t-PA; Thrombolytic Therapy; Thrombosis - drug therapy; Tissue Plasminogen Activator - pharmacology; Tissue Plasminogen Activator - therapeutic use; Urokinase-Type Plasminogen Activator - pharmacology; Urokinase-Type Plasminogen Activator - therapeutic use
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1111/j.2042-7158.2012.01457.x

Objectives  This review should give an overview about the natural human plasminogen activators and their various modified variants as well as similar substances isolated from animals, microorganisms and plants. When a blood clot is formed in a blood vessel, it avoids the oxygen supply of the surrounding tissue. A fast fibrinolytic therapy should redissolve the blood vessel and reduce the degradation of the tissue. All proteases that are part of the human blood coagulation and fibrinolytic system belong to the serine protease family. t‐PA (tissue plasminogen activator) and u‐PA (urokinase plasminogen activator) are the naturally occurring fibrinolytic agents that are also used in therapy. Key findings  Despite many years of research, t‐PA is still the gold standard in fibrinolytic therapy. But it has to be given as an infusion, which needs time. Modified fibrinolytic substances are, were, or perhaps will be in the market. They have different advantages over t‐PA, but often the disadvantages predominate. Conclusion  Many substances have been developed but an optimal fibrinolytic agent combined with a simple administration is not in therapeutic use to date.