Thrombolytic agents.
Thrombolytic agents are plasminogen activators that convert the zymogen plasminogen to the active enzyme plasmin, which degrades fibrin. Elucidation of the molecular mechanism of physiological fibrinolysis opened up a new era of fibrin-specific thrombolysis. Fibrin-specific plasminogen activators, including tissue-type plasminogen activator (t-PA), single-chain urokinase-type plasminogen activator (scu-PA) and staphylokinase (Sak), preferentially activate fibrin-associated plasminogen. Generated plasmin remains associated with fibrin, where it is protected from rapid inhibition and can efficiently degrade fibrin, avoiding systemic activation of the fibrinolytic system. Following a decade of clinical investigation t-PA and variants thereof are routinely used for treatment of patients with thromboembolic disease.
Collen
Désiré
D
Center for Molecular and Vascular Biology, KU Leuven, Herestraat 49, B-3000 Leuven, Belgium. desire.collen@med.kuleuven.ac.be
Lijnen
H Roger
HR
D005343:Fibrinolytic Agents / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D006801:Humans; D008666:Metalloendopeptidases / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D010959:Tissue Plasminogen Activator / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D014568:Urokinase-Type Plasminogen Activator / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use
D005343:Fibrinolytic Agents; D010959:Tissue Plasminogen Activator; D014568:Urokinase-Type Plasminogen Activator; D008666:Metalloendopeptidases; C022653:auR protein, Staphylococcus aureus