Plasminogen activator capable of being activated by thrombin

Details Plasminogen activator capable of being activated by thrombin Plasminogen activator capable of being activated by thrombin

C - Chemistry, Metallurgy

12

N

C12N 9/64 (2006.01) A61K 38/49 (2006.01) C12N 9/72 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2262751

A plasminogen activator (t-PA) is (a) modified in such a way that it can be split by thrombin and thus turned into its two-chain form; (b) modified in such a way that its zymogenity is at least 1.2 higher than that of t-PA; and (c) its fibrin binding power is so reduced that more than 50 % of the plasminogen activator can enter a blood clot. This plasminogen activator has an improved fibrin-specificity and less side effects.

L'invention concerne un activateur du plasminogène (t-PA) qui a) est modifié de manière que l'activateur du plasminogène soit clivable par thrombine et soit transformé dans la forme à deux chaînes suite à un tel clivage, b) est modifié de manière que comparativement à t-PA, la zymogénité soit supérieure d'au moins un facteur 1,2, et c) dont la liaison à la fibrine est réduite jusqu'à ce que plus de 50 % de l'activateur du plasminogène puisse pénétrer dans un caillot de sang. Cet activateur du plasminogène (t-PA) présente une spécificité fibrinique améliorée et des effets secondaires moindres.

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