Tsetse thrombin inhibitor

Details Tsetse thrombin inhibitor Tsetse thrombin inhibitor

C - Chemistry, Metallurgy

12

N

C12N 15/15 (2006.01) A61K 38/57 (2006.01) A61K 39/00 (2006.01) C07K 14/435 (2006.01) C07K 14/81 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2253851

A potent and specific inhibitor of the human coagulation protease thrombin was isolated and purified from salivary gland extracts of the tsetse fly, Glossina morsitans morsitans, an important vector of African trypanosomiasis. The inhibitor is a low molecular weight polypeptide exhibiting a molecular weight of 3530 Daltons (as determined by laser desorption mass spectrometry). Amino terminal sequencing of the purified protein reveals no homology to any previously identified serine protease inhibitor or naturally occurring anticoagulant. In addition, it is also a potent inhibitor of thrombin-induced platelet aggregation. The polypeptide is useful in pharmaceutical and vaccine compositions.

Cet inhibiteur spécifique et puissant de la protéase de coagulation humaine, la thrombine, a été isolé et purifié à partir d'extraits des glandes salivaires de la mouche tsé-tsé, Glossina morsitans morsitans, un vecteur important de la trypanosomiase africaine. Cet inhibiteur est un polypeptide d'un faible poids moléculaire de 3530 Daltons (tel que déterminé par spectrométrie de masse à désorption laser). Le séquençage N-terminal de la protéine purifiée ne révèle aucune homologie avec tout inhibiteur de sérine protéase précédemment identifié ou tout anticoagulant naturel. En outre, cet inhibiteur est également un inhibiteur puissant de l'agrégation plaquettaire induite par thrombine. Ce polypeptide est utile dans des compositions pharmaceutiques et vaccinales.

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