Kunitz type protease inhibitors

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

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

Patent

CA 2220497

Analogues of the Kunitz Protease Inhibitor (KPI) domain of amyloid precursor protein bind to and inhibit activity of serine proteases, including kallikrein, plasmin and coagulation factors such as factors VIIa, IXa, Xa, XIa and XIIa. Pharmaceutical compositions containing the KPI analogues, along with methods for using such compositions, are useful for ameliorating and treating clinical conditions associated with increased serine protease activity, such as blood loss related to cardiopulmonary bypass surgery. Nucleic acid sequences encoding these analogues and systems for expression of the peptides of the invention are provided.

L'invention se rapporte à des analogues du domaine des inhibiteurs de protéases de type Kunitz (KPI) d'une protéine précurseur amyloïde qui se lient et inhibent l'activité des sérine protéases, telles que la kallikréine, la plasmine, et des facteurs de coagulation tels que les facteurs VIIa, IXa, Xa, XIa et XIIa. Des compositions pharmaceutiques contenant les analogues de KPI, ainsi que les procédés d'utilisation de ces compositions, sont utiles pour améliorer et traiter des pathologies cliniques associées à l'activité de la sérine protéase, telles que des pertes de sang liées à des interventions chirurgicales impliquant une circulation extracorporelle. L'invention se rapporte également à des séquences nucléotidiques codant ces analogues et à des systèmes d'expression des peptides selon l'invention.

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