Protein c or activated protein c-like molecules

C - Chemistry – Metallurgy – 12 – N

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Details

C12N 9/64 (2006.01) A61K 38/48 (2006.01) C12N 15/57 (2006.01)

Patent

CA 2425221

The present invention relates to novel conjugates between polypeptide variants of pro-tein C and a non-polypeptide moiety, such as PEG or sugar moieties. In particular, the present invention provides novel protein C conjugates having an increased resistance to inactivation by e.g. human plasma and a1- antitrypsin. Consequently, such conjugates have an increased in vivo half- life. Preferred examples include protein C conjugates, wherein at least one additional in vivo N-glycosylation site has been introduced. The conjugates of the invention are useful for treating a variety of diseases, including septic shock.

La présente invention a trait à de nouveaux conjugués entre des variants polypeptidiques de protéine C et une fraction non polypeptidique, telle qu'une fraction PEG ou des fractions de sucre. L'invention concerne en particulier de nouveaux conjugués de protéine C présentant une résistance accrue à l'inactivation par le plasma humain ou l'.alpha.¿1?-antitrypsine par exemple. Par conséquent, de tels conjugués ont une demi-vie in vivo prolongée. Des exemples préférés comportent des conjugués de protéine C, dans lesquels au moins un site de N-glycosylation in vivo supplémentaire a été introduit. Les conjugués selon l'invention sont utiles dans le traitement de maladies diverses, notamment du choc septique.

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