G-csf conjugates

Details G-csf conjugates G-csf conjugates

C - Chemistry, Metallurgy

07

K

C07K 14/53 (2006.01)

Patent

CA 2452582

Polypeptide conjugates with G-CSF activity comprising a polypeptide having at least one introduced lysine residue and at least one removed lysine residue compared to the sequence of human G-CSF, and which are conjugated to 2-6 polyethylene glycol moieties. The conjugates have a lowin vitro bioactivity, a long in vivo half-life, a reduced receptor-mediated clearance, and provide a more rapid stimulation of production of white blood cells and neutrophils than non-conjugates recombinant human G-CSF.

Conjugués de polypeptides manifestant une activité de G-CSF comprenant un polypeptide possédant au moins un résidu de lysine introduit et au moins un résidu de lysine retiré en comparaison à la séquence de G-CSF humain, qui sont conjugués avec 2 à 6 groupes fonctionnels de polyéthylène glycol. Ces conjugués manifestent une faible bio-activité in vitro, une longue demi-vie in vivo, une plus faible clairance à médiation par le récepteur et assurent une stimulation plus rapide de la production de leucocytes et de neutrophiles que les G-CSF humains non recombinants.

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