Patent ID: 6423685
Filing Date: 2002-07-23
Classification: A61K,C07K,C12N,C12Y

Abstract:
A method for conjugating urokinase plasminogen activator1-48 having adjacent amino and alcohol groups at the N-terminus thereof to polyethylene glycol in the form of polyethylene glycol hydrazide or semicarbazide, comprising:(a) oxidatively cleaving between the adjacent amino and alcohol groups to yield an aldehyde functionality in place thereof, and (b) reacting the aldehyde-containing urokinase plasminogen activator1-48 provided in step (a) with the polyethylene glycol hydrazide or semicarbazide under reaction conditions effective to promote formation of PEGylated polypeptide, wherein the polypeptide is bound to polyethylene glycol through a hydrazone or semicarbazone linkage.