abstract |
This invention relates to a polypeptide-polymer conjugate that includes a polypeptide moiety, a polyalkylene oxide moiety, a linker connecting the polypeptide moiety with the polyalkylene oxide moiety, a first linkage between the polypeptide moiety and the linker, and a second linkage between the polyalkylene oxide moiety and the linker. The polypeptide moiety can contain a human interferon-α moiety and 1-6 additional amino acid residues at the N-terminus of the human interferon-α moiety. The polyalkylene oxide moiety can contain 1-20,000 C1-C8 alkylene oxide repeating units. The linker can be C1-C8 alkylene, C1-C8 heteroalkylene, C3-C8 cycloalkylene, C3-C8 heterocycloalkylene, arylene, heteroarylene, aralkylene, or -Ar-X-(CH2)n-, in which Ar can be arylene or heteroarylene, X can be O,S, or N(R), R being H or C1-C10 alkyl, and n can be 1-10. Each of the first and second linkages, independently, can be a carboxylic ester, carbonyl, carbonate, amide, carbamate, urea, ether, thio, sulfonyl, sulfinyl, amino, imino, hydroxyamino, phosphonate, or phosphate group. |