IP Library › Granted Patent US 8,853,161
Granted Patent B2
US 8,853,161 · App. 13/246,512 · Granted Oct 7, 2014

Glycopegylation methods and proteins/peptides produced by the methods

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Quick Facts
Patent No.
US 8,853,161
App. No.
13/246,512
Granted
Oct 7, 2014
Kind
B2
Abstract

The invention includes methods and compositions for remodeling a peptide molecule, including the addition or deletion of one or more glycosyl groups to a peptide, and/or the addition of a modifying group to a peptide.

Claims (18)

1. A covalent conjugate between Factor IX and a water-soluble polymer selected from the group consisting of poly(ethers), poly(amines), and poly(carboxylic acids), wherein said water-soluble polymer is covalently attached to Factor IX through an intact glycosyl linking group.

2. The covalent conjugate according to claim 1 , wherein said water-soluble polymer is a poly(ether).

3. The covalent conjugate according to claim 2 , wherein said poly(ether) is a poly(alkylene oxide).

4. The covalent conjugate according to claim 3 , wherein said poly(alkylene oxide) is a poly(ethylene glycol).

5. The covalent conjugate according to claim 4 , wherein said poly(ethylene glycol) is a member selected from linear poly(ethylene glycol) and branched poly(ethylene glycol).

6. The covalent conjugate according to claim 4 , wherein said poly(ethylene glycol) has a degree of polymerisation of from about 1 to about 5,000.

7. The covalent conjugate according to claim 6 , wherein said poly(ethylene glycol) has a degree of polymerisation of from about 1 to about 1,000.

8. The covalent conjugate according to claim 1 , wherein said intact glycosyl linking group is attached to a member selected from a carbohydrate moiety, an amino acid moiety and combinations thereof.

9. The covalent conjugate according to claim 8 , wherein said intact glycosyl linking group is attached to a carbohydrate moiety, wherein the carbohydrate moiety is an O- or N-linked glycan, or combination thereof.

10. The covalent conjugate according to claim 8 , wherein said intact glycosyl linking group is attached to a hydroxyl or amino group or a combination thereof of an amino acid moiety.

11. The covalent conjugate according to claim 8 , wherein said intact glycosyl linking group comprises sialic acid, galactose, N-acetylglucosamine or N-acetylgalactosamine residue.

12. The covalent conjugate according to claim 1 , wherein said water-soluble polymer is attached to a sialic acid residue at the 5- or 9-position of said sialic acid.

13. A pharmaceutical composition comprising the covalent conjugate according to claim 1 and a pharmaceutically acceptable diluent.

14. A cell-free, in vitro method of forming a covalent conjugate between Factor IX and a water-soluble polymer selected from the group consisting of poly(ethers), poly(amines), and poly(carboxylic acids), wherein said water-soluble polymer is covalently attached to Factor IX through an intact glycosyl linking group, said method comprising:

contacting Factor IX with a mixture comprising at least one nucleotide sugar covalently linked to said water soluble polymer and at least one glycosyltransferase for which said nucleotide sugar is a substrate, thereby forming said covalent conjugate of Factor IX.

15. The method according to claim 14 , wherein said water-soluble polymer is a poly(ether).

16. The method according to claim 15 , wherein said poly(ether) is a poly(ethylene glycol).

17. The method of claim 14 , wherein said glycosyltransferase is selected from the group consisting of sialyltransferase, galactosyltransferase, glucosyltransferase, GalNAc transferase, GlcNAc transferase, fucosyltransferase, and mannosyltransferase.