Granulocyte colony stimulating factor: remodeling and glycoconjugation G-CSF
View Patent ↗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.
1. A granulocyte-colony stimulating factor peptide conjugate having the formula
wherein AA is a terminal or internal threonine residue of a wild type granulocyte-colony stimulating factor peptide; X 1 is a glycosyl residue comprising a modifying group and a monosaccharyl or oligosaccharyl residue; X 1 is covalently linked to AA via an intact glycosyl linking group; and u is 1, and
wherein the glycosyl residue has the formula
wherein a and b are 0; c, d, and e are 1; and R is the modifying group,
wherein the modifying group is a water-soluble polymer selected from the group consisting of poly(ethers), poly(amines) and poly(carboxylic acids).
2. The conjugate of claim 1 , wherein the water-soluble polymer is polyethylene glycol.
3. A composition comprising the conjugate of claim 1 and a carrier therefor.
4. A composition comprising the conjugate of claim 2 and a carrier therefor.