Patent · US Expired

Cysteine-pegylated proteins

US5766897A · kind A · utility

209Cited by
40References
10Claims
0Family size

Assignee

Inventor

Key dates

Filing dateApr 21, 1995
Grant dateJun 16, 1998
Priority date
Expiry dateApr 21, 2015

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K38/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

Methods and compositions are provided for the production of PEGylated proteins having polyethylene glycol covalently bound to a cysteine residue present in either the naturally-occurring protein or introduced by site-specific mutation. Where the cysteine residue is introduced by mutation, the site for mutation is selected on the basis of the presence of an N-linked glycosylation site or the position of the residue which is normally solvent-accessible in the naturally-occurring protein. The modified proteins produced by the method of the invention are referred to as cysteine-PEGylated proteins. Proteins PEGylated according to the invention have increased half-lives following administration to a subject and decreased immunogenicity and antigenicity, while retaining substantially the same level of biological activity as that of the naturally-occurring, unmodified protein. Modification of proteins according to methods of the invention thus provide improved pharmaceutical compositions.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.