Thioester polymer derivatives and method of modifying the N-terminus of a polypeptide therewith
US6908963B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 9, 2001 |
| Grant date | Jun 21, 2005 |
| Priority date | — |
| Expiry date | Apr 6, 2023 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K47/60
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention provides reagents and methods for conjugating polymers specifically to the α-amine of polypeptides in high yield. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a thioester moiety capable of specifically conjugating to the α-amine of a polypeptide having a cysteine or histidine at the N-terminus. The invention provides active thioester derivatives of PEG that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG and polypeptide. Use of these active esters to prepare PEG-proteins and PEG-peptides is described.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.