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Mono-N-terminal poly(ethylene glycol)-protein conjugates
Olaf Kinstler1, Graham Molineux, Michael Treuheit
1Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1789, USA. okinstle@amgen.com
Advanced Drug Delivery Reviews
|June 8, 2002
Abstract:
A site-directed method of joining proteins to poly(ethylene glycol) is presented which allows for the preparation of essentially homogeneous PEG-protein derivatives with a single PEG chain conjugated to the amine terminus of the protein. This selectivity is achieved by conducting the reductive alkylation of proteins with PEG-aldehydes at lower pH. Working examples demonstrating the application of this method to improve the delivery characteristics and therapeutic value of several proteins are provided.