Deiters Alexander, Cropp T Ashton, Summerer Daniel, Mukherji Mridul, Schultz Peter G
Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Bioorg Med Chem Lett. 2004 Dec 6;14(23):5743-5. doi: 10.1016/j.bmcl.2004.09.059.
Here, we report a generally applicable PEGylation methodology based on the site-specific incorporation of para-azidophenylalanine into proteins in yeast. The azido group was used in a mild [3+2] cycloaddition reaction with an alkyne derivatized PEG reagent to afford selectively PEGylated protein. This strategy should be useful for the generation of selectively PEGylated proteins for therapeutic applications.