Site-specific PEGylation of proteins containing unnatural amino acids.

  title={Site-specific PEGylation of proteins containing unnatural amino acids.},
  author={Alexander Deiters and T. Ashton Cropp and Daniel Summerer and Mridul Mukherji and Peter G. Schultz},
  journal={Bioorganic & medicinal chemistry letters},
  volume={14 23},
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.