Site-specific PEGylation of proteins containing unnatural amino acids.
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.
Deiters
Alexander
A
Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Cropp
T Ashton
TA
Summerer
Daniel
D
Mukherji
Mridul
M
Schultz
Peter G
PG
D000596:Amino Acids / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D011092:Polyethylene Glycols / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding / Q000502:physiology; D013482:Superoxide Dismutase / Q000737:chemistry / Q000378:metabolism*
D000596:Amino Acids; D011092:Polyethylene Glycols; D013482:Superoxide Dismutase