| Site-specific polyethylene glycol (PEG) modification is the PEGylation of specific site of the protein. Compared with
non-specific PEGylation, the advantages of site-specific PEGylation are the uniqueness of PEGylated site , no interference of modified
isomers, preserved activity in vitro and in vivo; the modified product is homogeneous, stable, and convenient for quality control, and can
reduce side effects of modified isomers, increase production yield and decrease costs. Site-specific PEGylation protein drugs are already
on the market, others are still in clinical trials. This paper reviews the research progress of technique and clinical development of
site-specific PEGylated protein drugs, including typical site-specific PEG modifiers, general methods of site-specific PEGylation,
site-specific PEGylated drugs on the market and in clinical development, and problems faced with by researchers, and looks into the
future development of site-specific PEG modification technique. |
