title: Site-specific PEGylation of proteins: recent developments.
abstract: The attachment of linear polyethylene glycol (PEG) to peptides and proteins for their stabilization for in vivo applications is a milestone in pharmaceutical research and protein-drug development. However, conventional methods often lead to heterogeneous PEGylation mixtures with reduced protein activity. Current synthetic efforts aim to provide site-specific approaches by chemoselective targeting of canonical and noncanonical amino acids and to improve the PEG architecture. This synopsis highlights recent work in this area, which also resulted in improved pharmacokinetics of peptide and protein therapeutics.
authors.affiliation: Leibniz-Institut für Molekulare Pharmakologie (FMP) , Robert-Rössle-Strasse 10, 13125 Berlin, Germany.
authors.forename: Nicole
authors.initials: N
authors.lastname: Nischan
authors.forename: Christian P R
authors.initials: CP
authors.lastname: Hackenberger
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods; D010455:Peptides / Q000737:chemistry* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000737:chemistry*; D011487:Protein Conformation; D011506:Proteins / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D010455:Peptides; D011506:Proteins; D011092:Polyethylene Glycols