Site-specific PEGylation of Proteins: Recent Developments

N. Nischan, C.P.R. Hackenberger – 2014

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.

Titel
Site-specific PEGylation of Proteins: Recent Developments
Verfasser
N. Nischan, C.P.R. Hackenberger
Datum
2014
Kennung
10.1021/jo502136n
Zitierweise
J. Org. Chem., 2014, 79(22), 10727–10733
Art
Text
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