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Controlled Systemic Release of Therapeutic Peptides from PEGylated Prodrugs by Serum Proteases
Author(s) -
Nollmann Friederike Inga,
Goldbach Tina,
Berthold Nicole,
Hoffmann Ralf
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201301533
Subject(s) - pegylation , prodrug , proteases , peptide , linker , computer science , chemistry , peg ratio , computational biology , biochemistry , pharmacology , enzyme , medicine , biology , business , polyethylene glycol , finance , operating system
A novel concept to release peptidic drugs systemically by serum proteases from a PEGylated precursor makes it possible to tune release kinetics to fit the medical needs. Drug release depends on the size of the PEG polymer and the sequence and length of the peptide linker. The antimicrobial activities of the prodrugs were even better than those of the free peptides, whereas direct PEGylation abolished the peptide activity.