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Serum protease- degradable peptide linkers to control antimicrobial peptide release

Customized peptide linkers that are degraded by serum proteases could be used to control the release of therapeutic peptides from pegylated prodrugs. Antimicrobial peptides were conjugated to polyethylene glycol (PEG) using peptide linkers of up to five amino acids containing sequences recognized by serum proteases. In mouse sera, the release rate of the antimicrobial peptides and resulting antimicrobial activity were modulated in a linker-dependent manner. Ongoing studies include evaluating additional linker peptides to determine the extent that release kinetics can be modulated and applying the approach to other therapeutic peptides.

SciBX 6(28); doi:10.1038/scibx.2013.739
Published online July 25, 2013

Patent application filed; available for licensing

Nollmann, F.I. et al. Angew. Chem. Int. Ed.; published online June 13, 2013;
Contact: Ralf Hoffmann, Leipzig University, Leipzig, Germany