Journal
JOURNAL OF PEPTIDE SCIENCE
Volume 22, Issue 6, Pages 421-426Publisher
WILEY
DOI: 10.1002/psc.2885
Keywords
cell-penetrating peptides; click-reaction; drug delivery; peptide synthesis
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In this work we report synthesis and biological evaluation of a cell-penetrating peptide (CPP), that is partly cyclized via a triazole bridge. Recently, beneficious properties have been reported for cyclized peptides concerning their metabolic stability and intracellular uptake. A CPP based on human calcitonin was used in this study, and side chain cyclization was achieved via copper catalyzed alkyne-azide click reaction. Cell viability studies in several cell-lines revealed no cytotoxic effects. Furthermore, efficient uptake in breast cancer MCF-7 cells could be determined. Moreover, preliminary studies using this novel peptide as drug transporter for daunorubicin were performed. Copyright (c) 2016 European Peptide Society and John Wiley & Sons, Ltd.
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