Reichart, Florian, Horn, Mareike and Neundorf, Ines ORCID: 0000-0001-6450-3991 (2016). Cyclization of a cell-penetrating peptide via click-chemistry increases proteolytic resistance and improves drug delivery. J. Pept. Sci., 22 (6). S. 421 - 427. HOBOKEN: WILEY. ISSN 1099-1387

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Abstract

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.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Reichart, FlorianUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Horn, MareikeUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Neundorf, InesUNSPECIFIEDorcid.org/0000-0001-6450-3991UNSPECIFIED
URN: urn:nbn:de:hbz:38-273272
DOI: 10.1002/psc.2885
Journal or Publication Title: J. Pept. Sci.
Volume: 22
Number: 6
Page Range: S. 421 - 427
Date: 2016
Publisher: WILEY
Place of Publication: HOBOKEN
ISSN: 1099-1387
Language: English
Faculty: Faculty of Mathematics and Natural Sciences
Divisions: Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Biochemistry
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
HUMAN CALCITONIN; CARRIER PEPTIDES; ACIDMultiple languages
Biochemistry & Molecular Biology; Chemistry, AnalyticalMultiple languages
Refereed: Yes
URI: http://kups.ub.uni-koeln.de/id/eprint/27327

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