Journal
TETRAHEDRON
Volume 68, Issue 23, Pages 4406-4412Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.02.003
Keywords
gamma-Peptides; Anticancer; Antimicrobial peptides; Cell-penetrating peptides; Foldamers
Categories
Funding
- Spanish Ministry of Science and Innovation (MICINN) [CTQ2008-00177, CTQ2009-07758, CIT-090000-2008-10]
- Generalitat de Catalunya [2009SGR 1024]
- Institute for Research in Biomedicine
- Barcelona Science Park
- CIBER-BBN, Networking Centre on Bioengineering, Biomaterials, and Nanomedicine
- University of Girona
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In this study, we combined a cell-penetrating gamma-peptide, PEG-1, with antimicrobial undecapeptides in order to provide compounds with anticancer properties against MDA-MB-231 human breast cancer cells. We demonstrated that the conjugates were more cytotoxic than Ac-PEG-1 and the parent undecapeptides. We also evaluated the toxicity of the conjugates against non-malignant cells. The peptide conjugate with the best biological profile was BP77-PEG-1, which, at 10 mu M, showed a 71% growth inhibition in MDA-MB-231 cells and only a 17% inhibition in non-malignant cells. Therefore, this study suggests that PEG-1 mediated the undecapeptide delivery into cancer cells and that these conjugates are the proof-of-concept of this strategy to generate improved anticancer drugs based on peptides. (C) 2012 Elsevier Ltd. All rights reserved.
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