Journal
CHEMMEDCHEM
Volume 12, Issue 1, Pages 42-49Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201600498
Keywords
anticancer activity; cell-penetrating peptides; lytic peptides; tumor cells; tumor targeting
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Funding
- Jurgen-Manchot Stiftung (Germany)
- European Union [642004]
- Hungarian National Science Fund [OTKA K116295]
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Cell-penetrating peptides (CPPs) are still an interesting and viable alternative for drug delivery applications. CPPs contain considerably high amounts of positively charged amino acids, imparting them with cationic character. Tumor cells are characterized by an enhanced anionic nature of their membrane surface, a property that could be used by CPPs to target these cells. We recently identified a branched CPP that displays a high internalization capacity while exhibiting selectivity for certain tumor cell types. In this study we elucidated this observation in greater detail by investigating the underlying mechanism behind the cellular uptake of this peptide. An additional cytotoxicity screen against several cancer cell lines indeed demonstrates high cytotoxic activity against cancer cells over normal fibroblasts. Furthermore, we show that this feature can be used for delivering the anticancer drug actinomycinD with high efficiency in the MCF-7 cancer cell line.
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