title: Characterization of a Cell-Penetrating Peptide with Potential Anticancer Activity.
abstract: 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 actinomycin D with high efficiency in the MCF-7 cancer cell line.
authors.affiliation: University of Cologne, Department of Chemistry, Institute of Biochemistry, Zuelpicher Str. 47, 50674, Cologne, Germany.
authors.forename: Anja
authors.initials: A
authors.lastname: Gronewold
authors.affiliation: University of Cologne, Department of Chemistry, Institute of Biochemistry, Zuelpicher Str. 47, 50674, Cologne, Germany.
authors.forename: Mareike
authors.initials: M
authors.lastname: Horn
authors.affiliation: National Institute of Oncology, Department of Experimental Pharmacology, Ráth Gy. u. 7-9, 112, Budapest, Hungary.
authors.forename: Ivan
authors.initials: I
authors.lastname: Ranđelović
authors.affiliation: National Institute of Oncology, Department of Experimental Pharmacology, Ráth Gy. u. 7-9, 112, Budapest, Hungary.
authors.forename: József
authors.initials: J
authors.lastname: Tóvári
authors.affiliation: University Hospital of Cologne, Department of Nuclear Medicine, Kerpener Str. 62, 50937, Cologne, Germany.
authors.forename: Sergio
authors.initials: S
authors.lastname: Muñoz Vázquez
authors.affiliation: University Hospital of Cologne, Department of Nuclear Medicine, Kerpener Str. 62, 50937, Cologne, Germany.
authors.forename: Klaus
authors.initials: K
authors.lastname: Schomäcker
authors.affiliation: University of Cologne, Department of Chemistry, Institute of Biochemistry, Zuelpicher Str. 47, 50674, Cologne, Germany.
authors.forename: Ines
authors.initials: I
authors.lastname: Neundorf
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D057846:Cell-Penetrating Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003609:Dactinomycin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D057846:Cell-Penetrating Peptides; D003609:Dactinomycin
keywords: anticancer activity; cell-penetrating peptides; lytic peptides; tumor cells; tumor targeting