title: Highly efficient, nonpeptidic oligoguanidinium vectors that selectively internalize into mitochondria.
abstract: Oligoguanidinium-based cell delivery systems have gained broad interest in the drug delivery field since one decade ago. Thus, arginine-containing peptides as Tat or Antp, oligoarginine peptides, and derived peptoids have been described as shuttles for delivering nonpermeant drugs inside cancer cells. Herein we report a new family of tetraguanidinium cell penetrating vectors efficiently internalized in human tumor cells. Their high internalization, studied by confocal microscopy and flow cytometry, as well as their specific accumulation in mitochondria makes these new vectors likely vehicles for the targeted delivery of anticancer drugs to mitochondria.
authors.affiliation: Institut de Recerca Biomèdica de Barcelona, Parc Científic de Barcelona, Josep Samitier 1, E-08028 Barcelona, Spain.
authors.forename: Jimena
authors.initials: J
authors.lastname: Fernández-Carneado
authors.forename: Michiel
authors.initials: M
authors.lastname: Van Gool
authors.forename: Vera
authors.initials: V
authors.lastname: Martos
authors.forename: Susanna
authors.initials: S
authors.lastname: Castel
authors.forename: Pilar
authors.initials: P
authors.lastname: Prados
authors.forename: Javier
authors.initials: J
authors.lastname: de Mendoza
authors.forename: Ernest
authors.initials: E
authors.lastname: Giralt
mesh_terms: D000595:Amino Acid Sequence; D051943:Antennapedia Homeodomain Protein; D016503:Drug Delivery Systems; D005434:Flow Cytometry; D015696:Gene Products, tat / Q000493:pharmacokinetics; D019791:Guanidine / Q000493:pharmacokinetics* / Q000494:pharmacology; D006367:HeLa Cells; D018398:Homeodomain Proteins / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D018613:Microscopy, Confocal; D008928:Mitochondria / Q000378:metabolism*; D008969:Molecular Sequence Data; D009687:Nuclear Proteins / Q000493:pharmacokinetics / Q000494:pharmacology; D009757:Nylons / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D009842:Oligopeptides / Q000493:pharmacokinetics / Q000494:pharmacology; D010446:Peptide Fragments / Q000493:pharmacokinetics / Q000494:pharmacology; D014157:Transcription Factors / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D051943:Antennapedia Homeodomain Protein; D015696:Gene Products, tat; D018398:Homeodomain Proteins; D009687:Nuclear Proteins; D009757:Nylons; D009842:Oligopeptides; D010446:Peptide Fragments; D014157:Transcription Factors; D019791:Guanidine