Highly efficient, nonpeptidic oligoguanidinium vectors that selectively internalize into mitochondria.
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.
Fernández-Carneado
Jimena
J
Institut de Recerca Biomèdica de Barcelona, Parc Científic de Barcelona, Josep Samitier 1, E-08028 Barcelona, Spain.
Van Gool
Michiel
M
Martos
Vera
V
Castel
Susanna
S
Prados
Pilar
P
de Mendoza
Javier
J
Giralt
Ernest
E
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
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