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Highly Efficient, Nonpeptidic Oligoguanidinium Vectors that Selectively Internalize into Mitochondria
journal contribution
posted on 2005-01-26, 00:00 authored by Jimena Fernández-Carneado, Michiel Van Gool, Vera Martos, Susanna Castel, Pilar Prados, Javier de Mendoza, Ernest GiraltOligoguanidinium-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.