Receptor-mediated oligodeoxynucleotides delivery by estradiol and folic acid polylysine conjugates

Abstract

The lack of efficient and specific delivery to target cells still limits the potential application of antisense oligodeoxynucleotides as therapeutic agents in cancer disease. We have covalently linked a polylysine chain (10,000-20,000 mw) to compounds as folic acid, retinoic acid, transferrin, insulin and estradiol, to deliver c-myb antisense oligonucleotide into tumor cells. Using these complexes as carriers for the oligodeoxynucleotides can be achieved an increase in their uptake into target cells through a natural endocytosis pathway.

Induction of splice correction by cell‐penetrating peptide nucleic acids

“…However, neutral PNA cannot be administrated by polycations such as polyethyleneimine or cationic liposomes like Lipofectamine 2000. Instead, various peptides have been conjugated to different ONs in order to promote uptake [14][15][16]. In particular, one class of peptides, named cell-penetrating peptides (CPPs), has been used successfully in several classical antisense experiments (i.e.…”

A DNA uptake‐stimulating protein increases the antiproliferative effect of c‐myb antisense oligonucleotide on leukemic cells

“…During the last decade, several methods were devised and proposed for the improvement of ASO uptake by mammalian cells. These include (i) lipid-based procedures (Guy-Caffey et al, 1995;Krieg et al, 1993;Lewis et al, 1996;Vello´n et al, 2002), (ii) conjugate based methods (Citro et al, 1992;Citro et al, 1993;Wu et al, 1989), (iii) polymer based techniques (Schwab et al, 1994;Tondelli et al, 1998), and (iv) other miscellaneous procedures (Pardridge and Boado, 1991;Soukchareun et al, 1995).…”