Intracellular transfer of antisense oligonucleotides could be utilized for the development of new therapeutic approaches. Cellular uptake is greatly enhanced by conjugation of oligonucleotides to cell-penetrating peptides (CPPs), with minimal cytotoxicity observed. A novel CPP, BagP, derived from the normally expressed human protein Bag-1, was evaluated for its potential to ferry intracellularly, biologically-active oligonucleotides. An antisense oligonucleotide against c-myc, AACGTTGAGGGGCAT (antimyc-aug), was conjugated for this reason to BagP. The [BagP+antimyc-aug] conjugate was found to penetrate all cell lines tested at varying degrees. The internalization of the conjugate was found to silence c-myc, causing a severe decrease in the proliferation rate of the cells, that was further supported by a decrease found on the level of intracellular c-Myc protein.
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