Cationic oligonucleotide− peptide conjugates with aggregating properties enter efficiently into cells while maintaining hybridization properties and enzymatic …

AW Fraley, B Pons, D Dalkara, G Nullans… - Journal of the …, 2006 - ACS Publications
AW Fraley, B Pons, D Dalkara, G Nullans, JP Behr, G Zuber
Journal of the American Chemical Society, 2006ACS Publications
Oligonucleotide delivery is a crucial issue for therapeutical purposes and is often addressed
by conjugation to short cationic peptides although with controversial results. To further
examine this mechanism, a 15-mer anionic oligonucleotide was conjugated to a cationic
peptide in order to obtain a diblock compound with an overall positive charge with
aggregation properties. These microaggregates were efficiently internalized in cells via the
expeditious pathway used by commercial gene delivery systems. Moreover, stability of the …
Oligonucleotide delivery is a crucial issue for therapeutical purposes and is often addressed by conjugation to short cationic peptides although with controversial results. To further examine this mechanism, a 15-mer anionic oligonucleotide was conjugated to a cationic peptide in order to obtain a diblock compound with an overall positive charge with aggregation properties. These microaggregates were efficiently internalized in cells via the expeditious pathway used by commercial gene delivery systems. Moreover, stability of the duplex formed with the complementary sequence increased without inhibiting oligonucleotide enzyme recognition as shown by the properties of the conjugate to prime chain elongation by Taq DNA polymerase in a linear amplification/sequencing process.
ACS Publications
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