Cationic oligonucleotide-peptide conjugates with aggregating properties enter efficiently into cells while maintaining hybridization properties and enzymatic recognition.
Fiche publication
Date publication
août 2006
Auteurs
Membres identifiés du Cancéropôle Est :
Dr ZUBER Guy
Tous les auteurs :
Fraley AW, Pons B, Dalkara D, Nullans G, Behr JP, Zuber G
Lien Pubmed
Résumé
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.
Référence
J Am Chem Soc. 2006 Aug 23;128(33):10763-71.