Centre National De La Recherche Scientifique

Universitéde Strasbourg

Polyplus Transfection

Centre National De La Recherche Scientifique-Cnrs

Bénédicte Pons

Jean-Paul Behr

Mitsuharu Kotera

Jean-Serge Remy

Emilie Voirin

The invention relates to oligonucleotide-oligocation molecules ABH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein &#x2022;Ais an i-mer oligonucleotide residue, with i=5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical modifications or substitutions such as phosphorothioate, 2'-fluoro, 2&#x2032;-O-alkyl, or a marker group such as a fluorescent agent, &#x2022;Bj is a j-mer organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising &#x2022;&#x2014;HPO&#x2014;R&#x2014;(X&#x2014;R)&#x2014;X&#x2014;R&#x2014;O&#x2014;, where R, Rn and R, identical or different, are lower alkylene, X is NH or NC(NH), n varies from 1 to 5 and n1=2 to 20, &#x2022;&#x2014;HPO&#x2014;R&#x2014;CH(RX)&#x2014;R&#x2014;O&#x2014;, where Ris lower alkylene, Rand R, identical or different, are lower alkylene and Xis putrescine, spermidine or spermine residue, &#x2022;&#x2014;HPO&#x2014;R-(aa)-R&#x2014;O&#x2014;, where Ris lower alkylene and Ris lower alkylene, serine, a natural aminoalcohol, (aa)is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, -Histidine, Diaminopropionic acid and n2=2 to 20.

Cationic oligonucleotides, automated methods for preparing same and their uses

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Strasbourg, France

Bénédicte Pons