Amide Backbones with Conformationally Restricted Furanose Rings: Highly Improved Affinity of the Modified Oligonucleotides for Their RNA Complements

Amide Backbones with Conformationally Restricted Furanose Rings: Highly Improved Affinity of the Modified Oligonucleotides for Their RNA Complements

An increased stability of duplexes between amide‐modified oligonucleotides (depicted on the right) and RNA was achieved by the introduction of 2′‐OMe groups. Since the modified oligonucleotides display a very high affinity for their RNA complement and are more stable towards nucleases, they can be c...

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Veröffentlicht in:Angewandte Chemie International Edition 1996-12, Vol.35 (23-24), p.2790-2794
Hauptverfasser: De Mesmaeker, Alain, Lesueur, Catherine, Bévièrre, Marc-Olivier, Waldner, Adrian, Fritsch, Valérie, Wolf, Romain M.
Format: Artikel
Sprache:eng
Schlagworte:
amides
antisense oligonucleotides
deoxysugars
molecular modeling
nucleic acids
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Zusammenfassung:An increased stability of duplexes between amide‐modified oligonucleotides (depicted on the right) and RNA was achieved by the introduction of 2′‐OMe groups. Since the modified oligonucleotides display a very high affinity for their RNA complement and are more stable towards nucleases, they can be considered as promising antisense agents. X = H, OH, OMe; Y = H, OMe.
ISSN:0570-0833
1521-3773
DOI:10.1002/anie.199627901