Comparison of rigid and flexible backbones in antisense oligonucleotides

Stepwise restriction of free rotation, as well as introduction of positive changes in the internucleosidic linkage are factors which can positively influence the thermal melting behaviour of the corresponding duplexes formed between modified DNA and their RNA complement. By correct positioning of th...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1994-02, Vol.4 (3), p.395-398
Main Authors: De Mesmaeker, Alain, Waldner, Adrian, S. Sanghvi, Yogesh, Lebreton, Jacques
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
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Summary:Stepwise restriction of free rotation, as well as introduction of positive changes in the internucleosidic linkage are factors which can positively influence the thermal melting behaviour of the corresponding duplexes formed between modified DNA and their RNA complement. By correct positioning of the rigidity within backbone, it is possible to achieve even higher binding affinity (T m's) than with natural oligodeoxyribonucleotides (ODNs). Stepwise restriction of free rotation, as well as introduction of positive charges in the internucleosidic linkage are factors which can positively influence the thermal melting behaviour of the corresponding duplexes formed between modified DNA and their RNA complement. By correct positioning of the rigidity within the backbone, it is possible to achieve even higher binding affinity (T m's) than with natural oligodeoxyribonucleotides.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(94)80003-0