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Backbone Modification of Nucleic Acids: Synthesis, Structure and Therapeutic Applications

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Nucleic acids have been extensively modified by replacing the phosphodiester group or the whole sugar-phosphodiester backbone with alternative anionic, neutral and cationic structures. Several of these modified oligonucleotides exhibit improved properties including enhanced recognition and binding to RNA, duplex DNA and proteins. This has resulted in the development of new and more potent antisense and antigene agents, as well as aptamers. Furthermore, backbone modified oligonucleotides have also been used in the development of several alternative strategies, which rely on altogether different mechanisms of action and show significant promise for therapeutic intervention. In this review the latest advances in the synthesis and evaluation of the most promising backbone modified oligos will be discussed, with a view to their future as novel pharmaceuticals.

Keywords: Boranophosphate Oligos; Deoxyribonucleic Guanidine (DNG) Oligos; Methylphosophonates; Morpholino Oligos; Nucleic Acids Synthesis; Phosphoramidate Modification; Therapeutic Targets; antigene agents; aptamers; potent antisense

Document Type: Review Article


Publication date: August 1, 2001

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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