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Synthesis of 3 '-S-phosphorothiolate oligonucleotides for their potential use in RNA interference

Gaynor, J. W., Brazier, J. and Cosstick, R. (2007) Synthesis of 3 '-S-phosphorothiolate oligonucleotides for their potential use in RNA interference. Nucleosides Nucleotides & Nucleic Acids, 26 (6-7). pp. 709-712. ISSN 1525-7770

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To link to this item DOI: 10.1080/15257770701490753


The potency of RNA interference (RNAi) undoubtedly can be improved through chemical modifications to the small interfering RNAs (siRNA). By incorporation of the 3′-S-phosphorothiolate modification into strands of RNA, it is hoped that specific regions of a siRNA duplex can be stabilised to enhance the target binding affinity of a selected antisense strand into the activated RNA-induced silencing complex (RISC*). Oligonucleotides composed entirely of this modification are desirable so unconventional 5′ → 3′ synthesis is investigated, with initial solution-phase testing proving successful. The phosphoroamidite monomer required for solid-phase synthesis has also been produced.

Item Type:Article
Divisions:Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Medicinal Chemistry Research Group
ID Code:27314
Uncontrolled Keywords:RNA Interference, siRNA, phosphorothiolate, reverse synthesis, 5′-3′
Additional Information:Presented at the Joint Symposium of 18th International Roundtable on Nucleosides, Nucleotides and Nucleic Acids (IRTXVIII) and 35th International Symposium on Nucleic Acids Chemistry (SNAC)Times Cited: 3 Proceedings of the 17th International Roundtable of Nucleosides, Nucleotides, and Nucleic Acids MAR 07-SEP 07, 2006 Bern, SWITZERLAND

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