Synthesis of 3'- S-phosphorothiolate oligonucleotides for their potential use in RNA interference.
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.
Gaynor
James W
JW
Department of Chemistry, University of Liverpool, Liverpool, United Kingdom. j.w.gaynor@liverpool.ac.uk
Brazier
John
J
Cosstick
Rick
R
D047250:Calixarenes / Q000737:chemistry; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry; D010710:Phosphates / Q000138:chemical synthesis* / Q000737:chemistry; D034622:RNA Interference; D013777:Tetrazoles
C465503:3'-S-phosphorothiolate; D009841:Oligonucleotides; D010710:Phosphates; D013777:Tetrazoles; D047250:Calixarenes