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