Synthesis and physical properties of anti-HIV antisense oligonucleotides bearing terminal lipophilic groups

C. Mackellar, D. Graham, D.W. Will, S. Burgess, T. Brown

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Abstract

A number of phosphoramidite monomers have been prepared and used in the synthesis of antisense phosphorothioate oligonucleotides bearing 5'-polyalkyl and cholesterol moieties. Similar groups have also been attached to the 3'-end of oligonucleotides by means of functionalised CPG. Melting temperatures of duplexes formed between phosphorothioate oligonucleotides with lipophilic end-groups and complementary DNA strands were found to be identical to those formed by the equivalent unmodified phosphorothioates.
Original languageEnglish
Pages (from-to)3411-3417
Number of pages6
JournalNucleic Acids Research
Volume20
Issue number13
DOIs
Publication statusPublished - 11 Jul 1992

Keywords

  • human immunodeficiency virus
  • phosphorothioate oligodeoxynucleotide
  • cells
  • derivatives
  • cholesterol
  • inhibitors
  • infection
  • invitro

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