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Synthesis and physical properties of anti-HIV antisense oligonucleotides bearing terminal lipophilic groups
C MacKellar1, D Graham, D W Will
1Department of Chemistry, University of Edinburgh, UK.
Nucleic Acids Research
|July 11, 1992
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.