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

Mackellar, C. and Graham, D. and Will, D.W. and Burgess, S. and Brown, T. (1992) Synthesis and physical properties of anti-HIV antisense oligonucleotides bearing terminal lipophilic groups. Nucleic Acids Research, 20 (13). pp. 3411-3417. ISSN 0305-1048

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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.