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Nucleic Acids Research, 1992, Vol. 20, No. 13 3411-3417
© 1992

MOLECULAR BIOLOGY

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

Calum MacKellar, Duncan Graham, David W. Will, Stephen Burgess1 and Tom Brown*

Edinburgh Centre for Molecular Recognition, Department of Chemistry, University of Edinburgh West Mains Road, Edinburgh EH9 3JJ, UK 1Institute of Cell, Animal and Population Biology, Division of Biological Sciences, University of Edinburgh West Mains Road, Edinburgh EH9 3JJ, UK

* To whom correspondence should be addressed

Received March 19, 1992. Revised June 5, 1992. Accepted June 5, 1992.

A number of phosphoramldite 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.


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