Synthesis and physical properties of anti-HIV antisense oligonucleotides bearing terminal lipophilic groups.
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.
MacKellar
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C
Department of Chemistry, University of Edinburgh, UK.
Graham
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D
Will
D W
DW
Burgess
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S
Brown
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T
D001483:Base Sequence; D002784:Cholesterol / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D016655:HIV Core Protein p24 / Q000235:genetics*; D015497:HIV-1 / Q000235:genetics*; D008969:Molecular Sequence Data; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis* / Q000737:chemistry; D013696:Temperature; D013873:Thionucleotides / Q000138:chemical synthesis* / Q000737:chemistry; D014466:Ultraviolet Rays
D016655:HIV Core Protein p24; D016376:Oligonucleotides, Antisense; D013873:Thionucleotides; D002784:Cholesterol