Synthesis and properties of modified oligonucleotides.
Phosphorothioate oligonucleotide analogs conjugated to cholesteryl by a neutral, 6 atom linker are more effective inhibitors of HIV-1 in cell culture than the corresponding analogs conjugated via a phosphorothioate group. The antiviral activity correlates with the hydrophobic character of the oligonucleotide. Some new synthetic methodology is also discussed.
Letsinger
R L
RL
Department of Chemistry, Northwestern University, Evanston, IL 60208.
Alul
R A
RA
Farooqui
F
F
Gryaznov
S M
SM
Kinstler
O
O
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001483:Base Sequence; D002788:Cholesterol Esters / Q000138:chemical synthesis; D015497:HIV-1 / Q000187:drug effects*; D007202:Indicators and Reagents; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides / Q000138:chemical synthesis; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D002788:Cholesterol Esters; D007202:Indicators and Reagents; D009838:Oligodeoxyribonucleotides; D009841:Oligonucleotides; C027903:oligo (dT)