title: Inhibition of HIV-1 in vitro by C-5 propyne phosphorothioate antisense to rev.
abstract: A 15-mer C-5 propyne modified phosphorothioate oligodeoxynucleotide antisense to rev was approximately 5-fold more effective in providing viral inhibition compared to a 28-mer unmodified phosphorothioate oligodeoxynucleotide targeted to the same sequence and previously shown to inhibit HIV-1 in a sequence-dependent manner. The antiviral effect was obtained by lipofection or simple addition of 0.2-1 microM modified oligodeoxynucleotide to the culture medium of H9 cells chronically infected with the HIV-1LAI isolate of human immunodeficiency virus type 1. We conclude that C-5 propyne oligodeoxynucleotides in accordance with previous findings by others are superior to unmodified phosphorothioates in providing inhibition of HIV-1 in a sequence-dependent manner and that this inhibition can be conferred by oligodeoxynucleotides in free solution.
authors.affiliation: Laboratory for Infectious Diseases, Department 144, Hvidovre Hospital, Denmark.
authors.forename: O S
authors.initials: OS
authors.lastname: Lund
authors.forename: J O
authors.initials: JO
authors.lastname: Nielsen
authors.forename: J E
authors.initials: JE
authors.lastname: Hansen
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D001483:Base Sequence; D015757:Genes, rev; D015488:HIV Antigens / Q000032:analysis; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008969:Molecular Sequence Data; D016376:Oligonucleotides, Antisense / Q000737:chemistry / Q000494:pharmacology*; D010714:Phosphatidylethanolamines / Q000494:pharmacology; D012367:RNA, Viral; D013329:Structure-Activity Relationship; D013873:Thionucleotides / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors; D014407:Tumor Cells, Cultured
chemical_list: D000998:Antiviral Agents; D015488:HIV Antigens; D016376:Oligonucleotides, Antisense; D010714:Phosphatidylethanolamines; D012367:RNA, Viral; D013873:Thionucleotides; C020888:1,2-dielaidoylphosphatidylethanolamine