title: 5'-linked lipid-oligodeoxyridonucleotide derivatives as inhibitors of human immunodeficiency virus replication.
abstract: The covalent attachment of a phospholipid moiety, bound to the 5'-ends of phosphodiester and phosphorothioate oligonucleotides (L-ODNs and LS-ODNs), was achieved using H-phosphonate chemistry, and the lipid-oligonucleotides were assayed for the inhibition of virus replication in HIV-1 infected MT-4 cells. In the anti-HIV activity test, lipid-phosphorothioate oligonucleotides showed higher anti-HIV activities than non-lipid-phosphorothioate oligonucleotides, at the low concentration of 0.04 microM. LS-ODNs can inhibit HIV-1 reverse transcriptase activity through interactions with the enzyme. We found that the covalent attachment of a phospholipid group to the 5'-end of the phosphorothioate oligonucleotide enhances its nonsequence specific anti-HIV activity.
authors: Department of Industrial Chemistry, Chiba Institute of Technology, Japan.
authors: S G
authors: SG
authors: Kim
authors: H
authors: H
authors: Nakashima
authors: Y
authors: Y
authors: Shoji
authors: T
authors: T
authors: Inagawa
authors: N
authors: N
authors: Yamamoto
authors: Y
authors: Y
authors: Kinzuka
authors: K
authors: K
authors: Takai
authors: H
authors: H
authors: Takaku
mesh_terms: D001483:Base Sequence; D002461:Cell Line, Transformed / Q000166:cytology; D004305:Dose-Response Relationship, Drug; D006678:HIV / Q000187:drug effects* / Q000472:pathogenicity / Q000502:physiology; D006801:Humans; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides / Q000737:chemistry*; D010743:Phospholipids / Q000737:chemistry*; D012194:RNA-Directed DNA Polymerase / Q000187:drug effects* / Q000378:metabolism; D014779:Virus Replication / Q000187:drug effects* / Q000502:physiology
chemical_list: D009838:Oligodeoxyribonucleotides; D010743:Phospholipids; D012194:RNA-Directed DNA Polymerase