Newly designed six-membered azasugar nucleotide-containing phosphorothioate oligonucleotides as potent human immunodeficiency virus type 1 inhibitors.

ABSTRACT: A series of modified oligonucleotides (ONs), characterized by a phosphorothioate (P S) backbone and a six-membered azasugar (6-AZS) as a sugar substitute in a nucleotide, were newly synthesized and assessed for their ability to inhibit human immunodeficiency virus type 1 (HIV-1) via simple treatment of HIV-1-infected cultures, without any transfection process. While unmodified P S ONs exhibited only minor anti-HIV-1 activity, the six-membered azasugar nucleotide (6-AZN)-containing P S oligonucleotides (AZPSONs) exhibited remarkable antiviral activity against HIV-1/simian-human immunodeficiency virus (SHIV) replication and syncytium formation (50% effective concentration = 0.02 to 0.2 microM). The AZPSONs exhibited little cytotoxicity at concentrations of up to 100 microM. DBM 2198, one of

SUBMITTER: Lee DS 

PROVIDER: S-EPMC1251495 | biostudies-literature | 2005 Oct

REPOSITORIES: biostudies-literature