title: Three inhibitors of type 1 human immunodeficiency virus long terminal repeat-directed gene expression and virus replication.
abstract: Transcription of type 1 human immunodeficiency virus (HIV-1) provirus is governed by the viral long terminal repeat (LTR). Drugs can block HIV-1 replication by inhibiting activity of its LTR. We report that topotecan, beta-lapachone, and curcumin are potent and selective inhibitors of HIV-1 LTR-directed gene expression, at concentrations that have minor effects on cells. At these concentrations, each drug inhibited p24 antigen production in cells either acutely or chronically infected with HIV-1. Their target is transcriptional function of the LTR.
authors.affiliation: Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115.
authors.forename: C J
authors.initials: CJ
authors.lastname: Li
authors.forename: L J
authors.initials: LJ
authors.lastname: Zhang
authors.forename: B J
authors.initials: BJ
authors.lastname: Dezube
authors.forename: C S
authors.initials: CS
authors.lastname: Crumpacker
authors.forename: A B
authors.initials: AB
authors.lastname: Pardee
mesh_terms: D000208:Acute Disease; D000998:Antiviral Agents; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000494:pharmacology; D002478:Cells, Cultured; D002908:Chronic Disease; D003474:Curcumin / Q000494:pharmacology*; D015967:Gene Expression Regulation, Viral / Q000187:drug effects*; D015658:HIV Infections / Q000188:drug therapy; D016325:HIV Long Terminal Repeat / Q000235:genetics*; D015497:HIV-1 / Q000235:genetics*; D066298:In Vitro Techniques; D009285:Naphthoquinones / Q000494:pharmacology*; D012367:RNA, Viral / Q000096:biosynthesis; D019772:Topotecan; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D009285:Naphthoquinones; D012367:RNA, Viral; C014638:beta-lapachone; D019772:Topotecan; D003474:Curcumin; D002166:Camptothecin