title: Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.
abstract: A series of triterpene compounds characterized by a stringent structure-activity relationship were identified as potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replication. Currently studied botulinic derivatives have 50% inhibitory concentrations (IC50) against HIV-1 strain IIIB/LAI in the 10 nM range in several cellular infection assays but are inactive against HIV-2. These compounds did not significantly inhibit the in vitro activities of several purified HIV-1 enzymes. Rather, they appeared to block virus infection at a postbinding, envelope-dependent step involved in the fusion of the virus to the cell membrane.
authors.affiliation: Rhône Poulenc Rorer S.A., Centre de Recherche de Vitry-Alfortville, Vitry Sur Seine, France.
authors.forename: J F
authors.initials: JF
authors.lastname: Mayaux
authors.forename: A
authors.initials: A
authors.lastname: Bousseau
authors.forename: R
authors.initials: R
authors.lastname: Pauwels
authors.forename: T
authors.initials: T
authors.lastname: Huet
authors.forename: Y
authors.initials: Y
authors.lastname: Hénin
authors.forename: N
authors.initials: N
authors.lastname: Dereu
authors.forename: M
authors.initials: M
authors.lastname: Evers
authors.forename: F
authors.initials: F
authors.lastname: Soler
authors.forename: C
authors.initials: C
authors.lastname: Poujade
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000998:Antiviral Agents; D015704:CD4 Antigens / Q000378:metabolism; D002460:Cell Line; D015658:HIV Infections / Q000517:prevention & control*; D015497:HIV-1 / Q000472:pathogenicity*; D008561:Membrane Fusion; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D000998:Antiviral Agents; D015704:CD4 Antigens; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid