title: HIV-1 protease inhibitors containing statine: inhibitory potency and antiviral activity.
abstract: Several series of chemically different inhibitors of the HIV-1 aspartyl protease have been described. Nevertheless despite the high in vitro potency showed, in most cases these inhibitors are unable to inhibit viral replication in infected cells. Penetration of the inhibitors across the cell membrane might account for their low antiviral activity. The relationship between inhibitory potency, antiviral activity and chemical structures of a series of oligopeptides containing statine or statine derivatives are presented here.
authors.affiliation: Sanofi Recherche, Montpellier, France.
authors.forename: J A
authors.initials: JA
authors.lastname: Fehrentz
authors.forename: B
authors.initials: B
authors.lastname: Chomier
authors.forename: E
authors.initials: E
authors.lastname: Bignon
authors.forename: S
authors.initials: S
authors.lastname: Venaud
authors.forename: J C
authors.initials: JC
authors.lastname: Chermann
authors.forename: D
authors.initials: D
authors.lastname: Nisato
mesh_terms: D000595:Amino Acid Sequence; D000596:Amino Acids / Q000378:metabolism; D002460:Cell Line; D016333:HIV Protease / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D006801:Humans; D007700:Kinetics; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D000596:Amino Acids; D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D016333:HIV Protease; C013165:statine