Document 0784
 DOCN  M9650784
 TI    In vitro anti-HIV-1 activity of HIV protease inhibitor KNI-272 in
       resting and activated cells: implications for its combined use with AZT
       or ddI.
 DT    9605
 AU    Chokekijchai S; Shirasaka T; Weinstein JN; Mitsuya H; Experimental
       Retrovirology Section, National Cancer Institute,; Bethesda, MD 20892,
       USA.
 SO    Antiviral Res. 1995 Sep;28(1):25-38. Unique Identifier : AIDSLINE
       MED/96105495
 AB    KNI-272, a conformationally constrained human immunodeficiency virus
       (HIV) protease inhibitor containing a P1 allophenylnorstatine (Apns)
       ((2S,3S)- 3-amino-2-hydroxy-4-phenylbutyric acid), has been shown to be
       a selective and potent inhibitor of the replication of a wide spectrum
       of HIV strains in vitro. When KNI-272 was tested in combination with
       3'-azido-2',3'-dideoxythymidine (AZT) or 2',3'-dideoxyinosine (ddI)
       against a primary HIV-1 isolate in phytohemagglutin-activated peripheral
       blood mononuclear cells (PHA-PBM), its activity was identified to be
       additive, but not synergistic or antagonistic, as analyzed with the
       COMBO program package. When tested alone for anti-HIV-1 activity in
       resting PBM (R-PBM) and PHA-PBM, KNI-272 was found to be comparably
       potent against the virus in both target cell populations, whereas AZT
       was more potent in PHA-PBM than in R-PBM and ddI was more potent in
       R-PBM. These data suggest a potential clinical application of KNI-272
       and its analogs.
 DE    Antiviral Agents/*PHARMACOLOGY  Cells, Cultured
       Didanosine/*PHARMACOLOGY  Drug Interactions  Human  HIV Protease
       Inhibitors/*PHARMACOLOGY  HIV-1/*DRUG EFFECTS/ENZYMOLOGY  Leukocytes,
       Mononuclear/CYTOLOGY  Molecular Structure  Oligopeptides/*PHARMACOLOGY
       Phytohemagglutinins/PHARMACOLOGY  Zidovudine/*PHARMACOLOGY  JOURNAL
       ARTICLE

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