Document 0788
 DOCN  M9650788
 TI    Comparative analysis of anti-human immunodeficiency virus type 1
       activities of dideoxynucleoside analogs in resting and activated
       peripheral blood mononuclear cells.
 DT    9605
 AU    Shirasaka T; Chokekijchai S; Yamada A; Gosselin G; Imbach JL; Mitsuya H;
       Experimental Retrovirology Section, National Cancer Institute,; National
       Institutes of Health, Bethesda, Maryland 20892, USA.
 SO    Antimicrob Agents Chemother. 1995 Nov;39(11):2555-9. Unique Identifier :
       AIDSLINE MED/96139557
 AB    We determined the anti-human immunodeficiency virus type 1 (anti-HIV-1)
       activities of various dideoxy-nucleoside analogs by using
       phytohemagglutinin-activated peripheral blood mononuclear cells
       (PHA-PBMs) and resting PBMs (R-PBMs) as target cells. The comparative
       order of anti-HIV-1 activity in PHA-PBMs was azidothymidine (AZT) >
       dideoxycytidine (ddC) > dideoxythymidinene (d4T) > dideoxyinosine (ddI)
       and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) >
       2'-beta-fluoro-dideoxyadenosine (F-ara-ddA), while that in R-PBMs was
       ddC > ddI, PMEA, and F-ara-ddA, >> AZT and d4T. A pronucleotide,
       bis-(S-acetylthioethanol)phosphotriester-ddAMP, which bypasses the
       anabolic monophosphorylation step for the intracellular delivery of
       ddAMP, was highly active both in PHA-PBMs and R-PBMs. These data may
       have basic and clinical relevance in the design of anti-HIV
       chemotherapy, particularly combination chemotherapy with
       dideoxynucleosides, and in the development of active pronucleotides.
 DE    Antiviral Agents/*PHARMACOLOGY  Cells, Cultured  Comparative Study
       Dideoxynucleosides/*PHARMACOLOGY  Human  HIV Core Protein
       p24/BIOSYNTHESIS  HIV-1/*DRUG EFFECTS  Microbial Sensitivity Tests
       Monocytes/DRUG EFFECTS/PHYSIOLOGY/*VIROLOGY
       Phytohemagglutinins/PHARMACOLOGY  JOURNAL ARTICLE

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