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1996-03-30
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Document 1053
DOCN M9651053
TI Comparative analysis of anti-human immunodeficiency virus type 1
activities of dideoxynucleoside analogs in resting and activated
peripheral blood mononuclear cells.
DT 9505
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
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).