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M94A2240.TXT
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1994-10-25
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Document 2240
DOCN M94A2240
TI beta-L-2',3'-dideoxy-5-fluorocytidine (L-FDDC) a novel potent and
selective inhibitor of HIV and HBV replication in vitro.
DT 9412
AU Sommadossi JP; Faraj A; Schinazi R; Gosselin G; Imbach JL; Univ. of AL
at Birmingham 35294.
SO Int Conf AIDS. 1994 Aug 7-12;10(1):35 (abstract no. 112A). Unique
Identifier : AIDSLINE ICA10/94370335
AB beta-L-2',3'-dideoxy-5-fluorocytidine (L-FDDC) potently inhibited HIV-1,
and HIV-2 replication in vitro in various cell lines. L-FDDC exhibited
an EC90 of 0.15 microM in peripheral blood mononuclear cells infected by
HIV-1. L-FDDC showed the highest selectivity index (9000) as compared to
L-DDC (37), FDDC (35), and AZT (100) when the index was determined
relative to human bone marrow progenitor cells. Using a
poly(rI)n.oligo(dC)10-15 as a template primer, the 5'-triphosphate of
L-FDDC (L-FDDCTP) competitively inhibited HIV-1 RT with a Ki of 1.00
microM, with respect to dCTP. L-FDDCTP did not inhibit human DNA
polymerases alpha, beta, and gamma up to 50 microM. L-FDDC was also a
potent and selective inhibitor of HBV replication with an EC90 of 0.30
microM when HBV virion levels were measured in transfected 2.2.15 cells.
The EC90 values for L-DDC and L-FTC were 1.1 and 0.15 microM
respectively. L-FDCCTP inhibited woodchuck HBV DNA polymerase with an
IC50 approximating 1.75 microM. These data suggest that further
development of L-FDDC for treatment of HIV and HBV infections merits
consideration.
DE Antiviral Agents/*PHARMACOLOGY Binding, Competitive/DRUG EFFECTS Cell
Line Comparative Study Hepatitis B Virus/*DRUG EFFECTS/PHYSIOLOGY
Hepatitis Virus, Woodchuck/DRUG EFFECTS Human HIV-1/*DRUG
EFFECTS/PHYSIOLOGY HIV-2/*DRUG EFFECTS/PHYSIOLOGY Reverse
Transcriptase/METABOLISM Transfection Virus Replication/*DRUG EFFECTS
Zalcitabine/*ANALOGS & DERIVATIVES/*PHARMACOLOGY
Zidovudine/PHARMACOLOGY MEETING ABSTRACT
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).