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M94A2858.TXT
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1994-10-25
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Document 2858
DOCN M94A2858
TI Non-nucleoside RT inhibitors with structural diversity but potent
anti-HIV activity.
DT 9412
AU Yang SS; Buckheit RW Jr; Bader JP; DTP, NCI, Bethesda, MD 20892.
SO Int Conf AIDS. 1994 Aug 7-12;10(1):209 (abstract no. PB0264). Unique
Identifier : AIDSLINE ICA10/94369717
AB Current thrust in controlling AIDS targets the infection and replication
of the human immunodeficiency virus (HIV). To date treatment of AIDS has
relied upon nucleoside reverse transcriptase (RT) inhibitors such as
AZT, ddI, ddC, and ddA, which eventually become ineffective due to the
emergence of HIV mutants bearing resistance to the specific nucleoside
inhibitor, or because of intolerable toxicities. The National Cancer
Institute conducts and coordinates a highly organized and systematic in
vitro screening program on synthetic and natural compounds submitted by
various individuals or institutions world-wide. Over 3000 active
compounds were examined in a panel of laboratory and clinical strains of
HIV, including certain drug-resistant strains, in cell lines or fresh
human lymphocyte, macrophage/monocyte cell preparations. We were able to
identify 8 categories and 17 other unique compounds that fit within the
non-nucleoside RT inhibitor (NNRTI) group, based on their inhibition
patterns against various HIV strains. These compounds also inhibited
enzymatic RT when evaluated using heteropolymeric templates. When tested
in combination with AZT, many of the NNRTI's exhibit synergistic
inhibition of HIV-1, suggesting that combination antiviral therapy with
AZT may be therapeutically promising for AIDS treatment. Several
resistant HIV-1 strains were selected from cultures treated with one or
another of the NNRTI's. The pattern of cross resistance among the
compounds demonstrates that they are not identical with respect to
interaction with the viral RT.
DE Antiviral Agents/*PHARMACOLOGY Cell Line Cells, Cultured Drug
Resistance Drug Screening Drug Synergism Enzyme
Inhibitors/CLASSIFICATION/PHARMACOLOGY Human HIV-1/*DRUG EFFECTS
Lymphocytes/MICROBIOLOGY National Institutes of Health (U.S.)
Phagocytes/MICROBIOLOGY Reverse Transcriptase/*ANTAGONISTS & INHIB
United States Zidovudine/PHARMACOLOGY MEETING ABSTRACT
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).