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M94A0644.TXT
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1994-10-21
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Document 0644
DOCN M94A0644
TI In vitro activity of protease inhibitors against HIV.
DT 9412
AU Birch C; Tachedjian G; Tyssen D; Grobelny D; Virology Department, NCHVR,
Fairfield, Victoria.
SO Annu Conf Australas Soc HIV Med. 1993 Oct 28-30;5:62 (abstract no. TB2).
Unique Identifier : AIDSLINE ASHM5/94349011
AB HIV encodes a novel aspartyl protease that represents an important
virus-specific target for inhibitors. We have been studying a series of
transition state analogue inhibitors designed and synthesised in
Australia that have potent and specific activity against HIV replication
in cell culture. (Note: the structure of these compounds will not be
presented). The inhibitors are active against HIV-1 and HIV-2 in acutely
and chronically infected cells, working through a mechanism involving
inhibition of cleavage of p55 to its structural components. As a result,
virions produced in the presence of these drugs are noninfectious. The
inhibitors are also active against AZT-resistant HIV and the simian
immunodeficiency virus, but fail to inhibit feline immunodeficiency
virus. These results will be presented, along with preliminary details
on the pharmacokinetics of selected inhibitors.
DE Antiviral Agents/*PHARMACOLOGY Cells, Cultured Gene Products,
gag/ANTAGONISTS & INHIB Human HIV Protease Inhibitors/*PHARMACOLOGY
HIV-1/*DRUG EFFECTS HIV-2/*DRUG EFFECTS Protein Precursors/ANTAGONISTS
& INHIB Virus Replication/*DRUG EFFECTS MEETING ABSTRACT
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).