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1994-07-02
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Document 0001
DOCN M9470001
TI Competitive inhibition of HIV-1 protease by warfarin derivatives.
DT 9409
AU Tummino PJ; Ferguson D; Hupe D; Department of Biochemistry, Parke-Davis
Pharmaceutical Research,; Division of Warner-Lambert Company, Ann Arbor,
Michigan 48105.
SO Biochem Biophys Res Commun. 1994 May 30;201(1):290-4. Unique Identifier
: AIDSLINE MED/94256992
AB The oral anticoagulant warfarin (4-hydroxy-3-(3-oxo-1-phenylbutyl)-
benzopyran-2-one) is a structurally novel low micromolar competitive
inhibitor of HIV-1 protease in vitro. It was recently reported that
warfarin inhibits HIV-1 infection in U-1 monocytes and viral production
in ACH-2 lymphocytes (Bourinbaiar, A.S. et al., (1993) AIDS 7, 129-130).
Our results demonstrate that warfarin and a series of structurally
related analogs inhibit the viral protease, the most potent analog
having an IC50 = 1.9 microM. Kinetic analysis reveals inhibition by
warfarin occurs in a competitive manner, with Ki = 3.3 microM. While it
is unclear whether the cellular inhibition previously reported is due to
inhibition of HIV-1 protease, the warfarin analogs are a novel class of
nonpeptide HIV-1 protease inhibitors.
DE *HIV Protease Inhibitors Warfarin/*ANALOGS & DERIVATIVES/PHARMACOLOGY
JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).