INHIBITION OF HIV-1 INTEGRATION PROTEIN BY AURINTRICARBOXYLIC ACID MONOMERS, MONOMER ANALOGS, AND POLYMER FRACTIONS

被引:82
作者
CUSHMAN, M [1 ]
SHERMAN, P [1 ]
机构
[1] BURROUGHS WELLCOME CO, DIV EXPTL THERAPY, RES TRIANGLE PK, NC 27709 USA
关键词
D O I
10.1016/S0006-291X(05)80958-1
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several aurintricarboxylic acid (ATA) monomers, monomer analogs, and polymer fractions have been tested as inhibitors of HIV-1 integration protein (IN). Both of the ATA monomers and all of the ATA polymer fractions inhibited a selective DNA cleavage reaction catalyzed by IN. The ATA monomer analogs were inactive or had low activity. The activities of the substances as inhibitors of HIV IN correlated in a positive way with their activities as inhibitors of the cytopathic effect of HIV-1 in CEM and HIV-2 in MT4 cells. These results suggest that inhibition of HIV IN may contribute to the antiviral activity of the ATA monomers and monomer analogs in cell culture. © 1992 Academic Press, Inc.
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页码:85 / 90
页数:6
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