Inhibition of HIV-1 integration protein by aurintricarboxylic acid monomers, monomer analogs, and polymer fractions.
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.
Cushman
M
M
Department of Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, IN 47906.
Sherman
P
P
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy* / Q000473:pathology; D001312:Aurintricarboxylic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D002478:Cells, Cultured; D004254:DNA Nucleotidyltransferases / Q000187:drug effects*; D006678:HIV / Q000187:drug effects* / Q000472:pathogenicity; D015497:HIV-1 / Q000187:drug effects / Q000472:pathogenicity; D015498:HIV-2 / Q000187:drug effects / Q000472:pathogenicity; D006801:Humans; D019426:Integrases; D011108:Polymers / Q000494:pharmacology; D012191:Retroviridae Proteins / Q000187:drug effects*; D016662:Virus Integration / Q000187:drug effects
D011108:Polymers; D012191:Retroviridae Proteins; D001312:Aurintricarboxylic Acid; D004254:DNA Nucleotidyltransferases; D019426:Integrases