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- W2081497478 abstract "In our extensive screening of anti-HIV-1 agents in chronically infected cell lines, we have found acridone derivatives to be selective inhibitors of HIV-1 replication. Among the acridone derivatives, 1-hydroxy-10-methyl-9,10-dihydroacrid-9-one (RD6-5071) suppressed tumor necrosis factor (TNF)-α-induced HIV-1 expression in the latently infected cell line OM-10.1, U1, and ACH-2. Its 50% effective concentration for HIV-1 p24 antigen production was 2.0 μg/ml in OM-10.1 cells, while its 50% cytotoxic concentration was 18 μg/ml. The compound also inhibited phorbol 12-myristate 13-acetate (PMA)-induced HIV-1 expression in these cell lines. Furthermore, RD6-5071 was inhibitory to HIV-1 replication in acutely infected U937 and peripheral blood mononuclear cells. The compound was found to suppress TNF-α-induced HIV-1 long terminal repeat-driven gene expression. An inhibition assay for protein kinase C (PKC) revealed that RD6-5071 could reduce the enzyme activity. Furthermore, the compound was a moderate inhibitor of PMA-induced nuclear factor κB (NF-κB) activation, as determined by a gel mobility shift analysis. These results suggest that the acridone derivatives suppress HIV-1 replication at the transcriptional level primarily through a mechanism of PKC inhibition." @default.
- W2081497478 created "2016-06-24" @default.
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- W2081497478 date "1999-10-01" @default.
- W2081497478 modified "2023-09-27" @default.
- W2081497478 title "Acridone derivatives are selective inhibitors of HIV-1 replication in chronically infected cells" @default.
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- W2081497478 doi "https://doi.org/10.1016/s0166-3542(99)00045-5" @default.
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