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. 1998 Sep;42(9):2245–2253. doi: 10.1128/aac.42.9.2245

TABLE 1.

IC50s for inhibition of DNA-modifying enzymes by polyhydroxylated aromatic inhibitors of integrasea

Enzyme IC50 (μM)
QLZ ATC TMS QTN LCH ELA ARS
HIV-1 integrase 4 0.5 12 1 0.13 5 3
MoMLV RT (Mn) 0.11 ± 0.06 0.45 ± 0.3 >50 0.23 ± 0.15 0.58 ± 0.24 0.68 ± 0.45 0.14 ± 0.09
MoMLV RT (Mg) 2.9 ± 0.8 3.8 ± 1 >50 1.2 ± 0.9 8.3 ± 6.3 1.7 ± 1.9 0.75 ± 0.08
PvuII 15 ± 9 >50 >50 7 ± 6 >50 48 ± 22 22 ± 2
EcoRI 6 ± 4 >50 13 ± 2 2 ± 0.1 >50 2 ± 1 16 ± 1
MCV topoisomerase >50 >50 >50 >50 >50 >50 >50
EcoRI methylase >50 >50 >50 >50 >50 >50 >50
CpG methylase >50 >50 >50 >50 >50 >50 >50
a

IC50s for inhibition of integrase (terminal cleavage) are from this work unless indicated otherwise. Those for QLZ (28), ATC (23), QTN (34), and LCH (64) have been presented elsewhere. The IC50 for integrase inhibition was determined in the presence of Mn2+