TABLE 1.
Compound |
Kd without competitorsa |
Kd with HIV-1Δbulgeb |
Kd with HIV-1wtbulgec |
Degree of nonspecificity |
Degree of direct competition |
Relative specificity for bulge |
Hill coefficientd |
---|---|---|---|---|---|---|---|
Cinchonidine | 193.2 ± 21.3 | n.d. | n.d. | n.d. | n.d. | n.d. | 1.5 ± 0.15 |
Butamben | 39.4 ± 7.0 | n.d. | n.d. | n.d. | n.d. | n.d. | 1.7 ± 0.2 |
Idarubicin | 9.1 ± 1.3 | 17.6 ± 2.4 | 81.7 ± 3.4 | 17.6 ± 3.5% | 81.6 ± 12.1% | 4.7 ± 1.2 | 1.0 ± 0.15 |
Doxorubicin | 2.8 ± 0.4 | 8.4 ± 0.9 | 37.8 ± 6.1 | 27.3 ± 4.9% | 77.2 ± 16.7% | 2.8 ± 0.8 | 1.5 ± 0.15 |
Compounds were titrated into 2 μM HIV-1screen in 3 replicate experiments. Mean apparent Kd and SEM are indicated.
n.d. = not determined. 20 μM HIV-1Δbulge was included in the titrations. This is a 10-fold molar excess of RNA relative to the HIV-1screen RNA containing the 2-aminopurine reporter.
20 μM HIV-1wtbulge was included in the titrations. This is a 10-fold molar excess of RNA relative to the HIV-1screen RNA containing the 2-aminopurine reporter.
Hill coefficient errors are shown as standard errors resulting from the least-squares fit.