TABLE 4.
Percent inhibition by DCQAs of HIV-1 RNase H-catalyzed RNA-DNA hybrid cleavage
Compound | No preincubationa
|
Preincubationb | ||
---|---|---|---|---|
Expt 1 | Expt 2 | Avg | ||
Quinic acid | 7 | 18 | 13 | 17 |
Caffeic acid | 6 | 2 | 4 | 1 |
Chlorogenic acid | −9 | 9 | 0 | 4 |
1-MO-3,5-DCQA | 37 | 18 | 28 | 41 |
1,5-DCQA | −7 | −15 | −11 | 5 |
4,5-DCQA | −27 | −19 | −23 | 12 |
3,5-DCQA | −29 | −24 | −26 | −11 |
3,4-DCQA (synthetic) | −26 | −22 | −24 | −10 |
l-CCA | 14 | −5 | 5 | 22 |
Compounds were tested with the Amersham HIV-1 IN SPA kit according to the manufacturer’s instructions. Values are percent inhibitions of reactions after 15 min. Compounds were added to the reaction mix at the same time as the full-length RT proteins. The final concentration of each compound was 50 μg/ml. Values for each experiment are means of three separate reactions.
Compounds were preincubated with HIV-1 RT for 1 h at room temperature prior to testing in the Amersham HIV-1 RNase H SPA kit. Values are percent inhibitions of reactions after 15 min. The final concentration of each compound was 50 μg/ml. Results are means of triplicate samples in one experiment.