Table 3.
Effect of mutations of inhibitor-interacting RNH residues in RT on inhibition of RT RNH activity by acylhydrazones.
| INHIBITOR | IC50 for inhibition of RT-RNH activity (μM)
|
||||
|---|---|---|---|---|---|
| WT | A502G (A76)a |
A502F (A76) |
I505Vb (I79) |
A502G+D256G | |
|
| |||||
| DHBNH | 0.9 ± 0.3 | 13.7 ± 5.2 | > 10 | 0.9 ± 0.1 | > 50 |
| BHMP03 | 0.9 ± 0.2 | 4.2 ± 1.1 | > 10 | 1.0 ± 0.2 | 6.5 ± 2.1 |
| BHMP07 | 0.2 ± 0.1 | 1.0 ± 0.7 | > 10 | 0.3 ± 0.3 | 4.0 ± 1.3 |
a
The residue numbers in the parentheses indicate those in the RNH fragment sequence
b
Mutations other than I505V eliminated RT RNH activity and thus could not be studied.