TABLE 7.
Inhibition of bacterial IMPDHs and their ΔCBS variants by CpIMPDH-specific inhibitors
Assay conditions are described under “Experimental Procedures.”
| Enzyme | IC50 |
||||||
|---|---|---|---|---|---|---|---|
| 1 | 2 | 3 | 4 | 5 | 6 | 7 | |
| nm | |||||||
| BaIMPDHa | 63 ± 12 | 67 ± 14 | 670 ± 80 | 19 ± 5 | 47 ± 5 | 20 ± 11 | 23 ± 4 |
| BaIMPDHΔS | 137 ± 8 | 100 ± 4 | 800 ± 40 | 65 ± 11 | 40 ± 3 | 28 ± 4 | 38 ± 4 |
| BaIMPDHΔL | 43 ± 3 | 72 ± 13 | 700 ± 100 | NDb | 10 ± 1 | 6 ± 1 | 27 ± 6 |
| CjIMPDH | 140 ± 30 | 51 ± 9 | 169 ± 20 | 36 ± 8 | 22 ± 3 | 29 ± 4 | 13 ± 2 |
| CjIMPDHΔS | 107 ± 8 | 42 ± 2 | 200 ± 20 | 67 ± 13 | 39 ± 3 | 46 ± 4 | 19 ± 2 |
| ClpIMPDH | 74 ± 33 | 570 ± 20 | 1700 ± 230 | 15 ± 1 | 34 ± 6 | 24 ± 10 | 54 ± 4 |
| ClpIMPDHΔL | 364 ± 20 | 450 ± 50 | 3400 ± 190 | 44 ± 8 | 92 ± 7 | 66 ± 3 | 95 ± 6 |
| VcIMPDH | >5000 | >5000 | >5000 | >5000 | >5000 | >5000 | >5000 |
| VcIMPDHΔL | >5000 | >5000 | >5000 | >5000 | >5000 | >5000 | >5000 |
| CpIMPDHc | 9 ± 2 | 10 ± 1 | 24 ± 6 | 11 ± 5 | 5 ± 2 | 8 ± 2 | 6 ± 1 |