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Inhibition of DHFRs Modified at Position 115 by TMP and MTX
| DHFR | relative activity (%) |
trimethoprim (IC50) (nM) |
methotrexate (IC50) (nM) |
|---|---|---|---|
| wild type DHFR | 100 | 2.1 ± 0.2a | 1.0 ± 0.1 |
| A | 91 ± 3 | 26 ± 2.2 | 1.1 ± 0.1 |
| B | 25 ± 2 | 8.5 ± 0.7 | 1.4 ± 0.2 |
| C | 82 ± 3 | 10.6 ± 0.9 | 1.3 ± 0.2 |
| D | 12 ± 2 | 35.2 ± 2.9 | 1.2 ± 0.1 |
Standard deviation based on data from three experiments.
