Table 1. Second-Order Rate Constants (k2/Ks) for Acylation of the Active Site of PBP2a by Nitrocefin and by Ceftaroline and Dissociation Constants for Binding of Ceftaroline to the Allosteric Site of PBP2a.
| nitrocefin | ceftaroline |
||
|---|---|---|---|
| enzymes | k2/Ks (M–1 s–1) | k2/Ks (M–1 s–1) | Kd (μM) |
| wild-type | 220 ± 25 | 4500 ± 640 | 20 ± 4 |
| N146K | 270 ± 70 | 9150 ± 1560 | 20 ± 4 |
| E150K | 65 ± 5 | 820 ± 470 | 44 ± 6 |
| N146K/E150K | 330 ± 60 | 850 ± 140 | 30 ± 7 |
| N146K/E150K/H351N | 230 ± 30 | 1400 ± 140 | 26 ± 6 |