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KPC-2 W105 Variant Inhibitor Kineticsa
| Clavulanic acid | Sulbactam | Tazobactam | |
|---|---|---|---|
| Ki (μM) | |||
| WT | 11 ± 1 | 167 ± 16 | 74 ± 7 |
| Trp105Phe | 61 ± 6 | 177 ± 17 | 113 ± 10 |
| Trp105Asn | 234 ± 20 | 86 ± 8 | 85 ± 8 |
| Trp105Val | 107 ± 10 | 63 ± 6 | 160 ± 16 |
| Partition ratio (15 min) | |||
| WT | 2000 | 1500 | 250 |
| Trp105Phe | 4000 | 2000 | 250 |
| Trp105Asn | 5000 | 1500 | 125 |
| Trp105Val | 7500 | 125 | 125 |
Nitrocefin is the substrate used for inhibitor kinetics.
