TABLE 1.
PER-2 | Clavulanic acid |
Tazobactam |
||||||
---|---|---|---|---|---|---|---|---|
kinact (s−1) | Ki (μM) | kinact/Ki (μM−1 s−1) | Relative kinact/Ki (%)a | kinact (s−1) | Ki (μM) | kinact/Ki (μM−1 s−1) | Relative kinact/Ki (%)a | |
Wild type | 0.031 ± 0.001 | 0.064 ± 0.007 | 0.48 ± 0.07 | 100 | 0.047 ± 0.002 | 0.18 ± 0.02 | 0.26 ± 0.04 | 100 |
Mutant | ||||||||
Arg220Leu | 0.045 ± 0.001 | 4.1 ± 0.2 | 0.0109 ± 0.0008 | 2.3 | 0.016 ± 0.001 | 10 ± 1 | 0.0016 ± 0.0004 | 0.6 |
Arg220Ser | 0.055 ± 0.002 | 1.8 ± 0.1 | 0.031 ± 0.003 | 6.5 | 0.0172 ± 0.0005 | 2.8 ± 0.2 | 0.0062 ± 0.0007 | 2.4 |
Arg220Gly | 0.11 ± 0.01 | 80 ± 10 | 0.0014 ± 0.0003 | 0.3 | 0.0157 ± 0.0006 | 31 ± 3 | 0.00050 ± 0.00007 | 0.2 |
Arg220His | 0.032 ± 0.002 | 3.3 ± 0.5 | 0.010 ± 0.002 | 2.0 | 0.0150 ± 0.0005 | 5.1 ± 0.6 | 0.0029 ± 0.0004 | 1.1 |
Arg220Thr | NDb | ND | 0.0068 ± 0.0002 | 1.4 | 0.022 ± 0.001 | 11 ± 1 | 0.0019 ± 0.0004 | 0.7 |
Arg220Cys | 0.31 ± 0.04 | 19 ± 3 | 0.016 ± 0.005 | 3.3 | 0.0187 ± 0.0004 | 6.0 ± 0.4 | 0.0031 ± 0.0002 | 1.2 |
Thr237Ala | 0.027 ± 0.001 | 0.070 ± 0.009 | 0.38 ± 0.07 | 79.8 | 0.022 ± 0.002 | 0.27 ± 0.06 | 0.08 ± 0.02 | 30.6 |
Relative to wild-type PER-2.
ND, not determined.