TABLE 3.
Kinetic parameters of inhibition
Ki for the penems was determined by measuring initial steady-state velocities in the presence of a constant concentration of enzyme with increasing concentrations of inhibitors against nitrocefin (100 μm); the value was then corrected for nitrocefin affinity. IC50 was determined by measurements of inhibitor concentration that reduces the initial velocities by 50% after 5-min preincubation of enzyme with inhibitor. tn was determined as the ratio of inhibitor concentration to enzyme concentration necessary to decrease enzyme activity by 95% after 24 h.
Inhibitors | Enzymes |
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---|---|---|---|---|---|---|
OXA-1 |
OXA-24 |
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Ki | IC50 | tn | Ki | IC50 | tn | |
nm | nm | nm | nm | |||
Penem 1 | 50 ± 8 | 30 ± 8 | 2 | 30 ± 2 | 150 ± 30 | 900 |
Penem 3 | 380 ± 70 | 60 ± 5 | 2 | 150 ± 20 | 160 ± 40 | 925 |