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. 2014 Jan 17;289(9):6152–6164. doi: 10.1074/jbc.M113.533562

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
OXA-1
OXA-24
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