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. 2017 May 24;61(6):e02193-16. doi: 10.1128/AAC.02193-16

TABLE 1.

Inhibition parameters of PER-2 and derived Arg220 and Thr237 mutants

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
a

Relative to wild-type PER-2.

b

ND, not determined.