TABLE 1.
Impact of KPC-2 W105 mutations on reaction with vaborbactam
Enzyme mutation | k2/K (M−1 s−1) | koff (s−1) | Residence time (min) | Kd (nM) |
---|---|---|---|---|
WT | 5.8 × 103 ± 0.3 × 103 | 4.3 × 10−5 ± 0.6 × 10−5 | 394 ± 50 | 7.4 ± 0.9 |
W105F | 4.1 × 103 ± 0.1 × 103 | 3.9 × 10−5 ± 0.5 × 10−5 | 437 ± 59 | 9.3 ± 1.1 |
W105N | 2.9 × 103 ± 0.1 × 103 | 5.0 × 10−5 ± 0.6 × 10−5 | 337 ± 46 | 17 ± 2 |
W105L | 0.63 × 103 ± 0.01 × 103 | 2.3 × 10−5 ± 0.3 × 10−5 | 721 ± 101 | 37 ± 4 |
W105V | 0.94 × 103 ± 0.1 × 103 | 3.5 × 10−5 ± 0.3 × 10−5 | 473 ± 41 | 38 ± 3 |
W105D | 0.32 × 103 ± 0.07 × 103 | 3.5 × 10−5 ± 0.3 × 10−5 | 477 ± 48 | 110 ± 12 |
W105A | 0.85 × 103 ± 0.07 × 103 | 7.7 × 10−5 ± 0.8 × 10−5 | 219 ± 23 | 90 ± 10 |
W105Y | 3.8 × 103 ± 0.3 × 103 | 3.6 × 10−5 ± 0.2 × 10−5 | 463 ± 20 | 9.6 ± 0.8 |
W105S | 0.92 × 103 ± 0.08 × 103 | 4.4 × 10−5 ± 0.6 × 10−5 | 386 ± 53 | 47 ± 6 |