Table 3 Inhibition Constants of BLIPY50 mutants for Class A β-lactamases
BLIP Mutant | Ki (nM) KPC-2 | Ki (nM) TEM-1 | Ki (nM) Bla1 | |
|---|---|---|---|---|
Nonpolar | WT | 1.5 ± 0.2 | 0.5 ± 0.1 | 2.5 ± 0.3 |
Y50A | 1.9 ± 0.3 | 0.010 ± 0.001 | 1.2 ± 0.3 | |
Y50F | 15 ± 2 | 10.3 ± 0.8 | 90 ± 14 | |
Y50L | 0.7 ± 0.2 | 0.17 ± 0.02 | 160 ± 39 | |
Y50M | 0.5 ± 0.1 | 0.11 ± 0.01 | 34 ± 9 | |
Y50V | 10 ± 1 | 3.5 ± 0.6 | 200 ± 11 | |
Y50W | 1.1 ± 0.2 | 11 ± 1 | 90 ± 11 | |
Polar | Y50C | 42 ± 6 | 60 ± 10 | 360 ± 5 |
Y50N | 3.8 ± 0.8 | 7.8 ± 0.5 | 180 ± 43 | |
Y50Q | 1.0 ± 0.5 | 0.24 ± 0.02 | 1.3 ± 0.3 | |
Y50S | 5 ± 1 | 1.1 ± 0.1 | 3110 ± 5 | |
Y50T | 3.5 ± 0.4 | 2.5 ± 0.2 | 290 ± 53 | |
Small | Y50G | 0.72 ± 0.02 | 0.40 ± 0.06 | 0.58 ± 0.07 |
Y50P | 5 ± 1 | 40 ± 3 | 220 ± 28 | |
Charged | Y50H | 1.4 ± 0.1 | 5.0 ± 0.1 | 230 ± 2 |
Y50R | 11 ± 1 | 69 ± 2 | >1500 | |
Y50K | 260 ± 10 | 195.3 ± 0.2 | 180 ± 47 | |
Y50D | 3.2 ± 0.3 | 160 ± 23 | >4500 | |
Y50E | 5.5 ± 0.1 | 76 ± 6 | 331 ± 6 |