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Table 3 Inhibition Constants of BLIPY50 mutants for Class A β-lactamases

From: Systematic substitutions at BLIP position 50 result in changes in binding specificity 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
  1. BLIP Y50I could not be purified