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Table 4 The inhibition rates (%) of 33 β-lactam drugs on BlaR-CTD proteins of single point mutation and disulfide bond insertion (AVG ± SD, n = 5)

From: Analysis of the stability and affinity of BlaR-CTD protein to β-lactam antibiotics based on docking and mutagenesis studies

Drug BlaR-CTD A138E Q147K I188K S190Y V197D S19C-G24C R50C-Q147C E183C-I188C
Penicillin G 26.2 ± 2.1 15.3 ± 1.4 26.7 ± 3.4 25.3 ± 2.8 21.7 ± 1.6 34.2 ± 4.2 17.4 ± 1.5 34.6 ± 2.5 20.5 ± 1.4
Ampicillin 21.2 ± 1.1 21.0 ± 1.8 27.4 ± 2.5 17.4 ± 1.4 24.4 ± 2.4 19.3 ± 1.3 18.4 ± 1.3 17.5 ± 1.3 24.7 ± 2.2
Amoxicillin 19.6 ± 1.0 19.3 ± 1.6 28.9 ± 3.4 40.8 ± 3.7 21.7 ± 1.3 25.6 ± 2.8 22.6 ± 3.4 20.4 ± 3.1 16.8 ± 1.3
Nafcillin 29.0 ± 1.4 32.9 ± 4.8 29.5 ± 3.1 34.3 ± 3.5 24.0 ± 1.9 35.7 ± 3.3 31.4 ± 2.8 35.2 ± 3.8 26.6 ± 3.7
Oxacillin 23.4 ± 2.3 24.0 ± 3.6 29.3 ± 2.5 26.7 ± 2.9 22.3 ± 2.5 25.0 ± 3.4 26.6 ± 2.1 21.5 ± 2.4 23.6 ± 2.4
Azlocillin 15.2 ± 1.1 10.9 ± 1.7 14.7 ± 1.4 10.6 ± 1.3 16.7 ± 1.7 17.0 ± 1.6 14.1 ± 1.3 12.8 ± 1.2 24.9 ± 4.3
Penicillin V 15.5 ± 1.5 12.7 ± 1.2 7.5 ± 1.0 16.7 ± 1.1 10.9 ± 1.2 12.2 ± 1.2 25.9 ± 2.6 35.2 ± 4.6 16.4 ± 2.9
Piperacillin 6.5 ± 0.9 8.0 ± 1.0 12.0 ± 1.6 6.2 ± 0.8 27.3 ± 2.4 20.3 ± 3.6 13.2 ± 1.5 12.2 ± 1.5 10.4 ± 1.1
Dicloxacillin 27.5 ± 2.1 30.3 ± 2.9 23.2 ± 3.4 24.9 ± 2.4 31.7 ± 4.2 25.0 ± 4.5 31.6 ± 5.1 24.2 ± 2.0 26.1 ± 1.3
Cloxacillin 21.1 ± 1.8 25.5 ± 2.4 26.5 ± 3.1 44.4 ± 5.1 22.0 ± 2.5 25.3 ± 3.2 20.2 ± 1.3 31.7 ± 4.7 22.5 ± 3.4
Cefalotin 26.3 ± 2.4 24.6 ± 2.5 27.0 ± 1.9 24.7 ± 2.6 20.9 ± 1.7 34.0 ± 5.1 18.6 ± 1.2 18.4 ± 1.3 16.7 ± 1.2
Cefoperazone 21.5 ± 1.3 18.3 ± 1.7 29.1 ± 4.1 25.8 ± 2.7 30.5 ± 4.2 20.5 ± 3.6 16.2 ± 1.3 25.5 ± 2.1 31.5 ± 4.6
Cefazolin 32.0 ± 2.9 26.1 ± 2.3 30.5 ± 3.2 29.8 ± 3.1 23.4 ± 3.4 26.9 ± 3.4 40.1 ± 2.5 31.5 ± 4.5 40.2 ± 5.1
Cefalexin 88.4 ± 6.8 87.7 ± 9.4 81.9 ± 7.6 69.9 ± 4.5 65.2 ± 7.5 75.2 ± 10.1 63.5 ± 5.4 75.8 ± 9.1 62.5 ± 9.3
Cefatriaxone 25.5 ± 1.5 19.7 ± 1.2 24.8 ± 4.8 23.5 ± 2.4 19.4 ± 1.4 21.2 ± 1.8 17.3 ± 1.2 31.4 ± 2.7 20.5 ± 1.2
Cefadroxil 69.8 ± 4.8 70.6 ± 8.1 65.2 ± 5.6 59.6 ± 6.1 69.9 ± 8.5 56.7 ± 5.2 84.9 ± 10.5 55.2 ± 3.4 71.5 ± 7.9
Ceftiofur 21.4 ± 2.6 16.7 ± 1.5 25.7 ± 2.4 34.6 ± 3.2 28.6 ± 3.4 19.4 ± 1.4 20.6 ± 4.2 22.1 ± 1.5 25.1 ± 3.4
Cefepime 9.4 ± 0.8 17.7 ± 1.2 27.9 ± 2.8 21.7 ± 1.6 17.4 ± 1.8 18.0 ± 1.6 16.9 ± 1.6 14.5 ± 1.1 22.4 ± 2.6
Cefaclor 19.7 ± 1.4 18.5 ± 2.4 31.5 ± 3.4 20.9 ± 1.2 19.6 ± 1.6 17.4 ± 1.2 14.8 ± 2.1 15.8 ± 2.1 20.6 ± 1.3
Cefquinome 19.5 ± 1.2 11.8 ± 1.5 16.9 ± 1.4 23.9 ± 2.5 12.0 ± 1.3 16.6 ± 1.4 11.3 ± 1.2 16.8 ± 1.3 19.9 ± 1.2
Cefradine 61.2 ± 5.7 59.6 ± 6.3 67.3 ± 7.3 58.7 ± 5.6 72.0 ± 5.7 56.1 ± 7.1 49.9 ± 6.1 52.4 ± 4.5 68.4 ± 8.2
Cefapirin 19.6 ± 1.3 14.1 ± 1.2 29.1 ± 1.7 23.3 ± 1.3 10.4 ± 1.0 15.9 ± 1.9 8.3 ± 0.9 18.5 ± 3.1 22.4 ± 3.7
Cefuroxime 45.8 ± 5.3 49.5 ± 5.4 46.2 ± 3.1 52.4 ± 6.1 46.2 ± 6.1 43.6 ± 4.1 46.8 ± 5.2 45.1 ± 4.1 43.5 ± 5.1
Moxalactam 21.4 ± 2.9 19.5 ± 1.7 32.1 ± 4.5 23.4 ± 3.2 13.3 ± 1.2 22.1 ± 2.3 8.2 ± 1.0 20.4 ± 2.5 44.2 ± 3.1
Cefalonium 5.2 ± 0.7 6.2 ± 0.8 11.7 ± 1.6 6.3 ± 0.8 21.5 ± 3.3 32.9 ± 4.3 10.3 ± 1.3 14.2 ± 1.3 15.2 ± 1.5
Cefminox 19.0 ± 1.6 22.9 ± 3.4 18.0 ± 1.2 17.4 ± 1.5 12.8 ± 1.2 20.8 ± 3.4 16.2 ± 2.1 25.9 ± 3.0 18.5 ± 1.1
Ceftazidime 23.1 ± 2.6 19.8 ± 1.5 16.8 ± 2.3 19.6 ± 2.1 21.3 ± 2.3 19.3 ± 1.8 21.1 ± 1.9 18.5 ± 1.2 24.8 ± 3.1
Carbenicillin 6.7 ± 0.8 16.8 ± 1.1 15.2 ± 1.3 11.1 ± 1.0 19.6 ± 1.4 22.5 ± 2.0 15.0 ± 1.2 17.7 ± 1.1 15.9 ± 1.6
Cefoxitin 12.7 ± 2.6 17.0 ± 1.3 19.9 ± 1.2 16.0 ± 1.4 10.5 ± 2.1 11.7 ± 1.8 12.3 ± 2.1 11.5 ± 1.8 15.5 ± 1.0
Floxacillin 6.2 ± 0.8 7.8 ± 1.0 12.3 ± 1.3 8.7 ± 1.1 4.3 ± 0.5 7.2 ± 1.3 10.3 ± 1.3 20.4 ± 3.3 16.7 ± 2.1
Sulbenicillin 8.7 ± 1.1 12.5 ± 1.1 16.6 ± 2.5 10.0 ± 1.0 18.3 ± 1.7 25.5 ± 1.2 7.2 ± 0.9 13.5 ± 2.1 15.2 ± 1.3
Ticarcillin 12.5 ± 1.6 13.8 ± 2.4 15.4 ± 1.4 12.3 ± 2.6 27.9 ± 3.5 24.9 ± 2.1 15.1 ± 1.5 11.3 ± 1.3 11.4 ± 2.0
Aztreonam 93.1 ± 6.7 86.8 ± 5.7 95.4 ± 10.1 90.0 ± 9.4 94.3 ± 10.1 100.9 ± 9.7 106.4 ± 9.1 100.3 ± 9.0 97.5 ± 9.5
  1. Note: The statistical method was used to analyze the significant difference between the wild-type protein and mutant proteins. The underlined number indicated that the inhibition rate was significantly increased, and the boldface number showed that the inhibition rate was significantly reduced (p < 0.05)