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Table 5 The inhibition rate (%) of 33 β-lactam drugs on BlaR-CTD proteins of multipoint mutations (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/S19C/G24C Q147K/S19C/G24C I188K/S19C/G24C S190Y/S19C/G24C V197D/S19C/G24C A138E/R50C/Q147C S190Y/R50C/Q147C V197D/R50C/Q147C I188K/R50C/Q147C A138E/E183C/I188C Q147K/E183C/I188C S190Y/E183C/I188C V197D/E183C/I188C
Penicillin G 23.7 ± 3.5 18.5 ± 1.2 45.3 ± 4.5 7.4 ± 1.3 34.0 ± 3.3 32.2 ± 4.4 7.6 ± 1.0 36.5 ± 5.6 67.8 ± 7.9 10.4 ± 2.0 8.4 ± 1.0 8.9 ± 0.7 7.4 ± 1.1 47.1 ± 4.3
Ampicillin 28.2 ± 2.6 17.6 ± 3.4 5.1 ± 1.1 7.5 ± 1.4 10.9 ± 1.3 16.8 ± 1.7 37.3 ± 5.1 18.3 ± 2.3 10.6 ± 1.2 11.2 ± 2.1 14.0 ± 2.2 6.8 ± 1.1 7.2 ± 1.4 10.2 ± 1.4
Amoxicillin 21.2 ± 2.4 20.5 ± 3.4 5.3 ± 0.6 12.6 ± 2.4 8.8 ± 1.2 16.5 ± 1.1 11.6 ± 1.3 21.6 ± 2.7 12.3 ± 1.5 11.0 ± 1.3 8.6 ± 1..3 6.7 ± 0.6 7.2 ± 1.0 10.0 ± 1.2
Nafcillin 28.9 ± 3.7 27.9 ± 4.3 14.9 ± 0.7 18.4 ± 2.1 31.1 ± 2.5 14.6 ± 2.3 13.1 ± 2.0 26.5 ± 3.5 12.1 ± 1.2 17.8 ± 2.5 13.0 ± 2.5 9.6 ± 0.7 8.3 ± 1.2 15.3 ± 1.1
Oxacillin 24.0 ± 1.8 22.5 ± 2.3 5.9 ± 0.6 16.6 ± 2.3 10.4 ± 1.3 24.5 ± 3.5 11.7 ± 2.1 28.8 ± 3.4 13.5 ± 2.3 12.8 ± 1.6 9.6 ± 1.0 7.2 ± 1.0 7.0 ± 1.3 26.8 ± 3.5
Azlocillin 19.7 ± 2.5 12.0 ± 1.1 15.2 ± 1.1 11.6 ± 2.4 28.6 ± 3.4 12.6 ± 1.7 19.0 ± 1.3 19.7 ± 1.2 20.5 ± 3.5 8.9 ± 0.7 7.4 ± 1.0 5.5 ± 1.3 5.7 ± 0.9 11.2 ± 1.2
Penicillin V 24.7 ± 2.6 20.1 ± 1.4 5.2 ± 1.2 16.3 ± 2.2 29.4 ± 2.3 26.6 ± 3.4 17.9 ± 3.1 24.8 ± 4.5 12.6 ± 2.3 9.6 ± 1.0 7.8 ± 0.8 5.7 ± 1.0 6.0 ± 0.8 11.5 ± 2.4
Piperacillin 12.8 ± 3.1 24.0 ± 4.2 14.4 ± 4.1 9.2 ± 1.2 17.5 ± 2.3 15.1 ± 2.2 14.3 ± 1.3 12.8 ± 2.3 16.3 ± 1.2 8.9 ± 1.3 7.1 ± 1.4 5.6 ± 1.1 6.0 ± 1.0 12.1 ± 1.2
Dicloxacillin 24.3 ± 4.2 26.2 ± 1.3 4.8 ± 0.7 11.6 ± 2.4 29.0 ± 3.2 26.6 ± 1.8 24.5 ± 5.1 23.2 ± 3.5 7.0 ± 0.9 11.7 ± 2.3 9.2 ± 0.6 6.7 ± 0.5 8.1 ± 0.7 21.2 ± 3.4
Cloxacillin 23.6 ± 2.4 18.5 ± 2.4 15.2 ± 2.3 10.2 ± 4.2 29.4 ± 2.4 28.3 ± 3.4 14.2 ± 0.8 24.2 ± 2.7 24.3 ± 2.3 12.0 ± 2.1 9.6 ± 1.5 7.0 ± 1.2 6.7 ± 1.0 10.9 ± 1.1
Cefalotin 17.3 ± 1.5 13.0 ± 3.4 24.8 ± 3.4 8.6 ± 0.9 9.2 ± 1.1 14.3 ± 2.2 14.2 ± 1.0 8.1 ± 1.0 14.8 ± 2.2 11.6 ± 2.0 9.9 ± 1.1 6.7 ± 1.1 6.4 ± 1.1 38.7 ± 4.7
Cefoperazone 20.3 ± 2.4 8.7 ± 1.6 9.9 ± 1.1 6.2 ± 1.0 27.7 ± 3.3 18.8 ± 1.1 5.9 ± 0.4 8.6 ± 0.8 7.3 ± 1.1 21.6 ± 3.1 23.2 ± 3.7 7.7 ± 1.4 22.5 ± 1.3 9.2 ± 1.6
Cefazolin 31.3 ± 4.6 15.9 ± 2.3 20.8 ± 3.3 10.1 ± 2.6 21.4 ± 2.6 19.6 ± 2.3 12.1 ± 3.3 47.6 ± 6.7 19.1 ± 1.2 33.0 ± 2.4 21.2 ± 1.8 20.7 ± 2.2 13.7 ± 2.2 19.4 ± 2.2
Cefalexin 80.1 ± 9.7 83.3 ± 9.4 65.6 ± 7.9 63.5 ± 6.7 65.9 ± 5.9 80.1 ± 7.9 79.7 ± 6.4 38.4 ± 5.8 85.0 ± 9.9 91.5 ± 9.4 69.8 ± 5.5 69.0 ± 7.8 66.6 ± 7.9 77.4 ± 8.9
Cefatriaxone 22.1 ± 4.6 22.5 ± 2.3 26.5 ± 3.2 10.9 ± 1.0 41.9 ± 6.7 61.7 ± 7.7 15.0 ± 2.5 12.6 ± 1.3 29.5 ± 3.4 37.2 ± 4.6 26.6 ± 4.0 17.7 ± 2.3 10.2 ± 1.5 29.2 ± 3.4
Cefadroxil 70.2 ± 5.5 63.8 ± 5.4 58.8 ± 4.6 45.1 ± 6.1 56.3 ± 4.5 68.3 ± 5.6 59.8 ± 6.7 29.4 ± 3.5 76.0 ± 8.9 81.3 ± 7.6 51.0 ± 7.6 50.4 ± 5.5 37.7 ± 4.3 66.2 ± 7.8
Ceftiofur 16.1 ± 1.1 10.6 ± 1.7 15.2 ± 2.1 7.6 ± 0.8 12.0 ± 1.3 26.8 ± 1.5 8.8 ± 1.2 10.1 ± 1.2 14.2 ± 1.2 26.3 ± 4.8 24.2 ± 2.1 16.4 ± 1.6 8.3 ± 1.1 15.9 ± 3.4
Cefepime 13.2 ± 3.3 9.5 ± 1.1 13.2 ± 1.3 6.0 ± 1.0 18.3 ± 1.1 13.0 ± 4.7 7.1 ± 0.9 8.3 ± 1.1 8.9 ± 1.0 25.2 ± 2.2 26.7 ± 3.7 20.3 ± 2.2 16.6 ± 2.4 8.2 ± 0.7
Cefaclor 19.2 ± 2.2 32.6 ± 2.3 17.1 ± 3.4 8.1 ± 1.4 28.3 ± 2.7 38.4 ± 2.2 13.8 ± 2.1 13.0 ± 1.3 26.8 ± 3.4 40.2 ± 4.3 36.8 ± 4.6 31.4 ± 3.4 15.5 ± 2.3 28.9 ± 2.3
Cefquinome 21.1 ± 1.4 12.6 ± 2.2 4.4 ± 1.1 6.3 ± 0.7 21.5 ± 1.4 14.1 ± 1.3 6.4 ± 1.0 6.5 ± 0.8 27.8 ± 2.2 25.3 ± 3.4 23.1 ± 2.1 16.8 ± 1.2 16.8 ± 1.6 29.0 ± 4.5
Cefradine 59.6 ± 6.9 66.5 ± 8.9 68.0 ± 7.8 43.1 ± 8.7 51.8 ± 6.7 58.1 ± 8.9 74.2 ± 5.9 69.1 ± 5.2 65.4 ± 8.3 74.1 ± 6.4 58.7 ± 8.9 76.1 ± 7.6 74.6 ± 8.6 53.3 ± 8.9
Cefapirin 13.5 ± 3.4 10.2 ± 2.3 5.6 ± 1.1 5.8 ± 1.1 11.2 ± 1.7 14.9 ± 1.1 6.4 ± 1.1 6.9 ± 0.9 9.3 ± 1.4 22.2 ± 2.5 15.3 ± 2.4 16.0 ± 3.3 13.2 ± 1.5 7.4 ± 1.2
Cefuroxime 44.3 ± 5.6 47.4 ± 5.6 49.1 ± 6.5 30.0 ± 4.5 68.9 ± 5.5 57.1 ± 4.5 36.1 ± 3.5 20.5 ± 2.4 46.3 ± 3.4 39.2 ± 6.7 31.4 ± 3.8 26.0 ± 2.2 29.5 ± 3.6 33.1 ± 4.6
Moxalactam 20.0 ± 1.3 10.6 ± 1.5 14.9 ± 4.2 7.4 ± 0.8 29.6 ± 4.3 21.2 ± 3.4 29.0 ± 3.3 8.1 ± 1.0 12.0 ± 1.1 18.8 ± 2.7 18.4 ± 4.5 16.5 ± 2.7 17.9 ± 2.4 28.7 ± 3.4
Cefalonium 8.9 ± 1.1 7.6 ± 2.1 14.4 ± 1.1 6.5 ± 1.5 30.8 ± 5.4 28.0 ± 2.3 5.1 ± 1.0 6.6 ± 0.8 6.5 ± 0.8 19.8 ± 3.8 19.3 ± 1.2 14.8 ± 2.6 12.3 ± 3.3 9.9 ± 1.5
Cefminox 25.5 ± 3.6 42.4 ± 3.8 48.7 ± 6.9 20.2 ± 3.3 67.2 ± 7.5 66.9 ± 7.8 24.5 ± 4.5 17.5 ± 2.4 79.0 ± 5.8 24.8 ± 3.3 17.6 ± 3.3 22.5 ± 3.4 25.0 ± 4.1 82.0 ± 9.2
Ceftazidime 20.2 ± 4.4 10.8 ± 1.2 15.9 ± 3.4 8.1 ± 1.0 33.3 ± 3.6 37.2 ± 3.2 8.6 ± 2.2 9.1 ± 1.0 14.9 ± 2.2 21.7 ± 2.7 21.4 ± 3.2 17.4 ± 1.2 12.0 ± 2.3 13.4 ± 1.3
Carbenicillin 8.9 ± 1.1 6.1 ± 1.1 15.3 ± 4.2 6.8 ± 0.8 26.6 ± 4.5 30.1 ± 4.4 6.1 ± 1.1 7.4 ± 1.2 9.2 ± 1.6 10.0 ± 1.9 21.3 ± 2.4 21.7 ± 3.3 8.5 ± 0.9 8.1 ± 0.8
Cefoxitin 14.9 ± 2.2 9.3 ± 0.7 22.9 ± 2.2 9.7 ± 1.7 52.4 ± 6.7 40.6 ± 6.6 16.2 ± 3.4 12.2 ± 2.3 25.0 ± 3.5 9.2 ± 2.4 9.6 ± 1.0 10.2 ± 1.1 12.8 ± 2.2 14.0 ± 2.4
Floxacillin 6.3 ± 0.8 5.4 ± 0.9 15.0 ± 1.3 4.7 ± 1.3 33.8 ± 4.2 26.1 ± 6.3 5.6 ± 0.8 6.6 ± 1.1 7.5 ± 1.1 17.6 ± 1.3 13.1 ± 1.6 12.2 ± 2.6 6.8 ± 1.4 6.9 ± 1.1
Sulbenicillin 18.9 ± 2.3 10.4 ± 1.3 15.2 ± 2.1 7.2 ± 0.8 32.9 ± 3.7 32.7 ± 2.4 8.1 ± 1.1 7.9 ± 1.2 12.6 ± 2.3 20.6 ± 3.2 18.7 ± 3.3 13.3 ± 3.7 14.8 ± 3.3 9.3 ± 1.4
Ticarcillin 19.7 ± 1.7 10.5 ± 1.5 17.3 ± 3.4 8.8 ± 1.3 36.2 ± 5.4 30.9 ± 3.2 8.1 ± 1.6 8.0 ± 1.0 15.4 ± 1.2 16.9 ± 2.7 15.2 ± 1.2 14.8 ± 2.2 14.4 ± 2.7 10.2 ± 1.0
Aztreonam 102.5 ± 9.1 95.7 ± 10.4 100.1 ± 9.3 90.3 ± 6.6 62.5 ± 6.8 70.2 ± 6.5 105.6 ± 9.1 65.5 ± 8.2 74.3 ± 8.2 102.5 ± 9.9 89.6 ± 9.7 98.6 ± 7.8 95.0 ± 9.3 85.0 ± 5.3
  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