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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)
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Journal of Biological Engineering

ISSN: 1754-1611