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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