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Table 1 Compilation of EC 50 and fold change values for site-directed mutants of HIV-2 ROD9 and HIV-1 NL4-3 integrase

From: In vitro activity of dolutegravir against wild-type and integrase inhibitor-resistant HIV-2

HIV Type

Strain

EC 50 for DTG (nM) a

n b

Fold Change c

HIV-2

Wild-type

2.3 ± 0.7

24

 
 

E92Q

7.7 ± 1.2

3

3

 

T97A

3.2 ± 0.8

3

1

 

G140S

3.2 ± 0.8

3

1

 

Y143C

7.7 ± 2.2

3

3

 

Q148H

3.5 ± 1.4

4

1

 

Q148K

23 ± 10

4

10

 

Q148R

5.7 ± 2.1

4

2

 

N155H

5.0 ± 2.4

3

2

 

E92Q + Y143C

15 ± 10

5

6

 

T97A + Y143C

>10000

13

>5000

 

G140S + Q148R

108 ± 54

7

46

 

E92Q + N155H

25 ± 17

7

10

 

T97A + N155H

27 ± 13

3

12

HIV-1

Wild-type

1.5 ± 0.6

14

 
 

T97A + Y143C

1.5 ± 0.4

4

1

 

G140S + Q148R

6.8 ± 2.7

4

4

 

E92Q + N155H

3.6 ± 0.7

4

2

  1. a50% effective concentration of dolutegravir (DTG) as measured in the MAGIC-5A single-cycle assay. Values were compiled from the data used to generate Figures 2A and 2D and are expressed as means ± standard deviations. Numbers shown in bold type are significantly greater than the values for the corresponding wild-type strains (p < 0.05; ANOVA of log10-transformed EC50 values with Tukey’s post-test; performed in Prism version 6.0, GraphPad Software, Inc.).
  2. bNumber of independent determinations for each strain.
  3. cFold change in EC50 relative to the corresponding wild-type strain.