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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.