TABLE 4.
Susceptibilities of purified SIV recombinant integrase proteins for DTG, EVG, and RAL
| SIVmac239 IN protein type | Result fora: |
|||||
|---|---|---|---|---|---|---|
| DTG |
EVG |
RAL |
||||
| Ki (mean ± SEM nM) | ∼FC | Ki (mean ± SEM nM) | ∼FC | Ki (mean ± SEM nM) | ∼FC | |
| WT | 1.1 ± 0.19 | 1.0 | 2.7 ± 0.29 | 1.0 | 2.1 ± 0.22 | 1.0 |
| Recombinant | ||||||
| E92Q | 1.5 ± 0.54 | 1.4 | 11.0 ± 5.0* | 4.1 | 4.7 ± 0.36* | 2.2 |
| T97A | 0.95 ± 0.10 | 0.9 | 3.3 ± 0.51 | 1.2 | 3.9 ± 1.6 | 1.8 |
| G118R | 5.9 ± 0.65* | 5.6 | 7.3 ± 2.0* | 2.7 | 5.5 ± 1.3* | 2.6 |
| Y143R | 1.8 ± 0.95 | 1.7 | 3.6 ± 1.3 | 1.3 | 19.8 ± 3.9* | 9.4 |
| Q148R | 6.7 ± 2.4* | 6.4 | 328 ± 137* | 122.7 | 252 ± 111* | 119.8 |
| N155H | 1.9 ± 0.80 | 1.8 | 11.3 ± 1.6* | 4.2 | 8.8 ± 2.3* | 4.2 |
| R263K | 1.3 ± 0.37 | 1.2 | 4.0 ± 1.8 | 1.5 | 2.0 ± 0.79 | 0.9 |
| E92Q T97A | 1.1 ± 0.56 | 1.1 | 4.3 ± 1.4 | 1.6 | 4.8 ± 2.7 | 2.3 |
| E92Q Y143R | 2.1 ± 0.73 | 2.0 | 16.5 ± 5.9* | 6.2 | 108 ± 65.5* | 51.3 |
| G140S Q148R | 27.9 ± 6.8* | 26.6 | 679 ± 354* | 253.9 | 337 ± 174* | 160.3 |
| R263K H51Y | 1.5 ± 0.90 | 1.4 | 4.6 ± 2.5 | 1.7 | 2.8 ± 0.75 | 1.3 |
a
All data represent the results from at least 3 independent experiments. Fold changes (FC) of >10-fold are shown in boldface. *, statistically significant differences. Statistical significance was calculated for individual pairs of data using a one-sample two-tailed t test with a statistical cutoff of P ≤ 0.05.