TABLE 2.
NRTI resistance mutation(s)a | Mean change (fold) in EC50 ± SDb
|
||
---|---|---|---|
VRX-413638 (wt EC50 = 27.1 ± 3.40 nM) | AZT (wt EC50 = 16.4 ± 2.80 nM) | FTC (wt EC50 = 42.5 ± 3.70 nM) | |
K65R | 0.2 ± 0.03 | 0.6 ± 0.06 | 102.7 ± 7.16* |
M41L, D67N, T69N, K70R, T215F, K219E | 0.7 ± 0.14 | 21.0 ± 7.66* | 13.5 ± 6.60* |
M41L, E44D, D67N, T69D, V118I, L210W, T215Y | 0.7 ± 0.19 | 389.1 ± 143.78* | 25.8 ± 21.24* |
V75I, F77L, F116Y, Q151M | 0.9 ± 0.08 | 43.9 ± 9.43* | 17.9 ± 6.99* |
M184V | 3.0 ± 0.66* | 0.3 ± 0.03 | Max* |
M41L, K70R, T215F, K219E | 1.4 ± 0.03 | 83.7 ± 21.37* | 9.4 ± 4.30* |
K65R, K70R, V75I, F77L, F116Y, Q151M | 1.6 ± 0.65 | Max* | Max* |
D67N, T69N, K70R, M184V, T215F, K219Q | 1.9 ± 0.01 | 4.8 ± 2.20* | Max* |
M41L, D67N, V118I, M184V, L210W, T215Y | 4.4 ± 1.18* | 9.5 ± 0.91* | Max* |
M41L, D67N, M184V, L210W, T215Y | 5.7 ± 1.05* | 13.2 ± 7.32* | Max* |
M41L, E44D, D67N, T69D, V118I, M184V, L210W, T215Y | 11.2 ± 0.87* | 54.7 ± 8.68* | Max* |
T69K, K70G, V75I, F77L, F116Y, Q151M, M184V | 15.7 ± 2.98* | 274.3 ± 33.35* | Max* |
Molecular clones with K65R and M184V mutations were in the HIV-1 NL4-3 format. All other viruses were in pNLPFB and were obtained from the U.S. NIH AIDS Research and Reference Reagent Repository.
EC50 values were determined using the reporter cell line HeLa-JC-53-LTR-Luci. Mean EC50 values ± SD were from two tests. Max; the change could not be determined because the EC50 was >10 μM; *, EC50 was statistically significantly higher than that against wild-type virus (P < 0.05).