Table 2. Sensitivity and resistance of different mutation sites in HIV-1 CRF_BC pol region to NNRTIs using an in vitro phenotypic assaya.
Mutations | TMC-125 | DLV | NVP | EFV | ||||
EC50a (nM) | Fold changec | EC50 (µM) | Fold change | EC50 (µM) | Fold change | EC50 (nM) | Fold change | |
WTb (BC) | 1.03±0.10 | - | 0.09±0.00 | - | 0.10±0.01 | - | 1.713±0.180 | - |
W88C (BC) | 1.09±0.02 | 1.06 | 0.05±0.00 | 0.51 | 0.09±0.01 | 0.89 | 0.98±0.06 | 0.57 |
K101Q (BC) | 3.61±0.35 | 3.50 | 0.15±0.01 | 1.71 | 1.30±0.14 | 12.57 | 5.25±1.80 | 3.06 |
K103N (BC) | 1.400±0.06 | 1.35 | 7.35±0.23 | 82.56 | 17.23±1.36 | 167.23 | 97.48±4.06 | 56.91 |
I132L (BC) | 5.21±0.78 | 2.55 | 1.72±0.12 | 19.35 | 4.30±0.26 | 28.05 | 10.52±1.22 | 6.13 |
R135L (BC) | 1.36±0.15 | 1.32 | 0.07±0.00 | 0.75 | 0.12±0.00 | 1.13 | 1.87±0.13 | 1.09 |
T139R (BC) | 3.73±0.62 | 1.82 | 0.42±0.02 | 4.69 | 2.59±0.53 | 25.12 | 3.23±0.38 | 1.89 |
T139K (BC) | 4.82±0.96 | 4.67 | 0.33±0.02 | 3.66 | 0.76±0.02 | 7.35 | 5.65±0.12 | 3.30 |
M184V (BC) | 0.69±0.04 | 0.67 | 0.03±0.00 | 0.31 | 0.05±0.01 | 0.44 | 0.70±0.05 | 0.41 |
Y181C (BC) | 5.91±1.700 | 5.73 | 4.53±0.13 | 50.92 | 15.84±1.42 | 153.74 | 3.22±0.14 | 1.88 |
H221Y (BC) | 1.42±0.16 | 1.38 | 0.18±0.01 | 2.04 | 0.21±0.03 | 2.02 | 3.02±0.51 | 1.76 |
L228R (BC) | 1.02±0.101 | 0.99 | 0.042±0.001 | 0.47 | 0.11±0.00 | 1.03 | 0.79±0.04 | 0.46 |
WTb (B) | 1.66±0.35 | - | 0.11±0.00 | - | 0.19±0.01 | - | 3.26±0.25 | - |
I132L (B) | 6.51±1.19 | 3.91 | 0.51±0.02 | 4.61 | 1.20±0.03 | 6.38 | 11.61±0.19 | 3.56 |
T139K (B) | 5.21±1.03 | 3.13 | 0.200±0.01 | 1.78 | 0.43±0.03 | 2.26 | 6.87±0.79 | 2.10 |
T139R (B) | 9.64±0.87 | 5.79 | 0.44±0.01 | 3.99 | 1.09±0.05 | 5.78 | 8.97±0.63 | 2.75 |
Note:
The unit for the EC50 values of TMC-125 and EFV is nM, while that for the EC50 values of DLV and NVP is µM. Data were presented as the mean ± standard deviations of three separate determinations.
WT: HIV-1 CRF_BC strain N-14-1.
Fold change was determined by calculating the ratio of EC50s for mutations and WT viruses.