TABLE 2.
Antiviral activitiesa of NCINIs against NCINI-3-resistant HIV-1NL4-3 clones
| Recombinant HIV-1NL4-3 clone | NCINI-1 |
NCINI-2 |
NCINI-3 |
NCINI-4 |
RAL |
DRV |
||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mean EC50 (μM) ± SD | Fold change | Mean EC50 (μM) ± SD | Fold change | Mean EC50 (μM) ± SD | Fold change | Mean EC50 (μM) ± SD | Fold change | Mean EC50 (μM) ± SD | Fold change | Mean EC50 (μM) ± SD | Fold change | |
| INWT | 7.01 ± 5.41 | 1 | 2.60 ± 0.34 | 1 | 0.19 ± 0.13 | 1 | 0.027 ± 0.004 | 1 | 0.0017 ± 0.0025 | 1 | 0.0037 ± 0.0003 | 1 |
| INA128T | >10 | ND | >10 | ND | 3.12 ± 0.12 | 16.1 | 0.31 ± 0.01 | 11.6 | 0.0028 ± 0.0056 | 1.7 | 0.0094 ± 0.0008 | 2.5 |
| INP15 | >10 | ND | >10 | ND | 3.36 ± 0.11 | 17.3 | 0.32 ± 0.06 | 12.2 | 0.0028 ± 0.0058 | 1.7 | 0.0097 ± 0.0031 | 2.6 |
| INP20 | − | − | − | − | 2.14 ± 0.14 | 11.1 | 0.39 ± 0.04 | 14.7 | 0.0008 ± 0.0041 | 0.5 | 0.0074 ± 0.0018 | 2.0 |
| INP26 | − | − | − | − | 34.83 ± 2.21 | 179.8 | 2.43 ± 0.61 | 91.7 | 0.0017 ± 0.0025 | 1.0 | 0.0034 ± 0.0016 | 0.9 |
| INH171Q | >10 | ND | >10 | ND | 0.42 ± 0.08 | 2.2 | 0.31 ± 0.04 | 11.7 | 0.0027 ± 0.0051 | 1.6 | 0.0085 ± 0.0024 | 2.3 |
| INK173Q | >10 | ND | >10 | ND | 0.14 ± 0.03 | 0.7 | 0.021 ± 0.01 | 0.8 | 0.0022 ± 0.0011 | 1.3 | 0.0032 ± 0.0011 | 0.8 |
| INN254K | − | − | − | − | 0.27 ± 0.04 | 1.4 | 0.092 ± 0.03 | 3.5 | 0.0019 ± 0.0010 | 1.1 | 0.0054 ± 0.0020 | 1.4 |
a
MT-4 cells (1 × 104 cells/ml) were exposed to 100 TCID50s of each infectious HIV-1 clone, and the inhibition of p24 production by the drug was used as the endpoint on day 7 in culture. The fold changes represent EC50 ratios of each HIV-1 clone to wild-type HIV-1. All assays were performed in duplicate, and the data shown are mean values ± SD derived from the results of three independent experiments. ND, not determined; −, not examined.