Table 1.
Target cell line and inhibitor | Mean EC50 ± SD (μM) (mean % inhibition ± SD) |
|||
---|---|---|---|---|
HIV-1 | SRV-4 | MoMLV | FIV | |
TE671 | ||||
NRTIs | ||||
Thymidine analogs | ||||
AZT | 0.018 ± 0.0074 | 0.042 ± 0.012* | 0.019 ± 0.0043 | 0.029 ± 0.0035 |
d4T | 0.40 ± 0.10 | 0.17 ± 0.039 | 3.7 ± 0.82** | 0.52 ± 0.0055 |
Inosine analog | ||||
ddI | 10 ± 1.7 | 4.4 ± 1.3** | >10 (0) | 19 ± 1.7** |
Cytidine analogs | ||||
ddC | 5.6 ± 1.1 | 2.7 ± 0.13** | >10 (0)** | 3.2 ± 0.50** |
3TC | 4.4 ± 0.75 | 3.9 ± 1.2 | >10 (0)** | 2.2 ± 0.50* |
FTC | 0.48 ± 0.15 | 0.50 ± 0.082 | >10 (0)** | 0.35 ± 0.030 |
Adenosine analog | ||||
TDF | 0.0043 ± 0.00058 | 0.00080 ± 0.00037** | 0.0035 ± 0.0012 | 0.0015 ± 0.00076** |
INSTI | ||||
RAL | 0.0031 ± 0.0015 | 0.015 ± 0.0065 | 0.0017 ± 0.00036 | 0.049 ± 0.00090* |
MT-2 | ||||
NRTIs | ||||
Thymidine analogs | ||||
AZT | 0.037 ± 0.014 | 0.11 ± 0.037 | 0.71 ± 0.36* | 1.4 ± 0.40** |
d4T | 0.50 ± 0.13 | 2.3 ± 0.44 | 3.5 ± 0.61 | 21 ± 6.6** |
Inosine analog | ||||
ddI | 3.4 ± 0.70 | >10 (42 ± 4.4)* | >10 (0)* | 16 ± 4.7** |
Cytidine analogs | ||||
ddC | 7.2 ± 2.4 | 0.59 ± 0.45** | >10 (0) | 3.5 ± 1.1* |
3TC | 2.8 ± 1.0 | >10 (17 ± 3.3)** | >10 (0)** | 1.1 ± 0.10** |
FTC | 0.52 ± 0.12 | 3.0 ± 0.40** | >10 (0)** | 0.22 ± 0.12 |
Adenosine analog | ||||
TDF | 0.0071 ± 0.0018 | 0.0016 ± 0.00025** | 0.0071 ± 0.00056 | 0.0039 ± 0.0021 |
INSTI | ||||
RAL | 0.0033 ± 0.0010 | 0.0024 ± 0.00068 | 0.00064 ± 0.00057 | 0.062 ± 0.032** |
Antiviral activities of NRTIs and an INSTI against VSV-G-pseudotyped SRV-4, HIV-1, MoMLV, and FIV were determined by using a luciferase assay. Data are shown as means and standard deviations obtained from three or more independent experiments, and statistical analyses were performed (*, P < 0.05; **, P < 0.01; not indicated, P ≥ 0.05 [determined by Dunnett's test against control HIV-1]). EC50s shown as >10 indicate that more than 10 μM drugs is required to block viral infection by 50%. In this case, percent inhibition of viral infection at 10 μM is shown in parentheses and is considered 10 μM for statistical analysis.