TABLE 2.
Effects of selected anti-HBV drugs on replication of wt HBV and HBV laboratory strains of genotype D carrying lamivudine, adefovir, or lamivudine-adefovir resistance mutationsa
| HBV strainb | LAMc
|
ADVc
|
TDFc
|
ETVc
|
PMEO-DAPym
|
|||||
|---|---|---|---|---|---|---|---|---|---|---|
| EC50 (μM) | FRd | EC50 (μM) | FR | EC50 (μM) | FR | EC50 (μM) | FR | EC50e (μM) | FR | |
| wt | 2.48 ± 0.67 | 1 | 15.8 ± 1.9 | 1 | 10.3 ± 1.3 | 1 | 0.8 ± 0.1 | 1 | 4.0 ± 0.51 | 1 |
| ADVr | 2.65 ± 0.52 | 1.06 | 50.3 ± 11 | 3.2 | 46 ± 6 | 4.5 | 0.7 | 0.88 | 4.5 ± 0.35 | 1.1 |
| LAMr | >100 | >40 | 15.5 ± 1.8 | 0.98 | 35.2 ± 5.1 | 3.4 | 5 ± 0.25 | 6.25 | 4.7 ± 1.12 | 1.2 |
| LAMr +ADVr | >100 | >40 | 100 ± 20 | 6.3 | 45.5 ± 6.1 | 4.4 | 5 ± 0.7 | 6.25 | 5.7 ± 0.77 | 1.4 |
LAM, lamivudine; ADV, adefovir; TDF, tenofovir; ETV, entecavir.
Lamivudine-resistant (LAMr) mutant rtL180M/M204V, adefovir-resistant (ADVr) mutant rtN236T, and lamivudine-adefovir-resistant mutant (LAMr +ADVr) rtL180M/M204V/N236T.
Data were reported previously (3).
FR, fold resistance, which is equal to (mutant EC50)/(wt EC50).
The values represent the means of at least three independent experiments, each of which was performed in triplicate. For each experiment, the drug-resistant HBV strains and their corresponding wt strain were treated simultaneously with the same range of drug concentrations (from 0 to 100 μM for PMEO-DAPym, lamivudine, adefovir, and tenofovir; from 0 to 10 μM for entecavir), and all the samples were extracted and analyzed by Southern blotting in parallel.