Table 4. Antiviral sensitivities of site-directed mutants.
| Group | Genotype | FC EC50 | % in LANLa | % in LANLa | RC (%) | |
|---|---|---|---|---|---|---|
| GSK 3532795 | bevirimat | LANL Subtype B | LANL all subtypes | |||
| 1 | WTb | 1.0 ± 0.5 (1.2 nM) | 1.0 ± 0.2 (12.7 nM) | 50.8 | 39.3 | 100 |
| V370A | 1.8 ± 1.3 | 110 ± 24 | 16.2 | 39.9 | 100 | |
| V362I | 2.2 ± 1.2 | 0.6 | 15.4 | 7.8 | 68 | |
| ΔT371 | 2.0 ± 0.5 | 28 | 0.06 | 0.02 | 90 | |
| V370A/ΔT371 | 5.5 ± 0.6 | >862 | 0 | 0.06 | 74 | |
| ΔV370 | 5.8 ± 1.3 | >862 | 1.1 | 0.08 | 20 | |
| A364V | 835 | >862 | 0.18 | 0.13 | 82 | |
| 2 | T332S | 1.9 ± 0.5 | 21 | 0.37 | 22.9 | 61 |
| A326T | 2.2 ± 0.2 | 1.3 ± 0.3 | 0 | 94.4 | 96 | |
| R286K | 2.5 ± 1.2 | 1.9 ± 0.5 | 32.3 | 45 | 92 | |
| H219Q | 1.2 | 1.1 | 25.2 | 23.3 | ndc | |
| G221E | 0.9 ± 0.07 | 3.6 | 0.06 | 0.06 | nd | |
| A326S | 0.7 ± 0.01 | 3.9 | 13 | 5.2 | nd | |
| I333V | 2.2 ± 0.7 | 1.7 | 0 | 0.06 | nd | |
| I376V | 1.9 ± 0.3 | 12 | 16.9 | 17.6 | nd | |
| 3 | T332S/V370A | 1.9 ± 0.5 | nd | 0.06 | 3.1 | nd |
| R286K/T332S | 2.7 ± 0.3 | nd | 0.25 | 7.9 | 106 | |
| R286K/A326T | 3 ± 0.3 | 3.7 ± 1.5 | 0 | 0.02 | 106 | |
| A326T/V370A | 3.4 ± 0.7 | 21 ± 6.0 | 0 | 0.02 | 93 | |
| R286K/V370A | 5.3 ± 0.1 | 381 ± 98 | 4.32 | 17.8 | 36 | |
| A326T/V362I | 12 ± 3.3 | 4.5 | 0 | 0 | 93 | |
| V362I/T332S | 5.7 ± 1.7 | 2.9 | 0 | 0.4 | 65 | |
| A326T/ΔV370 | 29 | 153 | 0 | 0 | nd | |
| R286K/V362I | 61 ± 35 | nd | 2.96 | 2.5 | 41 | |
| V362I/V370A | 208 ± 1.7 | >862 | 1.79 | 5.4 | 60 | |
| 4 | R286K/A326T/V370A | 159 ± 123 | >233 | 0 | 0 | 86 |
| H219Q/V362I/V370A | 357 ± 86 | nd | 0.31 | 1.1 | 115 | |
| R286K/A326T /V362I | 437 ± 142 | nd | 0 | 0 | 94 | |
| V362I/V370A/ΔT371 | 1072 ± 321 | >862 | 0 | 0 | nd | |
a: 2018 version
b: NL4-3 virus
c: nd = not determined; RC, replicate capacity; FC EC50: EC50 target virus/EC50 NL4-3 wt virus; All experiments were performed in triplicate, and standard deviations were calculated from at least two separate experiments.