Table 4. Antiviral activity of GRL-121 and −142 against HIV-1 variants carrying single amino acid substitution in PR region.
| Mean IC50 ± SD (nM) | ||||
|---|---|---|---|---|
| Infectious clone | Amino acid substitution in PR | DRV | GRL-121 | GRL-142 |
| cHIVNL4-3WT | none | 3.2 ± 0.7 | (2.6 ± 0.5)×10−1 | (1.9 ± 1.7)×10−2 |
| cHIVNL4-3L10F | L10F | 3.3 ± 1.0 | (3.4 ± 1)×10−2 | (2.9 ± 1.2)×10−3 |
| cHIVNL4-3L24I | L24I | 3.1 ± 0.6 | (1.2 ± 1.1)×10−4 | (2.9 ± 1.6)×10−5 |
| cHIVNL4-3D30N | D30N | 4.7 ± 1.0 | (2.0 ± 3.0)×10−2 | (4.7 ± 2.0)×10−3 |
| cHIVNL4-3V32I | V32I | (3.0 ± 1.0)×10−1 | (8.0 ± 10.5)×10−5 | (1.2 ± 1.6)×10−8 |
| cHIVNL4-3L33F | L33F | 2.8 ± 1.1 | (3.5 ± 2.5)×10−1 | (1.8 ± 1.0)×10−2 |
| cHIVNL4-3M46I | M46I | 3.3 ± 0.2 | (2.2 ± 0.8)×10−2 | (2.2 ± 1.5)×10−3 |
| cHIVNL4-3I47V | I47V | 3.0 ± 0.6 | (3.2 ± 0.7)×10−2 | (1.2 ± 0.9)×10−3 |
| cHIVNL4-3G48V | G48V | (2.9 ± 0.6)×10−1 | (6.0 ± 1.1)×10−5 | (3.6 ± 6.0)×10−8 |
| cHIVNL4-3I50V | I50V | 2.7 ± 1.0 | (1.5 ± 2.4)×10−5 | (9.3 ± 15.1)×10−8 |
| cHIVNL4-3I54M | I54M | 3.2 ± 0.8 | (3.1 ± 3.4)×10−3 | (1.9 ± 2.3)×10−4 |
| cHIVNL4-3I54L | I54L | 3.3 ± 0.2 | (3.2 ± 0.3)×10−1 | (3.1 ± 2.6)×10−3 |
| cHIVNL4-3I54V | I54V | 3.0 ± 0.4 | (3.2 ± 1)×10−4 | (2.7 ± 1.1)×10−5 |
| cHIVNL4-3L63P | L63P | 2.3 ± 0.7 | (2.5 ± 2.6)×10−2 | (5.9 ± 5.8)×10−3 |
| cHIVNL4-3V82A | V82A | 2.9 ± 0.1 | (5.0 ± 2.0)×10−3 | (3.6 ± 10)×10−4 |
| cHIVNL4-3V82I | V82I | 4.0 ± 1.1 | (1.8 ± 1.8)×10−1 | (2.0 ± 0.5)×10−2 |
| cHIVNL4-3V82T | V82T | (5.7 ± 2.0)×10−1 | (1.5 ± 1.0)×10−5 | (3.1 ± 4.0)×10−6 |
| cHIVNL4-3I84V | I84V | 2.7 ± 1.1 | (1.7 ± 0.9)×10−3 | (3.9 ± 1.6)×10−5 |
| cHIVNL4-3L90M | L90M | 4.2 ± 0.5 | (3.2 ± 2.7)×10−2 | (5.8 ± 0.9)×10−4 |
All assays were conducted in triplicate, and the data shown represent mean values (±1 standard deviation) derived from the results of at least three independent experiments.