TABLE 1.
Antiviral activity of HIV-1 gp41-derived peptides against gp120 and/or gp41 recombinant virusesa
| Virus or substitution | EC50 (nM)
|
|||
|---|---|---|---|---|
| ddC | T-20 | N36 | C34 | |
| HIV-1WTb | 264 | 12 | 51 | 2.1 |
| ΔFNSTWc | 98 (0.4) | 18 (1.5) | 50 (1.0) | 9.5 (4.6) |
| A30V | 205 (0.8) | 6.3 (0.5) | 38 (0.7) | 7.0 (3.4) |
| D36G | 173 (0.7) | 0.92 (0.1) | 90 (1.7) | 1.6 (0.8) |
| D36Se | 166 (0.6) | 6.6 (0.6) | 89 (1.7) | 3.7 (0.6) |
| I37T | 284 (1.1) | 156 (13) | 40 (0.8) | 23 (11) |
| I37K | 326 (1.2) | 2,482 (212) | 99 (1.9) | 27 (13) |
| V38Me | 223 (0.8) | 305 (26) | 94 (1.8) | 31 (15) |
| Q39Hd | 330 (1.3) | 1.9 (0.2) | 165 (3.2) | 5.3 (2.6) |
| N126Kd | 380 (1.4) | 23 (1.9) | 137 (2.7) | 14 (6.8) |
| L204I | 247 (0.9) | 13 (1.1) | 105 (2.0) | 4.4 (2.1) |
| D36S/V38Me | 294 (1.1) | 60 (5.1) | 46 (0.9) | 16 (7.7) |
| I37T/N126K | 292 (1.1) | 158 (14) | 54 (1.1) | 22 (11) |
| I37K/N126K | 309 (1.2) | 1,570 (134) | 51 (1.0) | 57 (28) |
| A30V/I37K/N126K | 409 (1.5) | 198 (17) | 119 (2.3) | 22 (10) |
| D36G/I37K/N126K | 329 (1.2) | 269 (23) | 156 (3.0) | 148 (72) |
| D36G/I37K/N126K/L204Id | 209 (0.8) | 117 (10) | 41 (1.2) | 112 (54) |
| ΔFNSTW/D36G/I37K/N126K/L204Id | 213 (0.8) | 746 (64) | 54 (1.0) | 171 (83) |
a
Anti-HIV activity was determined with the MAGI assay. The data shown are mean values obtained from the results of at least three independent experiments, and resistance (n-fold) in EC50 for recombinant viruses compared to HIV-1WT is shown in parentheses.
b
HIV-1NL4-3 was used was a wild-type virus.
c
ΔFNSTW is the deletion of 5 amino acids at positions 364 to 368 in the gp120 V4 region of HIV-1NL4-3.
d
Mutant viruses observed during induction of C34 resistance variants in vitro (Fig. 1B).
e
D36S/V38M has been reported for T-20-resistant HIV-1 variants (26).