Table 3.
IC50 Values (μM) against Multiple HIV-1 Strains and Cytotoxicity of the New-Generation Peptidesa
| Peptide | Sequence | R5b | R5/X4 | X4 | LC50c (μM) | TId (μM) | ||||
|---|---|---|---|---|---|---|---|---|---|---|
| YU2 | BaL26 | 89.6 | HxB2 | NL4–3 | ||||||
| 181 | 184 | 189 | ||||||||
| 2Ce | CSSHFPYSQYQFWK | 28.0 ±7 | 65.0 ±3.0 | NAf | NDf | 53.0 ±2 | 190 | >125–250 | ||
| 16–2 | . . . . . .F. . . . . . . | 5.1 ±0.6 | ND | NA | 167±132 | 44.4 ± 13.3 | 80 | >63–250 | ||
| 18–2 | . . . Y . . F. . . . . . . | 1.9 ±0.6 | 27.4 ±5.6 | 132 ±111 | 72 ±89 | 11.8 ± 2.6 | 80 | >63–125 | ||
| 20–2 | . . .Y. .F. . . .W. . | 0.42 ±0.1 | 14.1 ±2.9 | 13 ± 1.9 | >50 | 7.6 ± 1.3 | 330 | >250 | ||
| 20–5 | . . .YY.F. . . .W. . | 0.72 ± 0.2 | 9.5 ±2.0 | 7.2 ± 1.0 | >100 | 5.9 ±0.8 | ND | ND | ||
| 30–2 | . . .Y. .W. . . .W. . | 0.96 ±0.1 | 6.4 ±0.9 | 0.6 ±0.2 | 21.3 ±5.2 | 3.8 ±0.4 | Non-toxicf | >500 | ||
| 40–2 | Y. .Y. .F. . . .W. . | 0.26 ±0.1 | 21.2 ±5.5 | 26.9 ±6.1 | 40.3 ± 13.4 | 17.1 ±3.8 | 550 | >250 | ||
| 50–2 | Y. .Y. .W. . . .W. . | 2.1 ±0.4 | ND | ND | ND | ND | ND | ND | ||
| 60–2 | S. .Y. .W. . . .W. . | 2.7 ±0.5 | ND | ND | ND | ND | ND | ND | ||
a
Data for select peptides. See Table S2 for additional peptides studied.
b
Virus tropism and HIV strain.
c
Effects on host cell line TZM-bl. Standard deviations averaged 20%.
d
Toxicity index. Ratio of cytotoxicity to neutralization IC50 values.
e
Data from ref 5.
f
Either peptides noted were not active, NA, at 500 μM; the IC50 values were not determined, ND, due to low potency and/or toxicity; or the peptides were nontoxic at 500 μM.