TABLE 1.
Anti-HIV activities of enfuvirtide-CP conjugates in virus infection (CEM cells infected with HIV-1 IIIB/LAI or HIV-2 ROD) and cell-cell fusion (HUT-78/HIV-1 IIIB/LAI cocultured with SupT1 cells) assays
| Compound | No. of ethylene glycol units (PEG) | Length (Å) of PEG linker | EC50 (nM)a |
||
|---|---|---|---|---|---|
| CEM cells infected with: |
HUT-78/HIV-1 IIIB/LAI cocultured with SupT1 | ||||
| HIV-1 IIIB/LAI | HIV-2 ROD | ||||
| EP40114 | 4 | 25 | 13 ± 12 | 280 ± 110 | 65 ± 4 |
| EP40111 | 12 | 54 | 6 ± 3 | 670 ± 67 | 72 ± 15 |
| EP40112 | 28 | 106 | 18 ± 7 | 630 ± 64 | 61 ± 0 |
| EP40113 | 70 | 247 | 15 ± 9 | 990 ± 730 | 51 ± 15 |
| Enfuvirtide | 3 ± 1 | 360 ± 46 | 275 ± 150 | ||
a
The results represent the means ± SDs of three independent experiments, each of which was performed in triplicate.