TABLE 1.
Binding and inhibitory activities of T-20 sequence-based lipopeptide HIV fusion inhibitorsa
| Inhibitor | No. of amino acids | CD data |
Mean IC50 ± SD (pM) for: |
|||||
|---|---|---|---|---|---|---|---|---|
| N peptide | Helix (%) | Tm (°C) | NL4-3 (X4) | JR-CSF (R5) | 89.6 (R5X4) | VSV | ||
| T-20 | 36 | N39 | 45 | 44 | 53,027.64 ± 6,155.69 | 4,468.08 ± 1,755.64 | 12,320.83 ± 1,863.22 | >1,250,000 |
| LP-40 | 28 | N39 | 60 | 50 | 20,152.66 ± 6,125.43 | 1,814.52 ± 855.93 | 20,834.58 ± 1,261.34 | >1,250,000 |
| LP-50 | 28 | N39 | 56 | 64 | 67.43 ± 15.52 | 23.38 ± 6.33 | 65.73 ± 7.71 | >1,250,000 |
| LP-51 | 28 | N39 | 53 | 71 | 24.68 ± 6.34 | 22.75 ± 5.80 | 53.91 ± 9.02 | >1,250,000 |
| LP-52 | 28 | N39 | 61 | 79 | 2.89 ± 1.54 | 8.95 ± 1.29 | 26.76 ± 7.42 | >1,250,000 |
| LP-80 | 28 | N39 | 57 | 79 | 2.66 ± 0.76 | 7.12 ± 0.28 | 13.00 ± 4.55 | >1,250,000 |
| LP-83 | 29 | N39 | 55 | 78 | 0.49 ± 0.03 | 4.54 ± 1.42 | 4.75 ± 0.83 | >1,250,000 |
| LP-86 | 29 | N39 | 51 | 77 | 0.43 ± 0.03 | 4.78 ± 0.69 | 7.24 ± 1.36 | >1,250,000 |
| LP-93 | 25 | N39 | 29 | 56 | 6.27 ± 1.26 | 6.55 ± 1.97 | 7.57 ± 0.62 | >1,250,000 |
| LP-94 | 24 | N39 | 36 | 67 | 1.75 ± 0.23 | 5.90 ± 1.80 | 15.69 ± 1.97 | >1,250,000 |
| LP-95 | 21 | N39 | 38 | 49 | 199.92 ± 32.69 | 24.36 ± 0.15 | 4,781.17 ± 699.33 | >1,250,000 |
| C34-Chol | 38 | N36 | 83 | 81 | 7.64 ± 1.76 | 50.86 ± 6.03 | 65.98 ± 7.92 | >1,250,000 |
| SP29-Chol | 29 | NAb | NA | NA | >1,250,000 | >1,250,000 | >1,250,000 | >1,250,000 |
| Cholesterol | NA | NA | NA | NA | >125,000,000 | >125,000,000 | >125,000,000 | >125,000,000 |
a
The anti-HIV assay was performed in triplicates and repeated three times.
b
NA, not applicable.