TABLE 1.
Inhibition constants from single-point measurement and dose-response curves compared to the values in the literature for known gp41 binders and fusion inhibitors
| Compound | Molecular mass (Da) |
Ki (μM)a
|
IC50 (μM [reference]) | |
|---|---|---|---|---|
| Single-point measurement | Dose-response curve | |||
| D10-p1-2K (oxidized) | 2,125 | 20 | NDb | 44c (12) |
| D10-p1-2K (reduced) | 2,127 | None | None | |
| ADS-J1 | 1,177 | 0.44 | 0.35 ± 0.09 | 3.28 ± 0.03c (46), 2.55 ± 0.16d (46) |
| Tannin | 1,701 | 0.39 | 0.18 ± 0.08 | ∼0.4d (34) |
| C18-Aib | 2,271 | 0.60 | 0.80 ± 0.13 | ND |
| 11{6,11} | 484.5 | 1.20 | 1.34 ± 0.19 | ∼8c (this work) |
| 11{3,5} | 490.5 | 1.15 | 1.51 ± 0.16 | ∼8c (this work) |
| Gallocatechin gallate | 458.4 | None | 7.55 ± 0.37c (35), 4.32 ± 0.94c (35) | |
| Epigallocatechin gallate | 458.4 | None | Nonec (35), 19.91 ± 1.27d (35) | |
a
Kis are from this work. Equation 8 was used to calculate the Kis from the dose-response curve, and the data represent the means and standard deviations from three independent experiments.
b
ND, not available at a concentration high enough to determine the dose-response curve.
c
Syncytium inhibition in cell culture.
d
Six-helix bundle formation assay (33).