Table 1.
K11777 inhibits entry of a variety of enveloped viruses.
| Pseudoviruses | Family | Genome type | Cells | IC50 (nM)a |
|---|---|---|---|---|
| SARS-CoV | Coronaviridae | ssRNA(+) | 293T-ACE2 | 0.68 ± 0.09 |
| HCoV-229E | Coronaviridae | ssRNA(+) | 293T-CD13 | 1.48 ± 0.13 |
| NL63 | Coronaviridae | ssRNA(+) | 293T-ACE2 | 6.78 ± 0.24 |
| MERS-CoV | Coronaviridae | ssRNA(+) | Vero | 46.12 ± 6.63 |
| Zaire ebolavirus (EBOV) | Filoviridae | ssRNA(−) | 293T | 0.87 ± 0.06 |
| Sudan ebolavirus (SUDV) | Filoviridae | ssRNA(−) | 293T | 1.14 ± 0.07 |
| Tai Forest ebolavirus (TAFV) | Filoviridae | ssRNA(−) | 293T | 2.26 ± 0.10 |
| Reston ebolavirus (RESTV) | Filoviridae | ssRNA(−) | 293T | 3.37 ± 0.29 |
| Bundibugyo ebolavirus (BEBOV) | Filoviridae | ssRNA(−) | 293T | 5.91 ± 0.50 |
| Marburg (MARV) | Filoviridae | ssRNA(−) | 293T | 1.90 ± 0.16 |
| Nipah | Paramyxoviridae | ssRNA(−) | 293T | 0.42 ± 0.03 |
| Chikungunya | Togaviridae | ssRNA(+) | 293T | >100 |
| Vesicular stomatitis | Rhabdoviridae | ssRNA(−) | 293T | >100 |
| Amphotropic murine leukemia | Retroviridae | ssRNA(−)RT | 293T | >100 |
| Xenotropic murine leukemia | Retroviridae | ssRNA(−)RT | 293T | >100 |
| Lassa | Arenaviridae | ssRNA(−) | 293T | >100 |
| Junin | Arenaviridae | ssRNA(−) | Vero | >100 |
| HCV (H77 envelope) genotype 1a | Flaviviridae | ssRNA(+) | Huh7.5 | >100 |
IC50 (inhibitory concentration) values are the concentrations required to inhibit the infectivity of the pseudotyped viruses on cells by 50%, which were determined from dose response curves. All envelopes apart from Nipah and Junin were used to make HIV-based pseudotypes. Target cells (293T, 293T expressing ACE2 or CD13, or Vero cells) were then pretreated with serial dilutions of K11777 and exposed to virus. VSV-based pseudotypes were made by transfecting cells with Nipah F and G plasmids, or Junin envelope, and transducing with VSVΔG(GFP)-G. Progeny virus was then collected and titered on target cells. A non-linear regression analysis based on the Sigmoidal dose response equation was applied to the percent inhibition and concentration data. Data is shown as means of triplicate measurements ± standard deviation. Values are representative of at least two independent experiments.