TABLE 2.
Therapeutic indicesa
| Name | EC50, INFV | EC50, LASVpv | EC50, Tox HEK | EC50, Tox MDCK | EC50, Tox Vero | Index (Tox HEK/LASVpv) |
|---|---|---|---|---|---|---|
| Vesicle-selected membrane-permeabilizing peptides | ||||||
| *VDVY* | 12.0 | 5.0 | >100 | ND | ND | >20 |
| *ARVA | 0.9 | 6.2 | >75 | >100 | >100 | >12 |
| *arva | 0.4 | ND | ND | ND | ND | ND |
| ARYV | 3.7 | 7.9 | ND | ND | ND | ND |
| VVRG | 6.1 | ND | ND | ND | ND | ND |
| Biologically selected antimicrobial peptides | ||||||
| *NRRV* | 8.0 | 26 | 15 | ND | ND | 0.6 |
| *ARNY* | 4.5 | 2.2 | >100 | ND | ND | >45 |
| *GRVY* | 9.1 | 2.1 | ND | ND | ND | ND |
| *RNNY* | 2.3 | 2.1 | 19 | ND | ND | 9 |
| *TNTN* | 6.1 | 1.1 | 22 | ND | ND | 20 |
| *NATT* | 0.7 | 1.2 | 43 | 60 | 41 | 36 |
| Synthetically evolved, 2nd-iteration (It1) pore-forming peptides | ||||||
| It1a | 1.6 | 1.6 | 19 | ND | ND | 12 |
| It1b | 2.3 | 1.4 | >75 | >100 | >100 | >54 |
| It1c | 1.2 | ND | ND | ND | ND | ND |
| It1d | 0.4 | 1.3 | >100 | ND | ND | >77 |
| It1e | 0.6 | 1.2 | >50 | ND | ND | >42 |
| It1f | 1.5 | 1.1 | 20 | ND | ND | 18 |
| Miscellaneous and control peptides | ||||||
| Arg9 | 6.7 | >100 | >75 | ND | ND | ND |
| Mel-L16G | ND | 28 | 21 | ND | ND | 0.8 |
| MelN4 | ND | >100 | >100 | >100 | >100 | ND |
a
Columns 2 and 3 contain EC50 values (micromolar) for inhibition of competent influenza virus (INFV) and inhibition of LASV pseudovirus, respectively. Column 3 contains EC50 values for cytotoxicity in HEK 293T/17 cells used in LASVpv assays. These values are from Fig. 1 and 2. Columns 4 and 5 contain EC50 values for cytotoxicity (Tox) for the four representative peptides against MDCK cells (used for influenza virus experiments) and Vero E6 cells (used for dengue virus, herpes simplex virus, and adenovirus experiments). Column 7 is a pseudo-therapeutic index containing the ratio of EC50 for cytotoxicity in HEK cells to EC50 for LASVpv inhibition. “ND” represents measurements that were not determined.