Table 1.
Protein solubility, denaturation temperatures and in vitro bioactivity of scTRAIL variants.
| Molecule | Solubility | Tm (°C) | EC50 (pM) of bioactivity1 |
|---|---|---|---|
| sTRAIL | yes | 46 | |
| scTRAIL-95L8 | yes | 47 | 219 ± 17 |
| scTRAIL-FLVGGGGSGGGSVRERGPQRVA | yes | 46 | 199 ± 110 |
| scTRAIL-FLVGGGGSVRERGPQRVA | yes | 47 | 135 ± 35 |
| scTRAIL-FLVGGGGSGGGSQRVA | yes | 49 | 123 ± 21 |
| scTRAIL-FLVGGGGSQRVA | yes | 50 | 77 ± 16 |
| scTRAIL-FLVGGGGPQRVA | yes | 52 | 65 ± 28 |
| scTRAIL-FLVGGGPQRVA | yes | 52 | 56 ± 13 |
| scTRAIL-FLVGGPQRVA | yes | 53 | 69 ± 9 |
| scTRAIL-FLVGGQRVA | yes | nd | nd |
| scTRAIL-FLVGGRVA | yes | 54 | 39 ± 3 * |
| scTRAIL-FLVGGVA | yes | 57 | 41 ± 6 * |
| scTRAIL-FLVGGGA | no | — | — |
| scTRAIL-FGVGGGA | no | — | — |
| scTRAIL-FLGGGGA | no | — | — |
| scTRAIL-FLGGGA | no | — | — |
| scTRAIL-FLVGGLA | no | — | — |
| scTRAIL-FLVGGMA | no | — | — |
| scTRAIL-FVVGGLA | no | — | — |
| scTRAIL-FLVGGIA | yes | 54 | 47 ± 19 * |
| scTRAIL-FLVGGAA | yes | 53.5 | 96 ± 43 |
| scTRAIL-FAVGGAA | yes | 53 | 129 ± 34 |
| scTRAIL-FLVSGIA | yes | 51.5 | 261 ± 68 |
| scTRAIL-FIVGGIA | yes | 52 | 45 ± 0.6 * |
| scTRAIL-FIVSGIA | yes | 51 | 229 ± 52 |
| scTRAIL-FAVGGIA | yes | 53 | 53 ± 11 * |
| scTRAIL-FAVSGIA | yes | 50.5 | 274 ± 55 |
| scTRAIL-FAVSGAA | yes | 54 | 80 ± 8 * |
1
analyzed on Colo 205 cells in presence of 250 ng/ml bortezomib, mean ± SD (n = 3).
*
percentage of oligomers >15% of the total protein.