Table 2.
Cellular uptake, endosomal escape and viability results for selected peptides
| Peptide | Focus | Description | # of COS-1 cells (n) |
% QD uptake (n) |
% Endosomal escape of total cells (n) |
% Escape in cells with uptake |
Overall uptake/escape |
Cellular viability (%)1 |
|---|---|---|---|---|---|---|---|---|
| JB747 | Pron-linker | Pro9→ Aib9 | 78 | 100% (78) | 58% (78) | 58% | high/moderate | 98 ± 1% |
| JB865 | Pron-linker | Pro9→ Pro12 | 82 | 80% (66) | 85% (56) | 68% | high/moderate | 81 ± 12% |
| JB864 | Pron-linker | Pro9→ Pro15 | 99 | 82% (81) | 70% (69) | 85% | high/high | 92 ±17% |
| JB869 | Charge | VKIKKP9→ amphipathic-[VRLP3]3 | 315 | 80% (253) | 44% (139) | 55% | high/moderate | 90 ±9% |
| JB641 | Fatty acid | Palmitoyl→ C8 group | 165 | 50% (83) | 44% (73) | 88% | moderate/high | 105 ±13% |
| JB729 | Fatty acid | Palmitoyl→ C8F17 | 80 | 64% (51) | 54% (43) | 84% | high/high | 93 ±12% |
| SI-09160 | Fatty acid | Palmitoyl→ cholesterol | 102 | 44% (45) | 42% (43) | 96% | moderate/high | 101 ±3% |
| JB858 | Fatty acid | Dap→Dab | ---- | ---- | >90% membrane localized | ---- | ---- | 103 ±3% |
| JB872 | Fatty acid | Palmitoyl→ farnesyl | 101 | 99% (100) | 78% (79) | 79% | high/high | 76 ±7% |
| JB860 | Order | Reversedsequence2 | 164 | 30% (50) | 18% (30) | 60% | moderate/moderate | 58 ±5% |
| IB829-JB26 | Control | JB577 analog (chemoligation) | 60 | 74% (44) | 71% (31) | 70% | high/high | 101 ±5% |
| JB434 | Control | Arg9 cell penetrating peptide | 573 | 82% (469) | 0 (0) | 0 % | high/ none | 106 ±8% |
| JB728 | Control | Rhodamine-labeledJB577 | 84 | 81% (68) | 76% (63) | 93% | high/high | 77 ±7% |
| JB5882 | Control | No His6/ Lys for EDC coupling | 64 | 94% (60) | 80% (51) | 85% | high/high | ND |
| JB719 | Control | Chariot peptide | 180 | 53% (96) | 6% (11) | 11% | moderate / low | 98 ±4% |
| Cell line | Cell type | # of cells (n) | ||||||
| JB577 | COS-1 | African Green Monkey kidney | 76 | 92% (70) | 69% (52) | 77% | high/high | 98 ±4% |
| JB577 | Hela | human cervical carcinoma | 163 | 90% (147) | 77% (126) | 86% | high/high | 98 ±1% |
| JB577 | HEK 293 | human embryonic kidney | 130 | 69% (89) | 59% (77) | 86% | high/high | 87 ±5% |
| JB577 | A549 | human adenocarcinomic alveolar basal epithelial | 69 | 87% (61) | 81% (56) | 92% | high/high | 96 ±3% |
| JB577 | PC12 | rat adrenal pheochromocytoma | 61 | 75% (46) | 68% (42) | 91% | high/high | 97 ±10% |
| JB577 | Fibroblasts | Primary human dermal fibroblasts | 123 | 90% (111) | 29% (36) | 32% | high/moderate | 92 ±6% |
1
Cell viability tested with exposure to 100 nM of 75 peptide/QD. ND – not determined.
2
Tested with eBiosciences NCs. A full listing of all results can be found in the SI.