Table 1 Antiviral activity (IC 50 ) and cytotoxicity (CC 50 ) of i & i + 7 stapled peptides against HIV-1 IIIB in MT-2 cells
From: Dual-acting stapled peptides target both HIV-1 entry and assembly
Peptide | Sequence | Net charge | IC50(μM ± SD) in MT-2 | CC50(μM ± SD) in MT-2 | SI |
|---|---|---|---|---|---|
CAI | ITFEDLLDYYGP-amide (Linear reference) | -2 | >100 | >100 | >1.0 |
NYAD-401 | Ac-IRQGPKEPFRDYVDR-amide (Linear control for NMR) | 1 | >100 | >100 | >1.0 |
NYAD-41 | Ac-ISFDELLDYYGESGS (linear control based on NYAD-36) | -5 | >100 | >100 | >1.0 |
NYAD-33 | Ac-ISF-R8-EWLQYY-S5-R-amide | 0 | 3.37 ± 0.06 | 9.2 ± 0.26 | 2.7 |
NYAD-36 | Ac-ISF-R8-ELLDYY-S5-ESGS-amide | -4 | 1.5 ± 0.17 | >189.4 | >126 |
NYAD-43 | Ac-ISF-R8-ELEDYY-S5-ESGS | -5 | >53.34 | >106.6 | >2.0 |
NYAD-44 | Ac-ISF-R8-ELLDYY-S5-ESGSKKK-amide | 0 | 11.7 ± 1 | 17.2 ± 1.4 | 1.5 |
NYAD-46 | Ac-ISF-R8-QLLDYY-S5-QSGSK-amide | 0 | 5.5 ± 1 | 10.6 ± 0.6 | 1.9 |
NYAD-55 | Ac-ISF-R8-ELLDYY-S5-EKSGSKD-amide | -2 | >89.7 | >89.7 | >1.0 |
NYAD-56 | Ac-ISF-R8-ELLRYY-S5-R-amide | 1 | 4.8 ± 0.9 | 16.4 ± 1.2 | 3.4 |
NYAD-57 | ISF-R8-ELLNYY-S5-ESGS-amide | -1 | 8.7 ± 0.7 | 39.6 ± 4.4 | 4.5 |
NYAD-58 | IRF-R8-QLLNYY-S5-ESGS-amide | 1 | 6.9 ± 0.06 | 14.9 ± 1 | 2.1 |
NYAD-61 | Ac-RSF-R8-RLLDYY-S5-ESGS-amide | 0 | 10.2 ± 1.1 | 31.7 ± 1.4 | 3.1 |
NYAD-62 | Ac-RRF-R8-ELLDYY-S5-ESGS-amide | -1 | 8 ± 0.3 | 15.4 ± 0.2 | 1.9 |
NYAD-63 | Ac-R-R8-FAELLD-S5-YGESGS-amide | -2 | 57.1 ± 3.2 | >113 | >2.0 |
NYAD-64 | Ac-SK-R8-ELLDYY-S5-ESGS-amide | -2 | >109 | >109 | >1.0 |
NYAD-65 | Ac-RSFE-R8-LLDYYG-S5-SGS-amide | -1 | >116 | >116 | >1.0 |
NYAD-66 | Ac-ISF-R8-ELLDYY-S5-ED-amide | -4 | 3.94 ± 0.32 | >115 (0%)a | >29.1 |
NYAD-67 | Ac-ISF-R8-EWLQAY-S5-EDE-amide | -4 | 3.88 ± 0.3 | >107.4 (0%)a | >27.7 |