Table 1.
Sequences, NEMO-Binding Affinities, and Cell-Permeability of Peptides in This Worka
| peptide ID | sequence | IC50 (nM) | perpermeability (%) |
|---|---|---|---|
| 1 | RQIKIWFQNRRMKWKKGGTALDWSWLQTE | >40 | 35 |
| 2 | Tm(GWIY)Δ(FΦRRRΔ)-BBK | 3.4 ± 0.6 | 76 |
| 3 | Tm(GWIY)Δ(FΦRRRRΔ)-BBK | 1.5 ± 0.2 | 55 |
| 4 | Tm(GWIY)Δ(FΦRRRΔ)-RBK | 1.8 ± 0.3 | 71 |
| 5 | Tm(GWIY)Δ(FΦRRRΔ)-rBK | 1.3 ± 0.4 | 71 |
| 6 | Tm(GWIY)Δ(FΦRrRΔ)-BBK | 5.9 ± 0.6 | 322 |
| 7 | Tm(GWIYA)Δ(FΦRrRΔ)-BBK | 1.0 ± 0.1 | 163 |
| 8 | Tm(GWIYa)Δ(FΦRrRΔ)-BBK | 2.9 ± 0.1 | |
| 9 | Tm(AGWIY)Δ(FΦRrRΔ)-BBK | 2.2 ± 0.1 | |
| 10 | Tm(aGWIY)Δ(FΦRrRΔ)-BBK | 2.3 ± 0.3 | |
| 11 | Tm(AWIYA)Δ(FΦRrRΔ)-BBK | 1.2 ± 0.2 | |
| 12 | Tm(GAIYA)Δ(FΦRrRΔ)-BBK | 3.0 ± 0.3 | |
| 13 | Tm(GWAYA)Δ(FΦRrRΔ)-BBK | 1.7 ± 0.1 | |
| 14 | Tm(GWIAA)Δ(FΦRrRΔ)-BBK | 2.8 ± 0.3 | |
| 15 | Tm(GWIYA)Δ(AΦRrRΔ)-BBK | 1.9 ± 0.2 | |
| 16 | Tm(GWIYA)Δ(FARrRΔ)-BBK | 2.8 ± 0.2 | |
| 17 | Tm(GWIYA)Δ(FΦArRΔ)-BBK | 1.1 ± 0.3 | |
| 18 | Tm(GWIYA)Δ(FΦRaRΔ)-BBK | 2.1 ± 0.2 | |
| 19 | Tm(GWIYA)Δ(FΦRrAΔ)-BBK | 1.2 ± 0.2 | |
| 20 | Tm(GAIAA)Δ(FΦRrRΔ)-BBK | 16 ± 2 | 176 |
| 21 | Tm(GAAAA)Δ(FΦRrRΔ)-BBK | >100 | 110 |
a
Tm, trimesic acid; Δ, l-2,3-diaminopropionic acid, Φ, l-2-naphthylalanine; B, l-β-alanine; r, d-arginine. See Figure S1 for detailed structures. Cell-permeability values are relative to that of CPP1 (100%).