Table 2.
Sequences and Biological Activity of B4 Analogs
| Peptide | Peptide Sequencea,b | HTRF IC50 (μM)c | CellTiter-Glo EC50 (μM)c |
|---|---|---|---|
| B3-4 | ΦOSQΦΠ-K-fArR-J-BBK-NH2 | 4.4 ± 1.3 | 22 ± 4 |
| B4 | ΦSQΦΠ-K-fArR-J-ΣrΨa-K-NH2 | 1.7 ± 0.3 | 14 ± 3 |
| B4-1 | ΦSNΦΠ-K-fArR-J-ΣrΨa-K-NH2 | 0.89 ± 0.26 | 7.2 ± 0.8 |
| B4-2 | ΦSNΦΠ-K-fArR-J-ΣrΨa-NH2 | 0.70 ± 0.24 | 6.0 ± 1.6 |
| B4-3 | ΦSNΦΠ-K-fArR-J-ΣrΨ-NH2 | 0.55 ± 0.07 | 15 ± 2 |
| B4-4 | ΦSNΦΠ-K-fArR-J-Σr-NH2 | 0.70 ± 0.10 | 16 ± 4 |
| B4-5 | ΦSNΦΠ-K-fArR-J-Σ-NH2 | 1.3 ± 0.5 | 17 ± 2 |
| B4-6 | ΦSNΦΠ-K-fArR-J-ΣrFa-NH2 | 0.51 ± 0.01 | 3.2 ± 1.5 |
| B4-7 | ΦSNΦΠ-K-fArR-J-ΣrYa-NH2 | 1.1 ± 0.1 | 19 ± 10 |
| B4-8 | ΦSNΦΠ-K-fArR-J-ΣrRa-NH2 | 1.0 ± 0.1 | 20 ± 1 |
| B4-9 | ΦSNΦΠ-K-fArR-J-Σrra-NH2 | 0.70 ± 0.0 | 10 ± 8 |
| B4-10 | ΦSNΦΠ-K-fArR-J-ΣrZa-NH2 | 0.77 ± 0.03 | 9.2 ± 1.1 |
| B4-11 | ΦSNΦΠ-K-fArR-J-ΣrWa-NH2 | 2.2 ± 0.8 | NA |
| B4-12 | ΦSNΦΠ-K-fArR-J-Σrϑa-NH2 | 0.94 ± 0.33 | 11 ± 4 |
| B4-13 | ΦSNΦΠ-K-fArR-J-ΣrΠa-NH2 | 0.76 ± 0.24 | 4.5 ± 3.0 |
| B4-14 | ΦSNΦΠ-K-fArR-J-ΣrΓa-NH2 | 0.50 ± 0.04 | 4.4 ± 0.3 |
| B4-15 | ΦSNΦΠ-K-fArR-J-ΣrΛa-NH2 | 0.33 ± 0.01 | 9.0 ± 0.7 |
| B4-16 | ΦSNΦΠ-K-fArR-J-ΣrPa-NH2 | 0.41 ± 0.06 | 6.6 ± 0.4 |
| B4-17 | ΦSNΦΠ-K-fArR-J-KrΨa-NH2 | 1.1 ± 0.4 | 4.4 ± 1.5 |
| B4-18 | ΦSNΦΠ-K-fArR-J- ΘrΨa-NH2 | 1.7 ± 0.2 | NA |
| B4-19 | ΦSNΦΠ-K-fArR-J- ΞrΨa-NH2 | 0.87 ± 0.05 | 12 ± 8 |
| B4-20 | ΦSNΦΠ-K-fArR-J-NrΨa-NH2 | 0.28 ± 0.06 | 8.4 ± 5.2 |
| B4-21 | ΦSNΦΠ-K-fArR-J-QrΨa-NH2 | 0.23 ± 0.02 | 7.5 ± 4.0 |
| B4-22 | ΦSNΦΠ-K-FArR-J-ΣrFa-NH2 | 0.65 ± 0.37 | 21 ± 1 |
| B4-23 | ΦSNΦΠ-K-farR-J-ΣrFa-NH2 | 0.52 ± 0.01 | 16 ± 8 |
| B4-24 | ΦSNΦΠ-K-fζrR-J-ΣrFa-NH2 | 0.61 ± 0.09 | 7.2 ± 2.7 |
| B4-25 | ΦSNΦΠ-K-fLrR-J-ΣrFa-NH2 | 0.79 ± 0.02 | 4.8 ± 1.1 |
| B4-26 | ΦSNΦΠ-K-fSrR-J-ΣrFa-NH2 | 0.56 ± 0.17 | 11 ± 8 |
| B4-27 | ΦSNΦΠ-K-fQrR-J-ΣrFa-NH2 | 0.69 ± 0.11 | 2.1 ± 0.1 |
| B4-28 | ΦSNΦΠ-K-fHrR-J-ΣrFa-NH2 | 1.0 ± 0.2 | 8.2 ± 4.8 |
| B4-29 | ΦSNΦΠ-K-fNrR-J-ΣrFa-NH2 | 1.2 ± 0.4 | 14 ± 3 |
| B4-30 | ΦSNΦΠ-K-fΣrR-J-ΣrFa-NH2 | 0.83 ± 0.20 | 6.4 ± 0.8 |
| B4-31 | ΩSNΦΠ-K-fQrR-J-ΣrFa-NH2 | 0.64 ± 0.09 | 5.2 ± 1.1 |
| B4-32 | ΦSNΩΠ-K-fQrR-J-ΣrFa-NH2 | 0.71 ± 0.08 | 4.9 ± 1.2 |
| B4-33 | ΦNNΦΠ-K-fQrR-J-ΣrFa-NH2 | 0.86 ± 0.12 | 17 ± 5 |
| B4-34 | ΦTNΦΠ-K-fQrR-J-ΣrFa-NH2 | 1.3 ± 0.3 | 23 ± 17 |
| B4-35 | ΦςNΦΠ-K-fQrR-J-ΣrFa-NH2 | 1.2 ± 0.2 | 5.9 ± 0.5 |
| B4-36 | ΦSAΦΠ-K-fQrR-J-ΣrFa-NH2 | 1.0 ± 0.2 | NA |
| B4-37 | ΦSSΦΠ-K-fQrR-J-ΣrFa-NH2 | 0.75 ± 0.18 | 17 ± 6 |
| B4-38 | ΦSNΦΠ-K-ψQrR-J-ΣrFa-NH2 | 0.55 ± 0.03 | 15 ± 5 |
| B4-39 | ΦSNΦΠ-K- λQrR -J-ΣrFa-NH2 | 0.71 ± 0.01 | 23 ± 7 |
| B4-40 | ΦSNΦΠ-K-fQrR-J-Σrfa-NH2 | 0.56 ± 0.24 | 5.0 ± 0.4 |
| B4-41 | ΦSNΦΠ-K-fQrR-J-ΣrXa-NH2 | 0.71 ± 0.09 | 7.4 ± 0.3 |
| B4-42 | ΦSNΦΠ-K-fQrR-J-ΣrFv-NH2 | 0.61 ± 0.17 | 7.1 ± 1.9 |
| B4-43 | ΦSNΦΠ-K-fQrR-J-ΣrFt-NH2 | 0.57 ± 0.10 | 2.6 ± 1.2 |
| B4-44 | ΦSNΦΠ-K-fQrR-J-ΣrFs-NH2 | 0.75 ± 0.03 | 5.3 ± 1.4 |
| B4-45 | ΦSNΦΠ-K-fQrR-J-ΣrFn-NH2 | 2.2 ± 1.7 | 3.1 ± 0.8 |
| B4-46 | ΦSNΦΠ-K-fQrR-J-ΣrFB-NH2 | 1.1 ± 0.4 | 12 ± 3 |
L-AA’s are shown as the capitalized one letter code while D-AA’s are lowercase.
J = L-2,3-diaminopropionic acid; Π = L-phenylglycine; Φ = D-2-napthylalanine; Σ = L-ornithine; Γ = L-3,4-difluorophenylalanine; ϧ = 3-cyclohexyl-L-alanine; Λ = L-3-chlorophenylalanine; λ = D-3-chlorophenylalanine; P = 3-(2-pyridyl)-L-alanine; Ω = 3-(3-benzo(b)thienyl)-D-alanine; Ψ = L-4-fluorophenylalanine; ψ = D-4-fluorophenylalanine; Z = L-homophenylalanine; Θ = L-2,3-dia-minopropionic acid; Ξ = L-2,4-diaminobutyric acid; ζ = L-α-aminobutyric acid; ς = L-homoserine; B = β-alanine; X = L-β-homo-phenylalanine.
Values reported represent the mean ± SD of 3 or more independent experiments. NA, no significant activity; NT, not tested.