Table 1 Solubility, bioactivity and percent helicity of glucagon analogs
Peptide | Amino acid | Solubility in PBS pH 7.4 (mg/mL) | EC50 (pM) GCGR ± SD | EC50 (nM) GLP-1Ra ± SD | % Helicity |
|---|---|---|---|---|---|
1 | d-His1 | 0.26 | 46.4 ± 5.6 | 26.3 ± 6.2 |  |
2 | d-Ser2 | 0.24 | 16.7 ± 3.4 | 5.5 ± 1.7 |  |
3 | d-Gln3 | 0.32 | 33.3 ± 8.9 | 29.1 ± 7.7 |  |
4 | G4(native) | 0.21 | 28.7 ± 9.1 | 1.1 ± 0.4 | 26.1 |
5 | d-Thr5 | 0.18 |  > 1000 | >1000 |  |
6 | d-Phe6 | 0.30 |  > 1000 | >1000 |  |
7 | d-Thr7 | 0.47 | 136 ± 43 | >1000 |  |
8 | d-Ser8 | 1.51 |  > 1000 | >1000 | 26.4 |
9 | d-Asp9 | 0.26 | 280 ± 49 | 608 ± 142 |  |
10 | d-Tyr10 | 1.22 | 35.6 ± 10.4 | 71.0 ± 28.0 |  |
11 | d-Ser11 | 0.66 | 57.9 ± 14.9 | 27.2 ± 9.5 |  |
12 | d-Lys12 | 1.76 | 34.7 ± 9.5 | 101 ± 47 | 19.4 |
13 | d-Tyr13 | 1.68 | 216 ± 67 | 103 ± 14 | 20.2 |
14 | d-Leu14 | 0.87 | 248 ± 92 | 7.0 ± 2.2 | 18.4 |
15 | d-Asp15 | 1.53 | 78.7 ± 22.1 | 10.2 ± 4.1 | 17.5 |
16 | d-Ser16 | 2.06 | 31.4 ± 10.3 | 4.9 ± 1.3 | 18.2 |
17 | d-Arg17 | 4.52 | 20.3 ± 9.4 | 11.7 ± 3.1 | 23.5 |
18 | d-Arg18 | 2.14 | 49.1 ± 9.9 | 0.5 ± 0.6 | 22 |
19 | d-Ala19 | 2.01 |  > 1000 | 5.8 ± 2.8 | 19.7 |
20 | d-Gln20 | 1.03 | 37.5 ± 12.4 | 8.6 ± 2.4 | 19.6 |
21 | d-Asp21 | 1.88 | 26.6 ± 11.2 | 11.1 ± 2.8 | 17.6 |
22 | d-Phe22 | 3.24 | 150 ± 70 | >1000 | 17.7 |
23 | d-Val23 | 4.00 | 66.3 ± 26.9 | 10.5 ± 4.9 | 14.5 |
24 | d-Gln24 | 1.73 | 22.1 ± 9.2 | 5.0 ± 2.6 |  |
25 | d-Trp25 | 3.17 | 317 ± 81 | 15.3 ± 7.8 |  |
26 | d-Leu26 | 2.39 |  > 1000 | 458 ± 111 |  |
27 | d-Met27 | 2.93 | 139 ± 84 | 5.9 ± 1.8 |  |
28 | d-Asn28 | 0.52 | 26.6 ± 11.5 | 0.5 ± 0.2 |  |
29 | d-Thr29 | 0.54 | 22.4 ± 10.4 | 0.5 ± 0.2 |  |
