Table 1.
Name | Sequence | cyclization | Buffer Solubility (μM) | ALogP | % Inhibition of RGS4-Gαo |
YJ34 | Ac-VKCTGICE-NH2 | S-S | 80 | -2.58 | -17 ± 4 (40 μM) |
1nd | YNCQGECK-NH2 | S-S | ≥ 420 | -2.8 | 2 ± 4 |
1ad | Ac-YNCQGECK-NH2 | S-S | 123 | -2.37 | 14 ± 6 |
2nd | GTCFGTCW-NH2 | S-S | 464 | -0.37 | 19 ± 3** |
2ad | Ac-GTCFGTCW-NH2 | S-S | 30 | 0.08 | 10 ± 4 (10 μM) |
3nd | LVCKGYCQ-NH2 | S-S | ≥ 470 | -0.37 | 12 ± 2 |
3ad | Ac-LVCKGYCQ-NH2 | S-S | 427 | 0.17 | 10 ± 3 |
4nd | KVCMGGCT-NH2 | S-S | ≥ 470 | -2.02 | 4 ± 3 |
4ad | Ac-KVCMGGCT-NH2 | S-S | 459 | -2.09 | 9 ± 6 |
5nl | YWCKGLCK-NH2 | Linear | 465 | 1.46 | -1 ± 10 |
5al | Ac-YWCKGLCK-NH2 | Linear | 460 | 1.66 | -2 ± 4 |
5nd* | YWCKGLCK-NH2 | S-S | 463 | 0.48 | 80 ± 5*** |
5ad* | Ac-YWCKGLCK-NH2 | S-S | 464 | 1.04 | 37 ± 3*** |
5nm | YWCKGLCK-NH2 | S-me-S | ≥ 470 | 0.53 | 3 ± 0.1 (100 μM) |
6nd* | KHCYGFCY-NH2 | S-S | Low | 0.94 | 23 ± 15 (25 μM) * |
6ad* | Ac-KHCYGFCY-NH2 | S-S | 421 | 1.24 | 27 ± 4*** |
Solubility in buffer was determined experimentally by HPLC. ALogP calculations are from http://www.vcclab.org, [9]. Percent inhibition values (50 μM unless otherwise stated) are from Figure 1, 2C, or 3A (mean ± S.E.M., n ≥ 3) *p < 0.05, **p < 0.01, ***p < 0.001 compared to no peptide. Peptides with significant inhibition in the FCPIA are in bold. *Peptides 5 and 6 were previously reported as peptides 7 and 14, respectively in Roof et al 2008.