Table 3. Inhibitory effects and IC50 of peptide binding rhNRP-1 (chemiluminescence detection).
Compound | AA2–AA3 fragment | 100 μM | 50 μM | Inhibition of NRP-1/VEGF-A165 binding [%] |
IC50 [μM] | ||||
25 μM | 10 μM | 5 μM | 2.5 μM | 1 μM | |||||
1 | n/a | 58.2 ± 1.2 | 43.8 ± 1.3 | 35.0 ± 2.6 | 30.8 ± 3.8 | — | — | — | 84.1 ± 2.9 a |
2 | Pro–Pro | 77.0 ± 1.0 | 67.9 ± 1.4 | 54.1 ± 1.0 | 37.1 ± 1.0 | — | — | — | 20.9 ± 0.3 b |
3 | Dab–Pro | 79.8 ± 0.8 | 76.6 ± 0.9 | 70.4 ± 0.5 | 58.6 ± 1.4 | 43.7 ± 0.7 | 31.4 ± 0.5 | 13.8 ± 0.3 | 8.9 ± 0.8 c |
4 | Pro–Ala | 70.7 ± 0.5 | 62.1 ± 0.3 | 50.3 ± 1.0 | 35.5 ± 2.0 | — | — | — | 23.4 ± 7.9 d |
alog IC50 = –3.08 ± 1.18.
blog IC50 = –4.68 ± 0.04.
clog IC50 = –5.05 ± 0.13.
dlog IC50 = –4.63 ± 0.12; R2 ranged between 0.96–0.99. Results are presented as the mean ± SEM. n/a means not applicable.