Table 1.
Inhibition of VGLUT by Tetrapeptides1
| X1 | X2 | X3 | X4 |
3H-lGlu uptake
(% of control)2 |
|---|---|---|---|---|
| Library 1 | ||||
| AA3 | AA | E | W | |
| Q | AA | E | W | 56 ± 1% |
| Q | W | E | W | 66 ± 4% |
| Q | I | E | W | 38 ± 5% |
| D-Q | D-I | L -E | D-W | 35 ± 3% |
| L-Q | D-I | L-E | D-W | 28 ± 3% |
| Library 2 | ||||
| AA | AA | E | F | |
| N | AA | E | F | 63 ±17% |
| W | AA | E | F | 36 ± 2% |
| W | N | E | F | 13 ± 3% |
| D-W | L-N | D-E | D-F | 41 ± 1% |
| Other | ||||
| Congo Red (2 μM) | 31 ± 2% | |||
1
Tetrapeptides tested as racemic mixtures at 2mM.
2
Control rate for 3H-L-glutamate uptake was 1847±130(n=17) pmol/min/mg protein.
3
AA = 19 different amino acids.