Table 1.
Screening of GAIs
| GAI | Sequence | Potency |
Cytotoxicity |
Side effect |
|---|---|---|---|---|
| Aggregation inhibitory activity (%) | Cell viability (%) | Effect on GAPDH activity (%) | ||
| 1 | SNASCTTNAL | 53.1 2.87 | 100 2.43 | 104 2.73 |
| 2 | SLKIISNASCTTNALAPLAK | 70.8 1.89 | 16.2 2.91∗,∗∗ | |
| 3 | SVKIISNASCTTNALAPLAK | 80.1 2.78 | 2.60 0.22∗,∗∗ | |
| 4 | SLKIISNASCTTNALAPVAK | 72.0 2.11 | 9.06 2.73∗,∗∗ | |
| 5 | SNASCTTNAL | |||
| 6 | SNASCTTNSL | 25.0 2.87 | 100 3.52 | 94.5 9.77 |
| 7 | SNASATTNCL | |||
| 8 | SNASCTTNDL | 58.7 2.55 | 102 3.68 | 99.5 2.68 |
| 9 | SNASCTTNFL | 22.8 2.44 | 101 3.18 | 104 1.60 |
| 10 | SNASCTTNGL | 56.4 2.77 | 102 1.28 | 97.0 3.32 |
| 11 | SCTTNAL | 48.3 1.06 | 101 3.28 | 106 3.32 |
| 12 | SNASCTT | 46.2 2.91 | 100 3.01 | 98.8 5.01 |
| 13 | SCTT | 89.6 2.79 | 101 3.05 | 97.6 6.14 |
| 14 | NASC | 74.9 3.00 | 101 1.44 | 96.5 6.15 |
| 15 | ASCT | 72.2 2.49 | 102 1.12 | 98.0 4.49 |
| 16 | CTTN | 70.8 2.10 | 101 1.24 | 96.1 10.6 |
| 17 | SCT | 97.2 1.88 | 101 2.95 | 100 1.19 |
| 18 | ASC | 80.3 2.18 | 102 2.95 | 109 4.57 |
| 19 | CTT | 89.7 2.56 | 101 2.15 | 108 4.80 |
| 20 | ACT | 83.4 1.84 | 102 1.85 | 103 9.17 |
| 21 | SCA | 86.5 2.56 | 101 0.90 | 93.6 8.71 |
| GSH | ECG | 43.3 2.55 | 101 3.17 | 98.5 3.60 |
Twenty peptides (GAI-2–21) based on the amino acid sequence of GAI-1 were synthesized and evaluated with GAPDH aggregation inhibitory effect (potency), the effect on cell viability (cytotoxicity), and GAPDH activity (side effect). n = 4, mean ± S.D. ∗p < 0.05 and ∗∗p < 0.01, relative to the treatment with vehicle, as determined by Student’s t test. Endogenous cysteine-containing tripeptide glutathione (GSH) was examined (bottom row), as compared with GAI-17. () means “not determined.”