Table 2.
Summary of the most active candidate drugs with antiaggregation activity against various γ-crystallins exposed to heating at 72 °C for 20 min
| Crystallin type | Drug codes in order of efficacy | Stoichiometric drug:protein ratio | % Suppression |
|---|---|---|---|
| Bovine γ-crystallinsa | |||
| 1. | CGMDVX | 1.7:1 | 60/48/40/40/36/30 |
| 2. | GCXBVD | 1.7:1 | 75/73/55/54/53/44 |
| HγDa | |||
| 1. | GDCBXM | 1.7:1 | 69/66/65/63/61/38 |
| 2. | DGCMBX | 1.7:1 | 78/75/73/73/60/47 |
| HγS | CXDBGT | 1.7:1 | 71/68/61/60/46/40 |
| HγS_N14D | CDGXBM | 1.7:1 | 77/76/73/60/51/48 |
| HγS_N76D | CXDBMG | 1.7:1 | 70/60/59/57/55/55 |
| HγS_N143D | CXGTDM | 1.7:1 | 52/50/48/42/30/25 |
| HγS_N14/76/143D | GCXBMD | 1.7:1 | 89/76/71/46/46/32 |
The proteins were tested at 75 μM concentration (1.5 mg/ml of 50 mM K+PO43−, pH 7.2) incubated for 20 min at 72 °C with 125 μM or less inhibitor concentration. This corresponds to 1.7:1 stoichiometric drug:protein ratio. For drug codes, refer to Table 1.
a
Denotes results from separate experiments.