TABLE 1.
NMR proteasome ChT-L and T-L activity only in the cytosolic fraction showed remarkable resistance to competitive inhibition as indicated by significant differences (*, p > 0.05) when compared to mouse values. IC50 values are indicated in μM ± S.E.
| Fraction/Inhibitor | ChT-L IC50 (μM) | T-L IC50 (μM) | ||
|---|---|---|---|---|
| NMR | Ms | NMR | Ms | |
| Cytosolic/ Adh (VS) | 125.0±5.6* | 5.56±1.57* | 80.6±2.5* | 16.2±1.9* |
| Cytosolic/ MG132 | 122.0±5.5* | 8.22±2.75* | 71.4±8.7* | 14.6±4.4* |
| Cytosolic/LC | 6.15±1.4* | 0.156±0.005* | -- | -- |
| Cytosolic/BZ | 2.45±0.74* | 0.015±0.004* | -- | -- |
| Microsomal/MG132 | 1.79 | 0.99 | 3.01 | 6.63 |
| Nuclear/ MG132 | 6.49±2.70 | 4.6±1.62 | 2.70±1.4 | 12.8±4.7 |
-- = no data; Adh (VS) = adamantane-acetyl-(6-aminohexanoyl)3-(leucinyl)3- vinyl-(methyl)-sulfone ; MG132 = N-(benzyl-oxycarbonyl) leucinyl-leucinyl- leucinal; LC = lactacystin; BZ = bortezomib