Table III.
Inhibition constants of PR11 and some its most active mutants.
Peptide | Ki (nM) | Error |
---|---|---|
PR11 (wild type) | 86.5 | 21.1 |
W12 | 39.5 | 2.3 |
F8W12 | 184 | 16.3 |
A8W12 | 50.7 | 16.8 |
Conditions: 5 nM human 20S proteasome, 20–100 µM Suc-LLVY-AMC substrate, 0, 75 or 100 nM PR-peptide, 25 mM Tris, pH 7.5, 0.03% SDS, 37 °C. Under these conditions, Km for the enzyme was 47.4±5 µM and Vmax was 0.55±0.03 µmol/h/mg.