Table 2.
Inhibitor | Ki (nM), subtype B | Ki (nM), subtype A | Ki (nM), subtype C |
---|---|---|---|
Indinavir | 0.8 ± 0.06 | 5.1 ± 0.2 | 2.5 ± 0.2 |
Ritonavir | 0.05 ± 0.005 | 0.36 ± 0.03 | 0.23 ± 0.02 |
Saquinavir | 0.5 ± 0.03 | 1.2 ± 0.08 | 1.1 ± 0.05 |
Nelfinavir | 1.0 ± 0.07 | 2.6 ± 0.2 | 2.1 ± 0.1 |
Inhibition constants, Ki, for the inhibitors indinavir, ritonavir, saquinavir, and nelfinavir were obtained at 25°C by measuring the rate of substrate hydrolysis using 15–30 nM Protease in 10 mM sodium acetate, 1 M NaCl, pH 5.0, and 42.5 μM substrate plus increasing amounts of inhibitor.