Figure 3.
Kinetic analysis of inhibition of hu i-20S and hu c-20S by oxathiazolones. Reaction progress curves of cleavage of Suc-LLVY-AMC by hu i-20S (A) or c-20S (B) in the absence or presence of HT2106 at 0.78–100 μM. The curves were fit to equation I: P = (Vi/kobs) × [1 – exp(−kobst)], to determine the apparent first-order rate constant kobs values. Inset: kobs vs [I] for i-20S in panel A and for c-20S in panel B. (C) Plot of kobs on inhibitor concentrations yielded kinact and KI by fitting to equation II: kobs = kinact/(1 + Ki/[inhibitor]).