Table 1.
Inhibition constants of phosphinate against GspS and various TryS enzymes. All assays were performed under conditions approximating to the intracellular physiological state (i.e. pH 7.2, 2 mm Spd, 0.2 mm GSH and 2 mm Mg2+-ATP), and were initiated with 100 nm each enzyme in the presence of various phosphinate concentrations. IC50 values and slope factors are from the inhibition profiles determined from Eqn (7), and Kiapp values were determined from the tight-binding inhibition equation (Eqn 8). The errors represent the standard error of the fit to the appropriate equation.
Enzyme |
|||||
---|---|---|---|---|---|
Inhibition constants | CfGspS | CfTryS | L. major TryS | T. cruzi TryS | T. brucei TryS |
IC50 (nm) | 72 ± 6 | 1380 ± 380 | 650 ± 25 | 530 ± 20 | 1300 ± 50 |
Slope factor | 1.2 ± 0.1 | 1.1 ± 0.3 | 1.1 ± 0.04 | 1.1 ± 0.04 | 1.1 ± 0.05 |
Kiapp (nm) | 29 ± 5 | 1330 ± 350 | 580 ± 30 | 490 ± 20 | 1200 ± 500 |