FIGURE 6.
2-Acetylamino-2-deoxy-3-O-methyl-d-mannose (8a) inhibits purified MNK. A coupled optical assay using enzymatic consumption of NADH was performed to show the effect of 8a on MNK activity. In a, purified MNK was incubated with ManNAc (125 μm), ATP (2 mm), and different concentrations of 8a. Obtained activity data were normalized to controls without inhibitor (0%). In b and c, MNK was tested with 8a (1.25 mm) and varying concentrations of ManNAc (b) or ATP (c), respectively. Measured data were compared with controls without inhibitor (gray triangles). Data shown represent the mean values and S.D. obtained in three independent experiments (n = 3) for a and b and five independent experiments (n = 5) in c. Linear (b and c) and sigmoidal dose response (a) curve approximations were performed to determine Km, Ki, and IC50 values.