Kinetic properties of mutants: effect of S773D mutation on the kinetics of PIK-75 inhibition with respect to the substrate PI
Kinetic analysis of the PIK-75 effect on PI binding to wild-type p110α, p110α S773D, and p110α H855E mutant enzymes. Kinetic constants Km for substrate and the Ki for PIK-75 were estimated using the Michaelis-Menten and competitive inhibition models, respectively (GraphPad Prism) (n = 4).
| Km PI | Ki PIK-75 | |
|---|---|---|
| μM | nM | |
| WT | 7.0 ± 1.5 | 2.3 ± 0.6 |
| S773D | 11.2 ± 1.9 | 146 ± 11 |
| H855E | 3.9 ± 0.8 | N.D. |
N.D., not determined.