TABLE 2.
Substrate inhibition and feedback inhibition of l-FMAU phosphorylation by cellular kinasesa
Enzyme |
Ki (μM)
|
IC50 (μM)b
|
||
---|---|---|---|---|
dThd | dCyd | TTP | dCTP | |
Cytosolic dThd kinase | 7 ± 0.1 | NDc | 4 ± 1 | ND |
Cytosolic dCyd kinase | ND | 1.2 ± 0.1 | ND | 0.8 ± 0.5 |
Mitochondrial dPyd kinase | 10.8 ± 2 | >100 | 12 ± 2 | 6 ± 0.1 |
The values presented here are the averages of triplicate experiments. Ki was determined by using the equation for a competitive inhibitor.
IC50, concentration required for 50% inhibition of l-FMAU phosphorylation.
ND, not detectable.