Table 2.
CoA preferentially binds to active, T288 phosphorylated Aurora A. The binding of T288 phosphorylated Aurora A (‘active’), or unphosphorylated Aurora A (‘inactive’), was assessed for each compound and the inhibitory constants were calculated. The data confirm that both the pantetheine and the 3′-phosphate of CoA participate in the interaction between Aurora A and CoA.
Compound | Aurora A (active) IC50 (μM), binding assay | Aurora A (inactive) IC50 (μM), binding assay | Aurora A (active) IC50 (μM), activity assay |
---|---|---|---|
ATP | 0.2 | 3.0 | – |
ADP | 0.17 | 1.3 | 54 |
dpCoA | 0.0003 | >100 | 17 |
CoA | 0.00001 | 0.28 | 5 |