Studies of the effect of inhibitors of PDE3A and its mutants
. | cGMP KI μmol/L (mean ± SD) . | Milrinone IC50 μmol/L (mean ± SD) . | Rolipram IC50 μmol/L . |
---|---|---|---|
PDE3AΔ1 | 0.76 ± 0.09 | 1.85 ± 0.26 | >100 |
H752A | 0.84 ± 0.15 | 1.65 ± 0.23 | >100 |
H756A | 1.01 ± 0.16 | 2.13 ± 0.41 | >100 |
E825A | 4.03 ± 0.35* | 1.72 ± 0.17 | >100 |
H836A | 135.3 ± 11.5* | 0.35 ± 0.10 | >100 |
E866A | 20.6 ± 2.08* | 2.39 ± 0.37 | >100 |
E971A | 1.06 ± 0.21 | 1.65 ± 0.24 | >100 |
. | cGMP KI μmol/L (mean ± SD) . | Milrinone IC50 μmol/L (mean ± SD) . | Rolipram IC50 μmol/L . |
---|---|---|---|
PDE3AΔ1 | 0.76 ± 0.09 | 1.85 ± 0.26 | >100 |
H752A | 0.84 ± 0.15 | 1.65 ± 0.23 | >100 |
H756A | 1.01 ± 0.16 | 2.13 ± 0.41 | >100 |
E825A | 4.03 ± 0.35* | 1.72 ± 0.17 | >100 |
H836A | 135.3 ± 11.5* | 0.35 ± 0.10 | >100 |
E866A | 20.6 ± 2.08* | 2.39 ± 0.37 | >100 |
E971A | 1.06 ± 0.21 | 1.65 ± 0.24 | >100 |
Each value is the mean ± SD of three independent experiments. Each mutant was compared to PDE3AΔ1 by the Student t-test.
P < .01.