Table 2.

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.

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