Cloned (Comment) | Organism |
---|---|
expression in insect cells or in Escherichia coli | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
vapor diffusion method, crystal structure of the catalytic domain of PDE2A (PDE2A residues 578-919) determined at 1.7 A resolution | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D811A | activity towards 3',5'-cGMP is similar to wild-type activity, activity towards 3',5'-cAMP is less than 50% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram | Homo sapiens |
D811A/Q812I | activity towards 3',5'-cGMP and 3',5'-cAMP is less than 50% of wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram | Homo sapiens |
I826V | activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram | Homo sapiens |
L858M | activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram | Homo sapiens |
L858S | activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity | Homo sapiens |
L907A | activity towards 3',5'-cGMP is less than 10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity | Homo sapiens |
M847L | activity towards 3',5'-cGMP is less than10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity | Homo sapiens |
Q812I | activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity towards 3',5'-cAMP is similar to wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram | Homo sapiens |
Q812P | activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity | Homo sapiens |
Q812P/T819Y | activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity | Homo sapiens |
T819Y | activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram | Homo sapiens |
Y827A | activity towards 3',5'-cGMP is less than 10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity | Homo sapiens |
Y827F | activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram | Homo sapiens |
Y827F/L907A | activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity | Homo sapiens |
Y827M | activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity | Homo sapiens |
Y827V | activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
erythro-9-(2-hydroxy-3-nonyl)adenine | IC50: 0.00061 mM for wild-type enzyme | Homo sapiens | |
rolipram | IC50: 0.15 mM for wild-type enzyme | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.032 | - |
3',5'-cAMP | catalytic domain of PDE2A (PDE2A residues 578-919), enzyme expressed in Escherichia coli | Homo sapiens | |
0.034 | - |
3',5'-cGMP | catalytic domain of PDE2A (PDE2A residues 578-919), enzyme expressed in Escherichia coli | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3',5'-cAMP + H2O | - |
Homo sapiens | 5'-AMP | - |
? | |
3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PDE2A | - |
Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.3 | - |
3',5'-cAMP | catalytic domain of PDE2A (PDE2A residues 578-919), enzyme expressed in Escherichia coli | Homo sapiens | |
4.2 | - |
3',5'-cGMP | catalytic domain of PDE2A (PDE2A residues 578-919), enzyme expressed in Escherichia coli | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00061 | - |
IC50: 0.00061 mM for wild-type enzyme | Homo sapiens | erythro-9-(2-hydroxy-3-nonyl)adenine | |
0.15 | - |
IC50: 0.15 mM for wild-type enzyme | Homo sapiens | rolipram |