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Literature summary for 3.1.4.17 extracted from

  • Iffland, A.; Kohls, D.; Low, S.; Luan, J.; Zhang, Y.; Kothe, M.; Cao, Q.; Kamath, A.V.; Ding, Y.H.; Ellenberger, T.
    Structural determinants for inhibitor specificity and selectivity in PDE2A using the wheat germ in vitro translation system (2005), Biochemistry, 44, 8312-8325.
    View publication on PubMed
Search for more literature for 3.1.4.17

Cloned(Commentary)

Cloned (Comment) Organism
expression in insect cells or in Escherichia coli Homo sapiens

Crystallization (Commentary)

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

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

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 [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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

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

Synonyms Comment Organism
PDE2A
-
 Homo sapiens

Turnover Number [1/s]

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 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