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Literature summary for 3.1.4.53 extracted from
- Recombinant expression of a type IV, cAMP-specific phosphodiesterase: Characterization and structure-function studies of deletion mutants (1997), Biochemistry, 36, 2968-2976.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| full coding sequence of the phosphodiesterase PDE4D1 is inserted in the bacterial expression vector pGEX-KG. N- and C-terminal truncations are also placed in the same vector, allowing the expression and purification of glutathione S-transferase (GST)-PDE fusion proteins using glutathione-Sepharose | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone | competitive | Rattus norvegicus |  |
| methylisobutylxanthine | - |
Rattus norvegicus | |
| additional information | removal of the last 35 amino acids of an N-terminal 80-residue highly conserved region (UCR2) results in a 6fold increase in PDE activity, providing evidence that this part of the molecule acts as an intramolecular inhibitor | Rattus norvegicus | |
| rolipram | - |
Rattus norvegicus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Co2+ | the enzyme is able to use Mg2+, Co2+, and Mn2+, but not Zn2+ | Rattus norvegicus | |
| Mg2+ | the enzyme is able to use Mg2+, Co2+, and Mn2+, but not Zn2+ | Rattus norvegicus | |
| Mn2+ | 0.015 mM, 20fold increase in activity | Rattus norvegicus | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| GST-rPDE4D1 fusion protein | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| adenosine 3',5'-cyclic phosphate + H2O | - |
Rattus norvegicus | adenosine 5'-phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDE4D1 | - |
Rattus norvegicus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0018 | - |
4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone | - |
Rattus norvegicus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0004 | - |
- |
Rattus norvegicus | rolipram | |
| 0.002 | - |
- |
Rattus norvegicus | Ro20-1724 | |
| 0.04 | - |
- |
Rattus norvegicus | methylisobutylxanthine | |
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Release 2023.1 (January 2023)
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