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Literature summary for 3.1.4.17 extracted from
- The flavonoid dioclein is a selective inhibitor of cyclic nucleotide phosphodiesterase type 1 (PDE1) and a cGMP-dependent protein kinase (PKG) vasorelaxant in human vascular tissue (2009), Eur. J. Pharmacol., 620, 78-83.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol | - |
Homo sapiens |  |
| 8-methoxymethyl-isobutylmethylxanthine | inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5, is 3times more potent in inhibiting PDE5 than PDE1 | Bos taurus | |
| dioclein | potent selective and calmodulin-independent inhibitor of PDE1, competitive inhibitor for cGMP hydrolysis by PDE1 in basal-activated (1 mM EGTA) and calmodulin-activated (18 nM calmodulin with 0.01 mM CaCl2) states. Dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold), PDE3 (19fold), PDE4 (11fold), and PDE5 (16fold) | Bos taurus | |
| dioclein | dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold) | Homo sapiens | |
| nimodipine | - |
Bos taurus | |
| vinpocetine | inhibitor of activated PDE1 | Bos taurus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| nucleoside 3',5'-cyclic phosphate + H2O | Homo sapiens | - |
nucleoside 5'-phosphate | - |
? | |
| nucleoside 3',5'-cyclic phosphate + H2O | Bos taurus | - |
nucleoside 5'-phosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Bos taurus | - |
- |
- |
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| anion exchange chromatography | Homo sapiens |
| anion exchange chromatography | Bos taurus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| aortic smooth muscle | isoform PDE1 | Bos taurus | - |
| blood platelet | isoform PDE2 | 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'-cAMP + H2O | - |
Bos taurus | 5'-AMP | - |
? | |
| 3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? | |
| 3',5'-cGMP + H2O | - |
Bos taurus | 5'-GMP | - |
? | |
| nucleoside 3',5'-cyclic phosphate + H2O | - |
Homo sapiens | nucleoside 5'-phosphate | - |
? | |
| nucleoside 3',5'-cyclic phosphate + H2O | - |
Bos taurus | nucleoside 5'-phosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cyclic nucleotide phosphodiesterase type 1 | - |
Bos taurus |
| PDE1 | isoform | Bos taurus |
| PDE2 | isoform | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| Calmodulin | - |
Homo sapiens | |
| Calmodulin | - |
Bos taurus | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00055 | - |
dioclein | isoform PDE1 in basal-activated state, pH and temperature not specified in the publication | Bos taurus | |
| 0.00062 | - |
dioclein | isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication | Bos taurus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00144 | - |
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication | Bos taurus | dioclein | |
| 0.0023 | - |
isoform PDE2, pH and temperature not specified in the publication | Homo sapiens | (2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol | |
| 0.00247 | - |
isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication | Bos taurus | dioclein | |
| 0.0032 | - |
isoform PDE1, pH and temperature not specified in the publication | Bos taurus | nimodipine | |
| 0.0152 | - |
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication | Bos taurus | 8-methoxymethyl-isobutylmethylxanthine | |
| 0.0382 | - |
isoform PDE2 in calmodulin-activated state, pH and temperature not specified in the publication | Homo sapiens | dioclein | |
| 0.1 | - |
isoform PDE2 in basal-activated state, pH and temperature not specified in the publication | Homo sapiens | dioclein | |
| 0.185 | - |
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication | Bos taurus | vinpocetine | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | inhibition of PDE1 is involved in the cGMP-dependent protein kinase-mediated vasorelaxant effect of dioclein in human saphenous vein | Bos taurus |
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