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Literature summary extracted from

  • Goncalves, R.L.; Lugnier, C.; Keravis, T.; Lopes, M.J.; Fantini, F.A.; Schmitt, M.; Cortes, S.F.; Lemos, V.S.
    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.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.12 cGMP
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.12 Rp-8-pCPT-cGMPS
-
 Homo sapiens
3.1.4.17 (2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol
-
 Homo sapiens
3.1.4.17 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
3.1.4.17 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
3.1.4.17 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
3.1.4.17 nimodipine
-
 Bos taurus
3.1.4.17 vinpocetine inhibitor of activated PDE1 Bos taurus
3.1.4.35 8-methoxymethyl-isobutylmethylxanthine inhibits isoform PDE5, is 3times more potent in inhibiting PDE5 than PDE1 Bos taurus
3.1.4.35 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 PDE5 (16fold) Bos taurus
3.1.4.35 sildenafil
-
 Bos taurus
3.1.4.53 8-methoxymethyl-isobutylmethylxanthine inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5 Bos taurus
3.1.4.53 dioclein dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 19fold more selective for the activated PDE1 isoform compared to PDE3 Bos taurus
3.1.4.53 rolipram
-
 Bos taurus
3.1.4.53 vinpocetine inhibitor of activated isoform PDE4 Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.12 ATP + a protein Homo sapiens
-
 ADP + a phosphoprotein
-
 ?
3.1.4.17 nucleoside 3',5'-cyclic phosphate + H2O Homo sapiens
-
 nucleoside 5'-phosphate
-
 ?
3.1.4.17 nucleoside 3',5'-cyclic phosphate + H2O Bos taurus
-
 nucleoside 5'-phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.12 Homo sapiens
-
-
-
3.1.4.17 Bos taurus
-
-
-
3.1.4.17 Homo sapiens
-
-
-
3.1.4.35 Bos taurus
-
-
-
3.1.4.53 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.4.17 anion exchange chromatography Homo sapiens
3.1.4.17 anion exchange chromatography Bos taurus
3.1.4.35 anion exchange chromatography Bos taurus
3.1.4.53 anion exchange chromatography Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.12 saphenous vein
-
 Homo sapiens
-
2.7.11.12 vascular tissue
-
 Homo sapiens
-
3.1.4.17 aortic smooth muscle isoform PDE1 Bos taurus
-
3.1.4.17 blood platelet isoform PDE2 Homo sapiens
-
3.1.4.35 aortic smooth muscle isoform PDE5 Bos taurus
-
3.1.4.53 aortic smooth muscle isoform PDE4 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.12 ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?
3.1.4.17 3',5'-cAMP + H2O
-
 Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cAMP + H2O
-
 Bos taurus 5'-AMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O
-
 Bos taurus 5'-GMP
-
 ?
3.1.4.17 nucleoside 3',5'-cyclic phosphate + H2O
-
 Homo sapiens nucleoside 5'-phosphate
-
 ?
3.1.4.17 nucleoside 3',5'-cyclic phosphate + H2O
-
 Bos taurus nucleoside 5'-phosphate
-
 ?
3.1.4.35 3',5'-cGMP + H2O
-
 Bos taurus 5'-GMP
-
 ?
3.1.4.53 3',5'-cAMP + H2O
-
 Bos taurus 5'-AMP
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.12 cGMP-dependent protein kinase
-
 Homo sapiens
2.7.11.12 PKG
-
 Homo sapiens
3.1.4.17 cyclic nucleotide phosphodiesterase type 1
-
 Bos taurus
3.1.4.17 PDE1 isoform Bos taurus
3.1.4.17 PDE2 isoform Homo sapiens
3.1.4.35 PDE5 isoform Bos taurus
3.1.4.53 PDE4 isoform Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
3.1.4.17 Calmodulin
-
 Homo sapiens
3.1.4.17 Calmodulin
-
 Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.17 0.00055
-
 dioclein isoform PDE1 in basal-activated state, pH and temperature not specified in the publication Bos taurus
3.1.4.17 0.00062
-
 dioclein isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.17 0.00144
-
 isoform PDE1 in basal-activated state, pH and temperature not specified in the publication Bos taurus dioclein
3.1.4.17 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
3.1.4.17 0.00247
-
 isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication Bos taurus dioclein
3.1.4.17 0.0032
-
 isoform PDE1, pH and temperature not specified in the publication Bos taurus nimodipine
3.1.4.17 0.0152
-
 isoform PDE1 in basal-activated state, pH and temperature not specified in the publication Bos taurus 8-methoxymethyl-isobutylmethylxanthine
3.1.4.17 0.0382
-
 isoform PDE2 in calmodulin-activated state, pH and temperature not specified in the publication Homo sapiens dioclein
3.1.4.17 0.1
-
 isoform PDE2 in basal-activated state, pH and temperature not specified in the publication Homo sapiens dioclein
3.1.4.17 0.185
-
 isoform PDE1 in basal-activated state, pH and temperature not specified in the publication Bos taurus vinpocetine
3.1.4.35 0.000002
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus sildenafil
3.1.4.35 0.0055
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus 8-methoxymethyl-isobutylmethylxanthine
3.1.4.35 0.023
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus dioclein
3.1.4.53 0.0007
-
 isoform PDE4, pH and temperature not specified in the publication Bos taurus rolipram
3.1.4.53 0.0168
-
 isoform PDE4, pH and temperature not specified in the publication Bos taurus dioclein
3.1.4.53 0.131
-
 isoform PDE4, pH and temperature not specified in the publication Bos taurus vinpocetine

General Information

EC Number General Information Comment Organism
2.7.11.12 physiological function cGMP-dependent protein kinase is involved in the vasodilation of human saphenous veins Homo sapiens
3.1.4.17 malfunction inhibition of PDE1 is involved in the cGMP-dependent protein kinase-mediated vasorelaxant effect of dioclein in human saphenous vein Bos taurus