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Literature summary for 3.1.4.35 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
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Inhibitors

Inhibitors Comment Organism Structure
8-methoxymethyl-isobutylmethylxanthine inhibits isoform PDE5, is 3times more potent in inhibiting PDE5 than PDE1 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 PDE5 (16fold) Bos taurus
sildenafil
-
 Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
anion exchange chromatography Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
aortic smooth muscle isoform PDE5 Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cGMP + H2O
-
 Bos taurus 5'-GMP
-
 ?

Synonyms

Synonyms Comment Organism
PDE5 isoform Bos taurus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus sildenafil
0.0055
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus 8-methoxymethyl-isobutylmethylxanthine
0.023
-
 isoform PDE5, pH and temperature not specified in the publication Bos taurus dioclein