Literature summary for 3.1.4.53 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.

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Inhibitors

Inhibitors	Comment	Organism	Structure
8-methoxymethyl-isobutylmethylxanthine	inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5	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 19fold more selective for the activated PDE1 isoform compared to PDE3	Bos taurus
rolipram	-	Bos taurus
vinpocetine	inhibitor of activated isoform PDE4	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 PDE4	Bos taurus	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
PDE4	isoform	Bos taurus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0007	-	isoform PDE4, pH and temperature not specified in the publication	Bos taurus	rolipram
0.0168	-	isoform PDE4, pH and temperature not specified in the publication	Bos taurus	dioclein
0.131	-	isoform PDE4, pH and temperature not specified in the publication	Bos taurus	vinpocetine

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Release 2023.1 (January 2023)