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2'-O-(N-methylanthraniloyl)adenosine-3',5'-cyclic monophosphate + H2O
2'-O-(N-methylanthraniloyl)adenosine-5'-monophosphate
fluorescent cAMP analogue
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-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
cGMP + H2O
5'-GMP
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-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
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?
additional information
?
-
3',5'-cAMP + H2O
5'-AMP
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?
3',5'-cAMP + H2O
5'-AMP
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?
3',5'-cAMP + H2O
5'-AMP
-
-
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?
3',5'-cAMP + H2O
5'-AMP
DdPDE4 regulates intercellular cAMP during multicellular development
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?
3',5'-cAMP + H2O
5'-AMP
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-
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?
3',5'-cAMP + H2O
5'-AMP
-
-
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?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
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?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
specific substrate
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-
?
3',5'-cAMP + H2O
5'-AMP
specific substrate
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-
?
3',5'-cAMP + H2O
5'-AMP
specific substrate
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-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7
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-
?
3',5'-cAMP + H2O
5'-AMP
-
specific for 3',5'-cAMP, PDE4
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-
?
3',5'-cAMP + H2O
5'-AMP
-
specific for 3',5'-cAMP, PDE8
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-
?
3',5'-cAMP + H2O
5'-AMP
PDE4 hydrolyses selectively 3',5'-cAMP with high affinity
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-
?
3',5'-cAMP + H2O
5'-AMP
LmjPDEB1 is completely cAMP-specific
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-
?
3',5'-cAMP + H2O
5'-AMP
LmjPDEB2 is completely cAMP-specific
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?
3',5'-cAMP + H2O
5'-AMP
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-
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?
3',5'-cAMP + H2O
5'-AMP
-
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?
3',5'-cAMP + H2O
5'-AMP
-
PDE7A1 possesses a non-catalytic activity that can contribute to the termination of cAMP signals via direct inhibition of C subunit of cAMP-dependent protein kinase
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-
?
3',5'-cAMP + H2O
5'-AMP
-
-
the reaction product, 5'-AMP, is further dephosphorylated to adenosine by PdeA and PdeB
-
?
3',5'-cAMP + H2O
5'-AMP
CpdA possesses 3',5'-cAMP phosphodiesterase activity in vitro
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-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
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?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
specific for cAMP
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-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
-
PDE4
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-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
-
PDE7
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-
?
3',5'-cGMP + H2O
5'-GMP
low activity
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-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7
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?
3',5'-cGMP + H2O
5'-GMP
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
DdPDE4 is a unique membrane-bound phosphodiesterase with an extracellular catalytic domain regulating intercellular cAMP during multicellular development
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
the enzyme is specific for cAMP
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
determination of reaction rate and mechanism using computational modeling, quantum mechanical/molecular mechanical-free energy perturbation, QM/MM-FE, and QM/MM-Poisson-Boltzmann surface area, PBSA, calculations. The onQM/MMreaction-coordinate calculations including the protein environment of any PDE-catalyzed reaction system identifies a unique catalytic reaction mechanism, overview
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
the enzyme is highly specific for cAMP
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
no activity with cGMP
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-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
PDE8 is specific for the hydrolysis of cAMP
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-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
the enzyme is specific for cAMP
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
both PDE8A and 8B hydrolyze cAMP with a very high affinity
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
PDE4B4 isoform may have a distinct functional role in regulating cAMP levels in specific cell types
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
attenuation of the activity of the cAMP-specific phosphodiesterase PDE4A5 by interaction with the immunophilin XAP2
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
no activity with cGMP
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?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
the enzyme is specific fpr cAMP
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?
cAMP + H2O
5'-AMP
-
degradation of extracellular cAMP
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?
cAMP + H2O
5'-AMP
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?
cAMP + H2O
5'-AMP
-
isoform PDE7A1 possesses a non-catalytic activity that can contribute to the termination of cAMP signals via direct inhibition of C subunit of cAMP-dependent protein kinase
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cAMP + H2O
5'-AMP
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?
cAMP + H2O
5'-AMP
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?
additional information
?
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isoform PDE4 regulates both GalphaS-dependent and GalphaS-indeoendent cAMP pools in the neurons controling locomotion rate
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?
additional information
?
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cGMP is hydrolyzed at least 100fold more slowly than cAMP
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?
additional information
?
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cGMP is hydrolyzed at least 100fold more slowly than cAMP
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?
additional information
?
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PDE4 may be involved in the cyclic nucleotide-mediated control of smooth muscle tone
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?
additional information
?
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enzyme variants PDE4B and/or PDE4D regulate cell growth through cAMP targets in the HMG malignant melanoma cell
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additional information
?
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interaction of PDE4D5 with both the N- and C-domains of beta-arrestin 2 are essential for beta2-adrenoceptor regulation
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?
additional information
?
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interaction of PDE4D5 with both the N- and C-domains of beta-arrestin 2 are essential for beta2-adrenoceptor regulation
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?
additional information
?
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PDE4D deficiency may contribute to heart failure and arrhythmias by promoting defective regulation of the RyR2 channel in humans
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?
additional information
?
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PDE4D deficiency may contribute to heart failure and arrhythmias by promoting defective regulation of the RyR2 channel in humans
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?
additional information
?
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PDE4D deficiency may contribute to heart failure and arrhythmias by promoting defective regulation of the RyR2 channel in humans
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?
additional information
?
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PDE4D5 plays a nonredundant and functionally significant role in its interaction with beta-arrestin and in the mechanics of beta2-adrenergic receptor signalling
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?
additional information
?
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no activity with cGMP
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?
additional information
?
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no hydrolysis of cGMP
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?
additional information
?
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no hydrolysis of cGMP
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?
additional information
?
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PDE7B does not hydrolyse cGMP
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?
additional information
?
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PDE7B does not hydrolyse cGMP
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?
additional information
?
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wild-type enzyme shows no activity with cGMP, mutant enzymes D440N and D440A show activity with cGMP
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?
additional information
?
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protein-protein interactions between EPAC1 and PDE4D, peptide mapping for binding site determination. A cell-permeable variant of this peptide antagonizes EPAC1-PDE4D binding and directly alters vascular endothelial cell permeability
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?
additional information
?
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recruitment of PDE4 to the beta2 adrenergic receptor
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?
additional information
?
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PDE4 is a component of signaling pathways involved in the mediation of antidepressant activity
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?
additional information
?
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PDE4B is involved in LPS signaling
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?
additional information
?
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PDE7A1 possesses a non-catalytic activity that can contribute to the termination of cAMP signals via direct inhibition of the C subunit of the cAMP-dependent kinase
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?
additional information
?
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PDE7B does not hydrolyse cGMP
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?
additional information
?
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PDE7B does not hydrolyse cGMP
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?
additional information
?
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PDE4 regulates adenosine A2A receptor signaling in striatopallidal neurons
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?
additional information
?
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Myxococcus xanthus PdeA and PdeB, enzymes hydrolyze 3',5'- and 2',3'-cyclic AMP to adenosine, and also demonstrate phosphatase activity toward nucleoside 5'-tri-, 5'-di-, 5'- and 3'-monophosphates with highest activities for nucleoside 5'-monophosphates. PdeA and PdeB also show high phosphomonoesterase activities against 50-UMP, 3'-AMP, and 3'-GMP, low activities against 5'-dAMP, and no activities toward 2'-AMP and 2'-GMP
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?
additional information
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iron and conserved residues are essential for CpdA activity, the catalytic mechanism for Pseudomonas aeruginosa CpdA utilizes a Fe3+-Fe2+ center
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?
additional information
?
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iron and conserved residues are essential for CpdA activity, the catalytic mechanism for Pseudomonas aeruginosa CpdA utilizes a Fe3+-Fe2+ center
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?
additional information
?
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during development PDE4 is the major PDE
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?
additional information
?
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almost all the PDE4D isoforms, known as the main cAMP-regulated rolipramsensitive PDE in Sertoli cells, are expressed throughout the early postpartum period, whereas only the short PDE4D isoforms (PDE4D1 and PDE4D2) are transcriptionally regulated by FSH
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?
additional information
?
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increased PDE4 activity, specifically phosphodiesterase 4B4 activity, reduces beta-adrenergic signaling in the kidney and contributes to salt-sensitive hypertension in the Dahl salt-sensitive rat
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?
additional information
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TbrPDEB1 and TbrPDEB2 are essential for virulence, making them valuable potential targets for new PDE-inhibitor based trypanocidal drugs
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?
additional information
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TbrPDEB1 and TbrPDEB2 are essential for virulence, making them valuable potential targets for new PDE-inhibitor based trypanocidal drugs
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?
additional information
?
-
TbrPDEB1 and TbrPDEB2 are essential for virulence, making them valuable potential targets for new PDE-inhibitor based trypanocidal drugs
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?
additional information
?
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TbrPDEB1 and TbrPDEB2 are essential for virulence, making them valuable potential targets for new PDE-inhibitor based trypanocidal drugs
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?
additional information
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cGMP neither activates the enzyme nor competes as a substrate
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?
additional information
?
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cGMP neither activates the enzyme nor competes as a substrate
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?
additional information
?
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no activity with cGMP
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?
additional information
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no activity with cGMP
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?
additional information
?
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no activity with up to 0.1 mM cGMP
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?
additional information
?
-
no activity with up to 0.1 mM cGMP
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?
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(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.1195 mM, PDE7
(2E)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
-
IC50: 0.31 mM, PDE4
(2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
IC50: 0.00043 mM, PDE4
(4aS,8aR)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
1,10-phenanthroline
-
0.3 mM, more than 95% inhibition
1-(2,4-dichlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
10-(3-pyrrolidin-1-ylpropyl)-2-(trifluoromethyl)-10H-phenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-trifluoromethylphenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-trifluoromethylphenoxazine
-
-
10-(4'-N-pyrrolidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
-
increase of Km value in presence of inhibitor
10-[3'-[(beta-hydroxyethyl)-piperazino]propyl]-2-trifluoromethylphenoxazine
-
-
10-[30-[(beta-hydroxy ethyl)-piperazino]propyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)-butyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)butyl]-2-trifluoromethylphenoxazine
-
-
10-[4'-[(beta-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
-
-
10-[4'-[(beta-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
-
-
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
IC50: 0.0203 mM, PDE7; IC50: 0.0453 mM, PDE4
3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide
-
-
3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride
-
3-isobutyl-1-methyl-xanthine
3-isobutyl-1-methylxanthine
3-isobutyl-methylxanthine
-
inhibitor of all PDE isoforms except PDE8
3-isobuytl-1-methylxanthine
-
4-(3,4-dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one
-
PDE4 inhibitor, potent inhibitor of isoform PDE4D3
4-(3,4-dimethoxyphenyl)-2-{5-[(2-{5-[2-(2-fluoro-5-methoxyphenyl)ethyl]tetrahydrofuran-2-yl}ethyl)amino]pentyl}-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
the dual PDE4 inhibitor/selective serotonin reuptake inhibitor shows potent and selective serotonin reuptake inhibition
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
-
4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone
-
competitive
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
i.e. NVP; i.e. NVP; i.e. NVP
6-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4,5-dihydropyridazin-3(2H)-one
-
-
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0513 mM, PDE7; IC50: 0.1008 mM, PDE4
8-(4-chlorophenyl)thioguanosine 3',5'-cyclic monophosphate
-
-
8-bromoguanosine 3',5'-cyclic monophosphate
-
-
8-methoxymethyl-isobutylmethylxanthine
-
inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5
alpha-alpha'-dipyridyl
treatment of CpdA with the Fe2+-specific chelator alpha-alpha'-dipyridyl results in a nearly complete loss of activity
apigenin-7-O-glucoside
-
-
apremilast
-
CC-10004, i.e. (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide, oral phosphodiesterase-4 inhibitor, apremilast shows no marked selectivity among PDE4 isozymes
AWD 12-281
-
selective PDE4 inhibitor
ayanin
-
i.e. quercetin-3,7,4'-O-trimethylether, non-selective phosphodiesterase 1-4 inhibitor
Biochanin A
-
IC50: 0.0085 mM, more selectively inhibits PDE4 than PDE1 or PDE2
BRL-50481
-
PDE7 inhibitor
cGMP
-
5% inhibition at 0.1 mM
chamomile
-
inhibits cAMP-PDE activity
CI-1044
-
i.e. (R)-N-[9-amino-3,4,6,7-tetrahydro-4-oxo-1-phenylpyrrolo[3,2,1-j,k][1,4] benzodiazepin-3-yl]-3-pyridinecarboxamide, selective inhibitor of PDE4, administration of 160 mg/kg of CI-1044 causes perivascular and interstitial inflammation, with infiltrates of admixed neutrophils and macrophages but without evidence of vascular necrosis, PDE4 inhibitor CI-1044 induces changes of vascular tone that could lead to histological alterations in the mesenteric area
cilostazol
-
IC50: 0.0214 mM, PDE7; IC50: 0.088 mM, PDE4
cis-(+)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+/-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[(E)-4-(1H-imidazol-1-yl)but-2-enyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[2-[2-(1H-imidazol-1-yl)ethoxy]ethyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylmethyl)-benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-[(1H-imidazol-1-yl)methyl]benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[2-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[3-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(piperidin-1-ylmethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-oxopiperidin-1-yl)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(dimethylamino)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.2.0]oct-4-en-2-one hydrochloride
-
-
DC-TA 46
-
the inhibitor affects memory retention in a visible/hidden-platform water maze task. This memory impairment can be correlated to the decrease of cAMP nucleotide, due to the induction of a PDE4D cAMP-specific PDE isoform
dexamethasone
-
dexmethasone at 0.1 mg/kg inhibits the activity of PDE4
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
diosmetin
-
IC50: 0.0202 mM, PDE4
erythro-9-(2-hydroxy-3-nonyl)-adenine hydrochloride
-
erythro-9-(2-hydroxy-3-nonyl)adenine
erythro-9-[3-(2-hydroxynonyl)]-adenine
-
erythro-9-[3-(2-hydroxynonyl)]adenine
-
0.1 mM, 12% inhibition, wild-type enzyme
ethaverine
-
IC50: 0.008 mM
ethyl 2-([4-(3-carbamoylpiperazin-1-yl)-6-[4-(dimethylamino)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[(3,4-dimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-[3-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([7-ethyl-6-[(4-sulfamoylbenzyl)amino]-7H-purin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4,6-bis(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00027 mM, PDE4D; IC50: 0.00031 mM, PDE4B
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
-
IC50: 0.017 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
-
IC50: 0.015 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00088 mM, PDE4D; IC50: 0.0015 mM, PDE4B
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
-
IC50: 0.06 mM, PDE4B; IC50: 0.082 mM, PDE4D
ethyl 4-methyl-2-([4-(4-methylpiperazin-1-yl)-6-[methyl(3,4,5-trimethoxybenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(methylamino)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(piperazin-1-yl)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[methyl(3,4,5-trimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-[[4-(piperazin-1-yl)-7-(3,4,5-trimethoxybenzyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,3-thiazole-5-carboxylate
-
-
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
-
IC50: 0.025 mM, PDE4B; IC50: 0.05 mM, PDE4D
genistein
-
IC50: 0.0095 mM, PDE4
hesperetin
-
IC50: 0.0282 mM, PDE4
IBMX
non-selective PDE inhibitor
imperatorin
-
potent PFE4 inhibitor, imperatorin is significantly more active against PDE4B than PDE4A
IR-284
-
dual PDE4/PDE7 inhibitor
L-826,141
-
PDE4-selective inhibitor
luteolin-7-glucoside
-
IC50: 0.043 mM, PDB4, dual inhibition of PDE2 and PDE4
luteolin-7-O-glucoside
-
-
methylisobutylxanthine
-
-
myricetin
-
IC50: 0.0389 mM, PDE4
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
10% inhibition at 0.01 mM; 11% inhibition at 0.01 mM; lead compound for Parkinson's disease treatment
N-[3-(1H-imidazol-1-yl)propyl]-2-[cis-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,8,8a-tetrahydrophthalazin-2(1H)-yl]acetamide
-
-
O-phospho-L-serine
-
PdeA and PdeB show 59% and 73% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphoserine
O-phospho-L-tyrosine
-
PdeA and PdeB show 44% and 52% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphotyrosine
orthovanadate
-
PdeA and PdeB show 26% and 29% residual activity, respectively, for 3',5'-cAMP hydrolysis at 1 mM orthovanadate
patuletin-7-O-glucoside
-
-
PF-04957325
-
a selective PDE8 inhibitor
prunetin
-
IC50: 0.0114 mM, PDE4
quazinone
-
0.1 mM, 26% inhibition, wild-type enzyme
quercetin-3,5,7,3',4'-O-pentaacetate
-
-
quercetin-3,5,7,3',4'-O-pentamethylether
-
-
quercetin-3,7,4'-O-trimethylether
-
ayanin
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
-
-
quercetin-3-O-methylether
-
-
quinazolinamine
-
IC50: 0.34 mM, PDE4
Ro-20-1724
-
inhibition of PDE4, resulting in increased intacelular cAMP
RP-73401
-
IC50: 0.0000016 mM, PDE4
RS-25344
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-25344 about 100fold
RS-33793
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-33793 about 330fold
XAP2
-
noncompetitive inhibition, aryl-hydrocarbon receptor-interacting protein XAP2 inhibits PDE4A5 activity by XAP2 does not require any intermediate proteins. XAP2 inhibits PDE4A5 and not other PDE4 isoforms
-
Zl-n-91
-
selective PDE4 inhibitor, Zl-n-91 at 0.03, 0.3 or 3 mg/kg dose dependently inhibits PDE4 activity
3-isobutyl-1-methyl-xanthine
-
-
3-isobutyl-1-methyl-xanthine
-
-
3-isobutyl-1-methyl-xanthine
-
3-isobutyl-1-methylxanthine
-
IC50: 0.007 mM, PDE7
3-isobutyl-1-methylxanthine
-
the inhibitor binds to a subpocket that comprises key residues Ile336, Phe340, Gln369 and Phe372 of PDE54D2. This subpocket may be a common site for binding nonselective inhibitors
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
nonselective inhibitor, the PDE8A1 catalytic domain is insensitive to 3-isobutyl-1-methylxanthine inhibition
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro20-1724
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro-20-1724
Caffeine
-
-
Caffeine
-
50 mM, 30% inhibition of soluble enzyme
carboxyamidotriazole
-
non-selective inhibition
carboxyamidotriazole
-
non-selective inhibition
cilomilast
-
Cilostamide
-
IC50: 0.022 mM, PDE7; IC50: 0.0888 mM, PDE4
Cilostamide
-
inhibitor of isoform PDE3
Cilostamide
-
IC50: 0.099 mM, PDE4
dipyridamole
-
-
dipyridamole
-
inhibits PDE8 at high concentrations
dipyridamole
-
IC50: 0.013 mM
EDTA
-
0.3 mM, more than 95% inhibition
EDTA
-
PdeA and PdeB show 39% residual activity, respectively, for 3',5'-cAMP hydrolysis at 0.1 mM EDTA
erythro-9-(2-hydroxy-3-nonyl)adenine
-
7.4% inhibition at 0.1 mM
erythro-9-(2-hydroxy-3-nonyl)adenine
-
a PDE2 selective inhibitor
erythro-9-(2-hydroxy-3-nonyl)adenine
i.e. EHNA
etazolate
-
etazolate
-
IC50: 0.025 mM
IC86340
-
-
-
isobutylmethylxanthine
0.1 mM, 14% inhibition; 0.1 mM, 32% inhibition
isobutylmethylxanthine
-
a non-specific PDE inhibitor
luteolin
-
IC50: 0.0191 mM, PDE4
Milrinone
-
IC50: 0.0175 mM, PDE4; IC50: 0.0583 mM, PDE7
Milrinone
-
42% inhibition at 0.1 mM
Milrinone
0.1 mM, 93% inhibition
papaverine
-
inhibitor of isoform PDE10
papaverine
-
IC50: 0.03 mM
quercetin
-
IC50: 0.0099 mM, PDE4
Ro 20-1724
0.1 mM, 12% inhibition; 0.1 mM, 4% inhibition
Ro 20-1724
-
selective PDE4 inhibitor
Ro20-1724
-
roflumilast
-
roflumilast is approximately 10fold more potent than rolipram
roflumilast
-
PDE4-selective inhibitor
rolipram
-
IC50: 0.00045 mM, PDE4
rolipram
-
inhibitor of isoform PDE4
rolipram
-
18% inhibition at 0.1 mM
rolipram
-
inhibition of PDE4, resulting in increased intacelular cAMP
rolipram
-
competitive inhibitor of the cytosol enzyme but as a partial competitive inhibitor of the particulate enzyme. Particulate PDE-46 shows a 60fold higher affinity for rolipram than cytosolic PDE-46
rolipram
-
specific PDE4 inhibitor, complete inhibition at 0.01 mM rolipram
rolipram
-
PDE4 inhibition by rolipram can promote regression of malignant brain tumors when administered as an adjunct to established therapies
rolipram
PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram
rolipram
-
a selective inhibitor of PDE4
rolipram
0.1 mM, 4% inhibition; 0.1 mM, 7% inhibition
rolipram
-
isozyme PDE4A is only partially inhibited by 0.02 mM rolipram, whereas PDE4B is completely inhibited at this concentration
rolipram
-
PDE4 inhibitor
rolipram
-
PDE4-selective inhibitor
rolipram
-
PDE4 inhibitor
rolipram
-
the inhibitor affects memory retention in a visible/hidden-platform water maze task. This memory impairment can be correlated to the decrease of cAMP nucleotide, due to the induction of a PDE4D cAMP-specific PDE isoform
rolipram
i.e. 4-[3-(cyclopentoxyl)-4-methoxyphenyl]-2-pyrrolidinone
rolipram
-
rolipram at 0.3 mg/kg inhibits the activity of PDE4
rolipram
-
Ro 20-1724, a PDE4 selective inhibitor
SB 207499
-
SCH 351591
-
SCH51866
-
-
sildenafil
-
IC50: 3190 nM, PDE4
sildenafil
-
0.1 mM, 29% inhibition, wild-type enzyme
sildenafil
-
IC50: 0.001 mM
tadalafil
-
IC50: above 10000 nM, PDE4
theophylline
weak inhibitor
theophylline
-
non-selective inhibitor of phosphodiesterases
trequinsin
-
IC50: 0.0025 mM
vardenafil
-
IC50: 2055 nM, PDE4; IC50: 4600 nM, PDE4
vardenafil
-
PDE5 inhibitor
vinpocetine
-
inhibitor of activated isoform PDE4
vinpocetine
-
0.1 mM, 34% inhibition
zaprinast
-
10% inhibition at 0.05 mM
zaprinast
0.1 mM, 67% inhibition; 0.1 mM, 72% inhibition
zardaverine
weak inhibitor
Zn2+
-
more than 90% inhibition at 0.05 mM Zn2+ in the presence of 0.1 mM EDTA, inhibition can be greatly relieved with EDTA at 0.30 mM
Zn2+
-
the 3',5'-phosphodiesterase enzyme activities of PdeA and PdeB are reduced to 24% and 28%, respectively, by 0.05 mM Zn2+ at pH 8.0 in 50 mM Tris-HCl buffer
additional information
-
the major enzyme activity (isoform PDE8) is insensitive towards 3-isobutyl-methylxanthine
-
additional information
-
not inhibited by quercetin-3,7,3',4'-O-tetramethylether
-
additional information
-
IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7; IC50 for sildenafil is above 100000 nM and IC50 for tadalafil and vardenafil is above 10000 nM, PDE8
-
additional information
-
treatment with oxidant t-butylhydroperoxide results in release of significant amounts of interleukin-8, which is prevented by inhibition of enzyme isoforms PDE1 and PDE4
-
additional information
the enzyme is insensitive (up to 100 mM) to a variety of PDE inhibitors including rolipram, zaprinast, vinpocetine, SKF-94120, and IBMX
-
additional information
-
the enzyme is insensitive (up to 100 mM) to a variety of PDE inhibitors including rolipram, zaprinast, vinpocetine, SKF-94120, and IBMX
-
additional information
-
EHNA, milrinone, rolipram, and zaprinast, which are PDE2, PDE3, and PDE4 inhibitors, respectively, do not inhibit the PDE7B activity up to concentrations of 0.100 mM
-
additional information
zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
-
additional information
-
zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
-
additional information
no inhibition by siguazodan or zaprinast
-
additional information
-
no inhibition by siguazodan or zaprinast
-
additional information
-
not affected by Ca2+, Fe2+, Mn2+, HSCH2CH2OH, methanol, and dimethylsulfoxide
-
additional information
-
not inhibited by alpha-bisabolol, caffeic acid, ferulic acid, quinic acid, rutin, chlorogenic acid, herniarin, and umbelliferone
-
additional information
-
the oxidant t-butylhydroperoxide signifcantly increases the cytosolic calcium concentration. Inhibition of both isoforms PDE1 and PDE4 completely prevent the t-butylhydroperoxide stimulated TNF-alpha release
-
additional information
zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
-
additional information
-
zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
-
additional information
-
unlike other cAMP-specific PDEs, PDE8s are insensitive to a common nonselective PDE inhibitor, 3-isobutyl-1-methylxanthine (IBMX), but ca be inhibited by a high concentration of dipyridamole
-
additional information
-
he 3',5'-phosphodiesterase activities of PdeA and PdeB are not inhibited by theophylline, 3-isobuthyl-1-methylxanthine, and beta-glycerophosphate
-
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
-
additional information
-
not inhibited by cilostamide
-
additional information
not inhibitory: 3-isobutyl-1-methylxanthine, papaverine, theophylline; TcrPDEA1 is resistant to the typical phosphodiesterase inhibitors, such as IBMX, papaverine and theophylline
-
additional information
-
not inhibitory: 3-isobutyl-1-methylxanthine, papaverine, theophylline; TcrPDEA1 is resistant to the typical phosphodiesterase inhibitors, such as IBMX, papaverine and theophylline
-
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0.1195
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.1195 mM, PDE7
0.31
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
Homo sapiens
-
IC50: 0.31 mM, PDE4
0.00043
(2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
Homo sapiens
-
IC50: 0.00043 mM, PDE4
0.000085
(4aS,8aR)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0001
1-(2,4-dichlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0011
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0009
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0012
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0024
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0034
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0002
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0006
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0009
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.002
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0012
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0023
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
Bos taurus
-
-
0.0031
10-[4'-[(b-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
Bos taurus
-
-
0.0044
10-[4'-[(b-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
Bos taurus
-
-
0.0203 - 0.0453
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
0.00381 - 3
3-isobutyl-1-methyl-xanthine
0.0021 - 0.698
3-isobutyl-1-methylxanthine
0.0059
3-isobuytl-1-methylxanthine
Homo sapiens
-
0.0087
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
Cavia porcellus
-
PDE4
0.00018 - 0.0073
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
0.00057 - 0.0057
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.0513 - 0.1008
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0041
apigenin
Homo sapiens
-
-
0.0102
apigenin-7-O-glucoside
Homo sapiens
-
-
0.00002 - 0.000074
apremilast
0.0004 - 0.0097
AWD 12-250
0.000015 - 0.0205
AWD12-281
0.0085
Biochanin A
Cavia porcellus
-
IC50: 0.0085 mM, more selectively inhibits PDE4 than PDE1 or PDE2
0.0002
BRL-50481
Homo sapiens
-
pH and temperature not specified in the publication
19
Caffeine
Leishmania mexicana
-
particulate enzyme
2.401 - 2.91
cAMP-N1-oxide
0.00159 - 0.0262
carboxyamidotriazole
0.0005
CI-1044
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008 - 0.02
Cibacron blue
0.000101 - 0.000114
cilomilast
0.022 - 0.099
Cilostamide
0.0214 - 0.088
cilostazol
0.0000003
cis-(+)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000088
cis-(-)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000004
cis-2-[(E)-4-(1H-imidazol-1-yl)but-2-enyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000052
cis-2-[2-[2-(1H-imidazol-1-yl)ethoxy]ethyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000013
cis-2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylmethyl)-benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000007
cis-2-[4-[(1H-imidazol-1-yl)methyl]benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000013
cis-4-(3,4-dimethoxyphenyl)-2-[2-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000014
cis-4-(3,4-dimethoxyphenyl)-2-[3-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.000001
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000009
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000082
cis-4-(3,4-dimethoxyphenyl)-2-[4-(piperidin-1-ylmethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.000002
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000009
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-oxopiperidin-1-yl)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000097
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(dimethylamino)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000459
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0000164
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.2.0]oct-4-en-2-one hydrochloride
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.0005
denbufylline
Homo sapiens
-
0.0168
dioclein
Bos taurus
-
isoform PDE4, pH and temperature not specified in the publication
0.0202
diosmetin
Cavia porcellus
-
IC50: 0.0202 mM, PDE4
0.000146 - 0.042
dipyridamole
0.009
dipyridimole
Homo sapiens
-
0.015
E4021
Homo sapiens
-
-
0.128
EHNA
Trypanosoma cruzi
30°C, pH 7.5
0.217
erythro-9-(2-hydroxy-3-nonyl)-adenine hydrochloride
Trypanosoma cruzi
-
0.13
erythro-9-[3-(2-hydroxynonyl)]-adenine
Mus musculus
-
0.008
ethaverine
Trypanosoma brucei
-
IC50: 0.008 mM
0.000082
ethyl 2-([4-(3-carbamoylpiperazin-1-yl)-6-[4-(dimethylamino)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000031
ethyl 2-([4-[(3,4-dimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000076
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000083
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00013
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00012
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-[3-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 2-([7-ethyl-6-[(4-sulfamoylbenzyl)amino]-7H-purin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000063
ethyl 2-[[4,6-bis(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000056
ethyl 2-[[4-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00027 - 0.00031
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
0.017 - 0.019
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
0.015 - 0.019
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
0.00088 - 0.0015
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
0.06 - 0.082
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
0.000039
ethyl 4-methyl-2-([4-(4-methylpiperazin-1-yl)-6-[methyl(3,4,5-trimethoxybenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0001
ethyl 4-methyl-2-([4-(methylamino)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 4-methyl-2-([4-(piperazin-1-yl)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00022
ethyl 4-methyl-2-([4-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 4-methyl-2-([4-[methyl(3,4,5-trimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000006
ethyl 4-methyl-2-[[4-(piperazin-1-yl)-7-(3,4,5-trimethoxybenzyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.025 - 0.05
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
0.0095
genistein
Cavia porcellus
-
IC50: 0.0095 mM, PDE4
0.0282
hesperetin
Cavia porcellus
-
IC50: 0.0282 mM, PDE4
0.0118
hyperoside
Homo sapiens
-
-
0.000085
IR-202
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004 - 0.0000013
L-826,141
0.00421 - 0.00728
LAS-31025
0.043
luteolin-7-glucoside
Cavia porcellus
-
IC50: 0.043 mM, PDB4, dual inhibitionof PDE2 and PDE4
0.0149
luteolin-7-O-glucoside
Homo sapiens
-
-
0.04
methylisobutylxanthine
Rattus norvegicus
-
-
0.0033 - 0.0583
Milrinone
0.0389
myricetin
Cavia porcellus
-
IC50: 0.0389 mM, PDE4
0.105
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
Trypanosoma cruzi
30°C, pH 7.5
0.0021
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 30°C
0.0000143
N-[3-(1H-imidazol-1-yl)propyl]-2-[cis-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,8,8a-tetrahydrophthalazin-2(1H)-yl]acetamide
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30°C
0.561 - 1.13
N6-monobutyyl-cAMP
0.0125 - 0.174
papaverine
0.0149
patuletin-7-O-glucoside
Homo sapiens
-
-
0.0000002 - 0.0000007
PF-04957325
0.0114
prunetin
Cavia porcellus
-
IC50: 0.0114 mM, PDE4
0.0185
quercetin-3,5,7,3',4'-O-pentaacetate
Cavia porcellus
-
PDE4
0.0051
quercetin-3,5,7,3',4'-O-pentamethylether
Cavia porcellus
-
PDE4
0.0158
quercetin-3,7,4'-O-trimethylether
Cavia porcellus
-
PDE4
0.0039
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
Cavia porcellus
-
PDE4
0.0285
quercetin-3-O-methylether
Cavia porcellus
-
PDE4
0.34
quinazolinamine
Homo sapiens
-
IC50: 0.34 mM, PDE4
0.000042 - 0.0022
Ro20-1724
0.0000001 - 0.0000006
roflumilast
0.0000016
RP-73401
Homo sapiens
-
IC50: 0.0000016 mM, PDE4
0.000001 - 0.0178
RPR-73401
0.000113 - 0.000117
SB 207499
0.000105 - 0.000109
SCH 351591
0.001 - 0.0861
sildenafil
0.01
tadalafil
Homo sapiens
-
IC50: above 10000 nM, PDE4
0.0025 - 1.958
trequinsin
0.002055 - 0.0046
vardenafil
0.059 - 0.134
vinpocetine
0.01
additional information
Homo sapiens
-
IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7
-
0.0203
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0203 mM, PDE7
0.0453
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0453 mM, PDE4
0.00381
3-isobutyl-1-methyl-xanthine
Mus musculus
pH 7.4, 30°C
0.0322
3-isobutyl-1-methyl-xanthine
Homo sapiens
-
wild-type enzyme
0.175
3-isobutyl-1-methyl-xanthine
Homo sapiens
-
mutant enzyme D440N
2
3-isobutyl-1-methyl-xanthine
Leishmania mexicana
-
soluble enzyme
3
3-isobutyl-1-methyl-xanthine
Leishmania mexicana
-
particulate enzyme
0.0021
3-isobutyl-1-methylxanthine
Mus musculus
-
0.0045
3-isobutyl-1-methylxanthine
Mus musculus
-
0.007
3-isobutyl-1-methylxanthine
Bos taurus
-
IC50: 0.007 mM, PDE7
0.00737
3-isobutyl-1-methylxanthine
Homo sapiens
pH 7.4, 30°C
0.0099
3-isobutyl-1-methylxanthine
Homo sapiens
-
-
0.0658
3-isobutyl-1-methylxanthine
Homo sapiens
mutant enzyme T748A, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C
0.1262
3-isobutyl-1-methylxanthine
Trypanosoma cruzi
-
0.304
3-isobutyl-1-methylxanthine
Trypanosoma brucei
-
0.698
3-isobutyl-1-methylxanthine
Homo sapiens
wild type enzyme, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C
0.00018
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
Homo sapiens
pH not specified in the publication, 30°C
0.0066
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
Homo sapiens
pH not specified in the publication, 30°C
0.0073
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
Homo sapiens
pH not specified in the publication, 30°C
0.00057
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
Homo sapiens
pH 7.5, 25°C
0.00065
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
Homo sapiens
pH 7.5, 25°C
0.0033
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
Homo sapiens
pH 7.5, 25°C
0.0057
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
Homo sapiens
pH 7.5, 25°C
0.0513
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0513 mM, PDE7
0.1008
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.1008 mM, PDE4
0.00002
apremilast
Homo sapiens
-
recombinant isoform PDE4A4, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.00003
apremilast
Homo sapiens
-
recombinant isoform PDE4D3, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.000049
apremilast
Homo sapiens
-
recombinant isoform PDE4B2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.00005
apremilast
Homo sapiens
-
recombinant isoform PDE4C2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.000074
apremilast
Homo sapiens
-
PDE4 purified from U-937 cells, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.0004
AWD 12-250
Homo sapiens
-
mutant enzyme D440N
0.0097
AWD 12-250
Homo sapiens
-
wild-type enzyme
0.000015
AWD12-281
Homo sapiens
-
wild-type enzyme
0.0205
AWD12-281
Homo sapiens
-
mutant enzyme D440N
2.401
cAMP-N1-oxide
Homo sapiens
-
wild-type enzyme
2.91
cAMP-N1-oxide
Homo sapiens
-
mutant enzyme D440N
0.00159
carboxyamidotriazole
Mus musculus
-
enzyme from peritoneal macrophage, at pH 8.0 and 30°C
0.00509
carboxyamidotriazole
Mus musculus
-
enzyme from lung, at pH 8.0 and 30°C
0.00562
carboxyamidotriazole
Mus musculus
-
enzyme from Lewis lung carcinoma cells, at pH 8.0 and 30°C
0.00789
carboxyamidotriazole
Mus musculus
-
enzyme from L1210 cells, at pH 8.0 and 30°C
0.0112
carboxyamidotriazole
Rattus norvegicus
-
enzyme from brain, at pH 8.0 and 30°C
0.0262
carboxyamidotriazole
Mus musculus
-
enzyme from RAW264.7 cells, at pH 8.0 and 30°C
0.008
Cibacron blue
Leishmania mexicana
-
soluble enzyme
0.02
Cibacron blue
Leishmania mexicana
-
particulate enzyme
0.000101
cilomilast
Homo sapiens
-
0.000114
cilomilast
Mus musculus
-
-
0.022
Cilostamide
Bos taurus
-
IC50: 0.022 mM, PDE7
0.0888
Cilostamide
Bos taurus
-
IC50: 0.0888 mM, PDE4
0.099
Cilostamide
Homo sapiens
-
IC50: 0.099 mM, PDE4
0.0214
cilostazol
Bos taurus
-
IC50: 0.0214 mM, PDE7
0.088
cilostazol
Bos taurus
-
IC50: 0.088 mM, PDE4
0.00008
D-22888
Homo sapiens
-
wild-type enzyme
0.0048
D-22888
Homo sapiens
-
mutant enzyme D440N
0.0094
diazepam
Mus musculus
-
0.043
diazepam
Mus musculus
-
0.000146
dipyridamole
Trypanosoma cruzi
-
0.00051
dipyridamole
Mus musculus
pH 7.4, 30°C
0.0011
dipyridamole
Homo sapiens
-
-
0.00113
dipyridamole
Trypanosoma cruzi
pH 7.5, 30°C
0.00194
dipyridamole
Homo sapiens
pH 7.4, 30°C
0.0045
dipyridamole
Mus musculus
-
0.009
dipyridamole
Mus musculus
-
0.0113
dipyridamole
Trypanosoma cruzi
30°C, pH 7.5
0.013
dipyridamole
Trypanosoma brucei
-
IC50: 0.013 mM
0.015
dipyridamole
Trypanosoma cruzi
30°C, pH 7.5
0.017
dipyridamole
Trypanosoma cruzi
-
0.027
dipyridamole
Trypanosoma brucei
-
0.042
dipyridamole
Mus musculus
-
0.0013
etazolate
Trypanosoma cruzi
-
0.025
etazolate
Trypanosoma brucei
-
IC50: 0.025 mM
0.127
etazolate
Trypanosoma brucei
-
1.3
etazolate
Trypanosoma cruzi
IC50: 1.3 mM
0.00027
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.00027 mM, PDE4D
0.00031
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.00031 mM, PDE4B
0.017
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.017 mM, PDE4B
0.019
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.019 mM, PDE4D
0.015
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.015 mM, PDE4B
0.019
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.019 mM, PDE4D
0.00088
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.00088 mM, PDE4D
0.0015
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.0015 mM, PDE4B
0.06
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.06 mM, PDE4B
0.082
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.082 mM, PDE4D
0.025
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.025 mM, PDE4B
0.05
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 0.05 mM, PDE4D
0.0000004
L-826,141
Rattus norvegicus
-
isozymes PDE4B and PDE4D
0.0000013
L-826,141
Rattus norvegicus
-
isozymes PDE4C and PDE4A
0.00421
LAS-31025
Homo sapiens
-
wild-type enzyme
0.00728
LAS-31025
Homo sapiens
-
mutant enzyme D440N
0.0013
luteolin
Homo sapiens
-
-
0.0191
luteolin
Cavia porcellus
-
IC50: 0.0191 mM, PDE4
0.0033
Milrinone
Homo sapiens
-
mutant enzyme D440N
0.00635
Milrinone
Homo sapiens
-
wild-type enzyme
0.0175
Milrinone
Bos taurus
-
IC50: 0.0175 mM, PDE4
0.0583
Milrinone
Bos taurus
-
IC50: 0.0583 mM, PDE7
0.561
N6-monobutyyl-cAMP
Homo sapiens
-
wild-type enzyme
1.13
N6-monobutyyl-cAMP
Homo sapiens
-
mutant enzyme D440N
0.3
OPC-3911
Leishmania mexicana
-
soluble enzyme
0.8
OPC-3911
Leishmania mexicana
-
particulate enzyme
0.0125
papaverine
Mus musculus
-
0.01288
papaverine
Trypanosoma cruzi
-
0.022
papaverine
Mus musculus
-
0.03
papaverine
Trypanosoma brucei
-
IC50: 0.03 mM
0.111
papaverine
Trypanosoma cruzi
-
0.127
papaverine
Trypanosoma brucei
-
0.174
papaverine
Mus musculus
-
0.0000002
PF-04957325
Mus musculus
-
PDE8B, pH and temperature not specified in the publication
0.0000007
PF-04957325
Mus musculus
-
PDE8A, pH and temperature not specified in the publication
0.0099
quercetin
Cavia porcellus
-
IC50: 0.0099 mM, PDE4
0.0099
quercetin
Cavia porcellus
-
PDE4
0.000042
Ro20-1724
Homo sapiens
-
0.002
Ro20-1724
Rattus norvegicus
-
-
0.0022
Ro20-1724
Homo sapiens
-
0.0000001
roflumilast
Rattus norvegicus
-
isozymes PDE4A, PDE4B, and PDE4D
0.0000006
roflumilast
Rattus norvegicus
-
isozyme PDE4C
0.00001
rolipram
Homo sapiens
-
in 20 mM Tris-HCl at pH 7.4, 10 mM MgCl2, and 0.1 mM EDTA, at 30°C
0.000011
rolipram
Homo sapiens
-
0.0000131
rolipram
Mus musculus
-
enzyme from lung, at pH 8.0 and 30°C
0.0000149
rolipram
Mus musculus
-
enzyme from RAW264.7 cells, at pH 8.0 and 30°C
0.0000188
rolipram
Mus musculus
-
enzyme from Lewis lung carcinoma cells, at pH 8.0 and 30°C
0.000021
rolipram
Homo sapiens
-
0.00005
rolipram
Homo sapiens
-
-
0.000083
rolipram
Rattus norvegicus
-
0.0000943
rolipram
Rattus norvegicus
-
enzyme from brain, at pH 8.0 and 30°C
0.0000945
rolipram
Mus musculus
-
enzyme from peritoneal macrophage, at pH 8.0 and 30°C
0.0001
rolipram
Cavia porcellus
-
-
0.000143
rolipram
Rattus norvegicus
-
0.000148
rolipram
Homo sapiens
-
0.000149
rolipram
Homo sapiens
-
mutant enzyme A590C
0.00017
rolipram
Mus musculus
-
0.000181
rolipram
Homo sapiens
-
wild-type enzyme
0.0002
rolipram
Homo sapiens
-
mutant enzyme L391A
0.000202
rolipram
Homo sapiens
-
mutant enzyme W375Y
0.000256
rolipram
Homo sapiens
-
mutant enzyme V501A
0.000293
rolipram
Homo sapiens
-
mutant enzyme W605F
0.00032
rolipram
Homo sapiens
-
mutant enzyme F484Y
0.00038
rolipram
Mus musculus
-
-
0.0004
rolipram
Rattus norvegicus
-
-
0.00045
rolipram
Bos taurus
-
IC50: 0.00045 mM, PDE4
0.0007
rolipram
Bos taurus
-
isoform PDE4, pH and temperature not specified in the publication
0.001
rolipram
Rattus norvegicus
-
-
0.0011
rolipram
Mus musculus
-
0.0023
rolipram
Cavia porcellus
-
PDE4
0.00245
rolipram
Homo sapiens
-
mutant enzyme P595I
0.01046
rolipram
Trypanosoma cruzi
-
0.04265
rolipram
Homo sapiens
-
mutant enzyme D440A
0.08923
rolipram
Homo sapiens
-
mutant enzyme D440N
0.18
rolipram
Mus musculus
-
0.18
rolipram
Homo sapiens
-
mutant enzyme W375F
0.28
rolipram
Trypanosoma brucei
-
IC50: 0.28 mM
0.6
rolipram
Leishmania mexicana
-
particulate enzyme
0.7
rolipram
Leishmania mexicana
-
soluble enzyme
10.46
rolipram
Trypanosoma cruzi
IC50: 10.46 mM
0.000001
RPR-73401
Homo sapiens
-
wild-type enzyme
0.0178
RPR-73401
Homo sapiens
-
mutant enzyme D440N
0.000113
SB 207499
Homo sapiens
-
0.000117
SB 207499
Rattus norvegicus
-
0.000105
SCH 351591
Homo sapiens
-
0.000109
SCH 351591
Rattus norvegicus
-
0.0015
SCH51866
Homo sapiens
-
PDE7B expressed in transfected COS-7 cells
0.035
SCH51866
Mus musculus
-
0.044
SCH51866
Mus musculus
-
0.001
sildenafil
Trypanosoma brucei
-
IC50: 0.001 mM
0.00319
sildenafil
Homo sapiens
-
IC50: 3190 nM, PDE4
0.0395
sildenafil
Homo sapiens
-
wild-type enzyme
0.0861
sildenafil
Homo sapiens
-
mutant enzyme D440N
3
theophylline
Leishmania mexicana
-
particulate enzyme
30
theophylline
Leishmania mexicana
-
soluble enzyme
0.0025
trequinsin
Trypanosoma brucei
-
IC50: 0.0025 mM
1.958
trequinsin
Trypanosoma cruzi
-
0.002055
vardenafil
Homo sapiens
-
IC50: 2055 nM, PDE4
0.0046
vardenafil
Homo sapiens
-
IC50: 4600 nM, PDE4
0.059
vinpocetine
Homo sapiens
-
-
0.131
vinpocetine
Bos taurus
-
isoform PDE4, pH and temperature not specified in the publication
0.134
vinpocetine
Trypanosoma cruzi
-
0.04
zaprinast
Leishmania mexicana
-
particulate enzyme
0.0525
zaprinast
Homo sapiens
-
mutant enzyme D440N
0.728
zaprinast
Trypanosoma cruzi
-
2.8
zaprinast
Leishmania mexicana
-
soluble enzyme
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-
-
brenda
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axillae
brenda
-
isoform PDE4
brenda
-
-
brenda
-
brenda
-
-
brenda
-
brenda
-
carcinoma of salivary gland
brenda
-
-
brenda
-
PDE4
brenda
-
PDE4
brenda
-
-
brenda
-
-
brenda
-
phosphodiesterase 4 is detected in smooth muscle cells of the wall, and in the cytoplasm of luminal endothelial cells of cavernous arteries
brenda
-
brenda
-
brenda
-
brenda
-
brenda
-
presence of isoform PDE4 in nonvascular smooth musculature of the corpus carnosum
brenda
-
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
-
sinusoidal endothelial and subendothelialn layer of clitoris, presence of isoform PDE4
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
FTC133 and FTC236
brenda
-
brenda
-
lowering cyclic adenosine-3',5'-monophosphate levels by expression of a cAMP-specific phosphodiesterase decreases intrinsic pulsatile gonadotropin-releasing hormone secretion from GT1 cells
brenda
-
brenda
-
brenda
-
brenda
-
-
brenda
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
human middle ear epithelial cell
brenda
-
brenda
-
macrophage cell
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
PDE7A1
brenda
-
PDE4B. Ablation of PDE4B partially protects mice from LPS-induced shock
brenda
-
PDE4
brenda
-
gingiva-derived malignant melanoma cell, expression of variants PDE4B and PDE4D
brenda
-
-
brenda
-
monocytic cells may express different PDE4 isozymes, depending on their state of activation or differentiation. These isozymes could thus regulate intracellular cAMP levels at various stages of monocyte activation and could thereby be important in limiting the inflammatory response
brenda
-
-
brenda
-
-
brenda
-
strong expression of isoform PDE4 throughout the nervous system
brenda
-
brenda
-
-
brenda
-
human bronchial epithelial cell
brenda
-
-
brenda
-
brenda
-
-
brenda
-
cultured, PDE7
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
brenda
PDE7A1
brenda
-
-
brenda
-
-
brenda
-
abundantly present in the fibromusclular stroma as well as in glandular structures of the transition zone
brenda
-
-
brenda
-
carcinoma of salivary gland
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
brenda
-
PDE4 and PDE2
brenda
-
PDE4
brenda
-
PDE7
brenda
-
brenda
-
-
brenda
-
-
brenda
-
brenda
-
-
brenda
-
PDE4
brenda
-
-
brenda
-
brenda
-
lung epithelial cell
brenda
PDE4A expression in GH-secreting adenomas is highly variable and independent from the presence of the gsp oncogene
brenda
PDE4B expression in GH-secreting adenomas is highly variable and independent from the presence of the gsp oncogene
brenda
the level of PDE4C transcripts in gsp+ tumors is significantly higher than that found in gsp- adenomas
brenda
the level of PDE4D transcripts in gsp+ tumors is significantly higher than that found in gsp- adenomas
brenda
-
brenda
tumor tissues from patients with isolated micronodular adrenocortical disease and no mutations in the coding PDE8B sequence or any other related genes (PRKAR1A, PDE11A) show downregulated PDE8B expression compared to normal adrenal cortex. PDE8B is a PDE gene linked to isolated micronodular adrenocortical disease. It is a candidate causative gene for other adrenocortical lesions linked to the cAMP signaling pathway and possibly for tumors in other tissues
brenda
-
-
brenda
-
of newborn mice
brenda
-
brenda
-
brenda
-
brenda
weak activity
brenda
-
-
brenda
-
brenda
-
-
brenda
-
brenda
weak activity
brenda
-
-
brenda
-
brenda
-
PDE4
brenda
-
PDE7
brenda
-
PDE8
brenda
-
-
brenda
-
PDE7A1 co-localizes with PKA II in the Golgi centrosome region
brenda
-
-
brenda
-
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
brenda
-
brenda
-
brenda
and skeletal muscle, predominant expression
brenda
isoform PDE4B5 is brain-specific
brenda
parietal, frontal, temporal cortex, hippocampus, striatum, thalamus, hypothalamus, substantia nigra, nucleus accumbens, cerebellum
brenda
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
-
PDE4B5 is brain-specific
brenda
PDE7A1
brenda
in the brain, PDE4D11 expression levels increase in the cerebellum, but decrease in the hippocampus with progressive age
brenda
-
isoforms PDE4A, PDE4D, PDE7A, PDE8A, PDE8B show an age-related increase or decrease in mRNA expression in at least 1 of the 4 brain regions examined (hippocampus, cortex, striatum, and cerebellum). mRNA expression of isoforms PDE7A, PDE7B does not change with age. Age-related increases in PDE11A4, PDE8A3, PDE8A4/5, and PDE1C1 protein expression are confirmed in hippocampus of old versus young rodents, as are age-related increases in PDE8A3 protein expression in the striatum
brenda
-
-
brenda
-
brenda
-
brenda
high activity
brenda
-
of normal and triethyltin-intoxicated rats
brenda
-
isoforms PDE4A, PDE4D, PDE7A, PDE8A, PDE8B show an age-related increase or decrease in mRNA expression in at least 1 of the 4 brain regions examined (hippocampus, cortex, striatum, and cerebellum). mRNA expression of isoforms PDE7A, PDE7B does not change with age. Age-related increases in PDE11A4, PDE8A3, PDE8A4/5, and PDE1C1 protein expression are confirmed in hippocampus of old versus young rodents, as are age-related increases in PDE8A3 protein expression in the striatum
brenda
-
-
brenda
-
-
brenda
-
brenda
-
brenda
-
-
brenda
-
brenda
-
brenda
PDE4D11 expression levels increase in the cerebellum with progressive age
brenda
-
PDE4 is observed in the nonvascular smooth musculature of the corpus cavernosum clitoris, sinusoidal endothelial and subendothelial layers, and nerve fibers innervating the tissue
brenda
-
presence of isoform PDE4 in nonvascular smooth musculature of the corpus carnosum, in sinusoidal endothelial and subendothelial layers, and nerve fiber innervating the tissue
brenda
-
-
brenda
-
-
brenda
-
-
brenda
-
age-related increases in isoform PDE8A3 protein expression are confirmed in hippocampus of old versus young rodents
brenda
-
-
brenda
-
age-related increases in isoform PDE8A3 protein expression are confirmed in hippocampus of old versus young rodents
brenda
-
-
brenda
-
brenda
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
-
-
brenda
-
brenda
-
brenda
-
-
brenda
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
PDE7A2
brenda
lowest expression in heart
brenda
-
neonatal cardiac myocyte
brenda
-
-
brenda
-
-
brenda
-
brenda
PDE4D11 expression levels decrease in the hippocampus with progressive age
brenda
-
age-related increases in isoforms PDE8A3, PDE8A4/5 and PDE1C1 protein expression are confirmed in hippocampus of old versus young rodents
brenda
-
age-related increases in isoforms PDE8A3, PDE8A4/5 protein expression are confirmed in hippocampus of old versus young rodents. Relative to young rats, the hippocampi of old rats demonstrate strikingly decreased phosphorylation of GluR1, CaMKIIalpha, and CaMKIIbeta, decreased expression of the transmembrane AMPA regulatory proteins gamma2 (a.k.a. stargazin) and gamma8, and increased trimethylation of H3K27. Expression of isoforms of PDE8A4/5, PDE8A3 correlate with these functional endpoints in young but not old rats
brenda
-
brenda
-
-
brenda
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
PDE7A1
brenda
-
brenda
-
the phosphodiesterase 4B4 isoform present in kidney tissue from spontaneously hypertensive rats, hypertensive Dahl salt-sensitive rats, and Dahl salt-resistant rats, phosphodiesterase 4B expression is detected in the renal vasculature, proximal tubules, and distal tubules
brenda
-
-
brenda
-
brenda
-
brenda
weak activity
brenda
-
-
brenda
-
brenda
highest expression level
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
-
-
brenda
-
brenda
-
brenda
-
-
brenda
-
brenda
-
brenda
-
PDE4
brenda
-
-
brenda
-
brenda
-
weak activity
brenda
PDE7A1
brenda
-
-
brenda
-
brenda
-
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
-
-
brenda
-
brenda
most highly expressed in pancreas followed by brain, heart, thyroid, skeletal muscle, eye, ovary, submaxillary gland, epididymus, and liver
brenda
PDE7A1
brenda
-
-
brenda
-
brenda
weak activity
brenda
-
brenda
high activity
brenda
-
PDE4
brenda
-
PDE7
brenda
-
-
brenda
-
-
brenda
-
immature cell. Almost all PDE4D variants are expressed throughout the early postpartum period with a specific increase in PDE4 activity in both soluble and particulate fraction of 20 day old Sertoli cells
brenda
-
isolated from 10-, 20-, and 30-days-old rats. Specific increase in PDE4 activity in both the soluble and particulate subcellular fractions of 20-days-old Sertoli cells. Almost all the PDE4D isoforms, known as the main cAMP-regulated rolipramsensitive PDE in Sertoli cells, are expressed throughout the early postpartum period, whereas only the short PDE4D isoforms (PDE4D1 and PDE4D2) are transcriptionally regulated by FSH. The subcellular distribution and expression of PDE4D proteins are unaffected by the developmental status of the Sertoli cells. Only the expression of short PDE4D1 appears to be upregulated by FSH and only in 20-days-old Sertoli cells, which suggests phenotype-dependent differential regulation of Pde4d1 mRNA translation
brenda
-
-
brenda
-
brenda
-
brenda
-
brenda
-
PDE7
brenda
and brain, predominant expression
brenda
-
brenda
-
weak activity
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order
brenda
PDE7A2
brenda
-
-
brenda
-
brenda
-
brenda
-
brenda
-
-
brenda
-
of central cavernous arteries
brenda
-
-
brenda
-
-
brenda
-
brenda
highest expression level
brenda
-
brenda
-
brenda
-
brenda
-
brenda
-
PDE4 is present in young and adult gland. During development PDE4 is the major PDE
brenda
-
-
brenda
-
brenda
-
brenda
high activity
brenda
-
PDE8
brenda
-
brenda
-
weak activity
brenda
highest expression in testis, followed by eye, liver, skeletal muscle, heart, 7-day embryo, kidney, ovary, and brain in decreasing order. In testis PDE8 is expressed in the seminiferous epithelium in a stage-specific manner
brenda
-
brenda
high activity
brenda
-
PDE8
brenda
-
brenda
-
brenda
numerous PDE4D gene-derived variants including PDE4D3, PDE4D5, PDE4D7, PDE4D8, and PDE4D9
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
-
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
PDE IVB is not detected in Placenta, liver, kidney, or pancreas
brenda
additional information
-
PDE IVB is not detected in Placenta, liver, kidney, or pancreas
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
determination of tissue distribution and level of the different PDE isozymes via quantitative real-time PCR expresssion analysis, overview
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
additional information
mRNA expression levels of PDEs 4A, 4B, 4C and 4D are significantly higher in rats than in humans. Higher PDE4 expression levels are correlated with a higher enzyme activity level in rat leukocytes
brenda
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additional information
-
PDE4 is a cAMP-specific PDE which has four subfamilies, A thru D, that include over 50 isoforms
malfunction
deletion of cpdA results in the accumulation of intracellular cAMP and altered regulation of Pseudomonas aeruginosa virulence traits
malfunction
-
PDE4 inhibition together with transforming growth factor-beta1 results in augmented PGE2 production together with increased expression of COX mRNA and protein. inhibitors may attenuate fibroblast activities that can lead to fibrosis, PDE4 inhibitors may be particularly effective in the presence of transforming growth factor-beta1-induced fibroblast stimulation
malfunction
a pdeHDELTA/pdeLDELTA mutant shows reduced conidiation, exhibits dramatically increased cAMP levels relative to the wild-type, and is completely defective in virulence
malfunction
deletion of cpdA results in the accumulation of intracellular cAMP and altered regulation of Pseudomonas aeruginosa virulence traits. The cpdA mutant has a cAMP-independent small-colony, slow-growth phenotype
malfunction
-
effects of acute hypoxia on cAMP accumulation induced by PDE inhibitors in oxygen-specific chemosensors, the carotid bodies and in non-chemosensitive CB-related structures: carotid arteries and superior cervical ganglia, overview. Acute hypoxia enhances the effects of IBMX and PDE4 inhibitors on cAMP accumulation in carotid arteries and bodies, while in superior cervical ganglia In SCG, acute hypoxia reduces cAMP accumulation induced by all the four PDE inhibitors
malfunction
loss of PdeH leads to increased accumulation of intracellular cAMP during vegetative and infectious growth. Furthermore, the pdeHD shows 2-3fold enhanced conidiation, precocious appressorial development, loss of surface dependency during pathogenesis, and highly reduced in planta growth and host colonization. A pdeHDELTA/pdeLDELTA mutant shows reduced conidiation, exhibits dramatically increased cAMP levels relative to the wild-type, and is completely defective in virulence
malfunction
-
PDE8B KO mice have elevated levels of urinary corticosterone in both basal and stressed conditions compared with their littermate wild-type controls. PDE8B KO mice exhibit adrenal hypersensitivity toward adrenocorticotropin. PDE8B gene ablation increases mRNA expressions of StAR protein and MC2R
malfunction
-
in cultured smooth muscle cells, isoform PDE1C deficiency or PDE1 inhibition attenuates smooth muscle cell proliferation and migration
malfunction
-
in cultured smooth muscle cells, isoform PDE1C deficiency or PDE1 inhibition attenuates smooth muscle cell proliferation and migration
malfunction
-
in cultured smooth muscle cells, isoform PDE1C deficiency or PDE1 inhibition attenuates smooth muscle cell proliferation and migration
metabolism
cyclic AMP-dependent pathways mediate the communication between external stimuli and the intracellular signaling machinery, thereby influencing important aspects of cellular growth, morphogenesis and differentiation. Crucial to proper function and robustness of these signaling cascades is the strict regulation and maintenance of intracellular levels of cAMP through a fine balance between biosynthesis, by adenylate cyclases, and hydrolysis, by cAMP phosphodiesterases
metabolism
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PKA, EPAC1, and PDE4D differentially regulate humanarterial endothelial cell vascular endothelial cadherin-based structures, overview. Protein-protein interactions between EPAC1 and PDE4D serve to foster their integration into vascular endothelial cadherin-based complexes and allow robust local regulation of EPAC1-based stabilization of vascular endothelial cadherin-based adhesions
metabolism
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a transmembrane-adenylyl-cyclase-cAMP-protein kinase A cascade modulated by isoform PDE1C is critical in regulating platelet-derived growth factor -receptor-beta degradation
metabolism
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a transmembrane-adenylyl-cyclase-cAMP-protein kinase A cascade modulated by isoform PDE1C is critical in regulating platelet-derived growth factor -receptor-beta degradation
metabolism
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a transmembrane-adenylyl-cyclase-cAMP-protein kinase A cascade modulated by isoform PDE1C is critical in regulating platelet-derived growth factor -receptor-beta degradation
physiological function
CpdA is required for cAMP homeostasis and virulence factor regulation, CpdA affects vfr expression and Vfr protein levels and production of virulence factors ExoS, ToxA, and protease IV
physiological function
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phosphodiesterase 4 contributes to maintenance of retinal vascular tone
physiological function
cAMP-specific PDE 4 isoforms underpin compartmentalized cAMP signalling in mammalian cells through targeting to specific signalling complexes. Phosphorylation of PDE4A5 by MK2 confers the amplification of intracellular cAMP accumulation in response to adenylate cyclase activation by attenuating a major desensitization system to cAMP. Long PDE4 isoforms thus provide a novel node for cross-talk between the cAMP and p38 MAPK signalling systems at the level of MK2
physiological function
CpdA possesses 3',5'-cAMP phosphodiesterase activity in vitro and that it utilizes an iron-dependent catalytic mechanism. The cAMP-dependent transcription factor Vfr directly regulates cpdA expression in response to intracellular cAMP accumulation, thus providing a feedback mechanism for controlling cAMP levels and fine-tuning virulence factor expression. CpdA affects vfr expression and Vfr protein levels. CpdA affects production of virulence factors ExoS, ToxA, and protease IV
physiological function
expendable PdeL function
physiological function
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importance of PDE8s in cAMP regulation of steroid production. PDE8A plays an important role in regulating a pool of cAMP that promotes testicular steroidogenesis. PDE8B regulates adrenocorticotropin-stimulated AZF steroidogenesis by both short- and long-term mechanisms
physiological function
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in cardiac myocytes coupling of PDE4 members to the beta2 adrenergic receptor regulates several aspects of beta2 adrenergic signaling. Inhibition of PDE4 increases cAMP in response to activation of beta2 adrenergic receptors, but has no effect on beta1 adrenergic signaling, demonstrating the selectivity of PDE association. Recruitment of PDE4 to the beta2 adrenergic receptor allows PDE4 to act locally and hydrolyze cAMP produced in response to activation of this receptor, modulating its downstream effects. PDE4 activation is regulated via phosphorylation by PKA in the UCR or phosphorylation by ERK in the C-terminus, depending on the individual isoform. The regulated release of ATP from erythrocytes occurs via a defined signaling pathway and requires increases in cAMP. It is well recognized that cAMP is a critical second messenger in diverse signaling pathways. In all cells increases in cAMP are localized and regulated by the activity of phosphodiesterases, PDEs. The subcellular localization of PDEs is recognized to be a key mechanism for compartmentalization of cyclic nucleotide signaling. PDEs within these cells regulate the compartmentalization of cAMP signaling allowing for specific cell responses. The subcellular location of PDEs is critical for coupling these enzymes to specific signal transduction pathways, which permit specific PDEs to regulate local increases in cAMP produced by activation of ligand specific receptor
physiological function
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PDE4D regulates both the activity and subcellular localization of EPAC1, mechanism for regulated EPAC1 signaling in these cells, overview
physiological function
PDEH is necessary for proper aerial hyphal growth. PdeH-dependent biphasic regulation of cAMP levels during early and late stages of appressorial development. PdeH-mediated sustainance and dynamic regulation of cAMP signaling during Magnaporthe oryzae development is crucial for successful establishment and spread of the blast disease in rice. The PdeH activity is a key regulator of asexual and pathogenic development in Magnaporthe oryzae
physiological function
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the autocrine production of cAMP and extracellular cAMP-specific phosphodiesterase is an important constituent of the mechanism controlling the motile behavior of the plasmodium
physiological function
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the PDE4-catalyzed hydrolysis of cAMP consists of two reaction stages: cAMP hydrolysis and bridging hydroxide ion regeneration. The stage 1 includes the binding of cAMP in the active site, nucleophilic attack of the bridging hydroxide ion on the phosphorus atom of cAMP, cleavage of O3'-P phosphoesteric bond of cAMP, protonation of the departing O3' atom, and dissociation of hydrolysis product, AMP. The stage 2 includes the binding of solvent water molecules with the metal ions in the active site and regeneration of the bridging hydroxide ion. The dissociation of the hydrolysis product is found to be rate-determining for the enzymatic reaction process
physiological function
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constitutive signaling of the overexpressed HA-tagged 5-hydroxytryptamine4(b) receptor in HEK293 cells is regulated predominantly by cAMP-specific phosphodiesterase PDE4,with a secondary role for dual specific phosphodiesterase PDE3 that is unmasked in the presence of PDE4 inhibition. Overexpressed PDE4D3 and PDE3A1, and to a smaller extent PDE4D5 co-immunoprecipitate constitutively with the 5-hydroxytryptamine4(b) receptor. Phosphodiesterase activity measurements in immunoprecipitates of the 5-hydroxytryptamine4(b) receptor confirm the association of PDE4D3 with the receptor and provide evidence that the activity of this phophodiesterase may be increased upon receptor stimulation with 5-hydroxytryptamine
physiological function
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isoform PDE4B is involved in beta-adrenergic signaling in the heart. Genetic ablation of PDE4B disrupts beta-adrenergic signaling-induced cAMP transients at the sarcolemma but not in the bulk cytosol of cardiomyocytes. PDE4B regulates beta1-adrenergic signaling-, but not beta2-adrenergic signaling- or PGE2-induced responses. PDE4B shows selective effects on protein kinase A-mediated phosphorylation patterns. PDE4B limits the proein kinase A-mediated phosphorylation of key players in excitation-contraction coupling that reside in the sarcolemmal compartment, including L-type Ca2+ channels and ryanodine receptors, but not phosphorylation of distal cytosolic proteins. beta1-Adrenergic signaling- but not beta2-adrenergic signaling-ligation induced protein kinase A-dependent activation of PDE4B and interruption of this negative feedback with protein kinase A inhibitors increase sarcolemmal cAMP
physiological function
mutation in cAMP-specific phosphodiesterase RegA in cells lacking either G protein Galpha2 or Galpha4 subunits has no major effects on developmental morphology but enriches the distribution of the Galpha mutant cells to the prespore/prestalk border in chimeric aggregates. The loss of RegA function has no effect on Galpha4-mediated folate chemotaxis. The RegA gene disruption in cells lacking Galpha4 results in a substantial rescue and acceleration of spore production. This rescue in sporulation requires cell autonomous signaling. Intercellular signals from strains lacking RegA increase the expression of the prestalk gene ecmB and accelerate the vacuolization of stalk cells. Intercellular signaling from the strain lacking both Galpha4 and RegA do not induce ecmA gene expression indicating cell-type specificity in the promotion of prestalk cell development. RegA gene disruption in a Galpha4 overexpression strain does not result in precocious sporulation or stalk cell development
physiological function
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phosphodiesterase 4B mediates Streptococcus pneumoniae-induced mucin gene MUC5AC up-regulation by inhibiting the expression of a negative regulator MKP-1, which in turn leads to enhanced MAPK ERK activation and subsequent up-regulation of MUC5AC. PDE4B inhibits MKP-1 expression in a cAMP-PKA-dependent manner. PDE4-specific inhibitor rolipram inhibits Streptomyces pneumoniae-induced MUC5AC up-regulation both in vitro and in vivo. PDE4B plays a critical role in MUC5AC induction. Topical and post-infection administration of rolipram into the middle ear potently inhibits Streptomyces pneumoniae-induced MUC5AC up-regulation
physiological function
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hepatic isoforms PDE4A, B and D play a causal role in the development of liver injury and fibrosis
physiological function
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cAMP-phosphodiesterase 1C plays a role in regulating growth factor receptor stability, vascular smooth muscle cell growth, migration, and neointimal hyperplasia
physiological function
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cAMP-phosphodiesterase 1C plays a role in regulating growth factor receptor stability, vascular smooth muscle cell growth, migration, and neointimal hyperplasia
physiological function
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cAMP-phosphodiesterase 1C plays a role in regulating growth factor receptor stability, vascular smooth muscle cell growth, migration, and neointimal hyperplasia
physiological function
isoform PDE4D7 is important in prostate cancer progression and ischemic stroke
physiological function
the enzyme exhibits protection against oxidative damage and participates in the regulation of the carbon metanolism
physiological function
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the enzyme participates in biofilm formation
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