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Information on EC 3.1.4.17 - 3',5'-cyclic-nucleotide phosphodiesterase and Organism(s) Bos taurus
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3.1.4.17 3',5'-cyclic-nucleotide phosphodiesteraseIUBMB Comments
Acts on 3',5'-cyclic AMP, 3',5'-cyclic dAMP, 3',5'-cyclic IMP, 3',5'-cyclic GMP and 3',5'-cyclic CMP.
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Word Map
- 3.1.4.17
- cyclase
- adenylate
- rolipram
- cardiac
- artery
- pka
- guanosine
- agonist
-
camp-dependent
- forskolin
- ibmx
-
contractile
-
adenylyl
- theophylline
- milrinone
- cilostazol
- platelet
- isoproterenol
- prostaglandin
- striatal
-
schizophrenia
- 3-isobutyl-1-methylxanthine
-
vasodilator
- zaprinast
- papaverine
-
inotropic
- dipyridamole
-
spiny
-
camp-mediated
-
beta-adrenergic
-
guanylyl
- sildenafil
- 3',5'-monophosphate
-
prkar1a
-
cardiotonic
- phosphodiesterase-4
- amrinone
- isobutylmethylxanthine
- trifluoperazine
- isoprenaline
-
bronchodilator
- methylxanthines
-
low-km
-
antilipolytic
- ehna
- aminophylline
- roflumilast
- molecular biology
- vardenafil
- medicine
- tadalafil
-
camp-elevating
The taxonomic range for the selected organisms is: Bos taurus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Synonyms
pde4d, cyclic nucleotide phosphodiesterase, pde10a, camp phosphodiesterase, pde3a, pde3b, pde2a, camp-pde, phosphodiesterase 3, pde11a, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
3',5'-cyclic nucleoside monophosphate phosphodiesterase
-
-
-
-
3',5'-cyclonucleotide phosphodiesterase
-
-
-
-
3',5'-nucleotide phosphodiesterase
-
-
-
-
3':5'-CNP
-
-
-
-
3':5'-cyclic nucleotide 5'-nucleotidohydrolase
-
-
-
-
61 kDa Cam-PDE
-
-
-
-
63 kDa Cam-PDE
-
-
-
-
Cam-PDE 1A
-
-
-
-
Cam-PDE 1B
-
-
-
-
Cam-PDE 1C
-
-
-
-
CGB-PDE
-
-
-
-
CGIP1
-
-
-
-
CGIPDE1
-
-
-
-
cGMP-binding cGMP-specific phosphodiesterase
-
-
-
-
CGS-PDE
-
-
-
-
cGSPDE
-
-
-
-
cyclic 3',5'-mononucleotide phosphodiesterase
-
-
-
-
cyclic 3',5'-nucleotide phosphodiesterase
-
-
-
-
cyclic 3',5'-phosphodiesterase
-
-
-
-
cyclic 3',5-nucleotide monophosphate phosphodiesterase
-
-
-
-
Cyclic GMP stimulated phosphodiesterase
-
-
-
-
cyclic nucleotide phosphodiesterase
-
-
-
-
DPDE1
-
-
-
-
DPDE2
-
-
-
-
DPDE3
-
-
-
-
DPDE4
-
-
-
-
Dunce protein
-
-
-
-
GMP-PDE alpha
-
-
-
-
GMP-PDE beta
-
-
-
-
GMP-PDE delta
-
-
-
-
GMP-PDE gamma
-
-
-
-
HCP1
-
-
-
-
High-affinity cAMP phosphodiesterase
-
-
-
-
Learning/ memory process protein
-
-
-
-
Low-affinity cAMP phosphodiesterase
-
-
-
-
MMPDE8
-
-
-
-
nucleoside 3',5'-cyclic phosphate diesterase
-
-
-
-
nucleoside-3',5-monophosphate phosphodiesterase
-
-
-
-
p17 protein
-
-
-
-
P2A
-
-
-
-
PDE V-B1
-
-
-
-
PDE V-C1
-
-
-
-
PDE1
PDE21
-
-
-
-
PDE32
-
-
-
-
PDE43
-
-
-
-
PDE46
-
-
-
-
PDEase
-
-
-
-
PDEase regA
-
-
-
-
phosphodiesterase, cyclic 3',5'-nucleotide
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-
-
-
TM22
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of phosphoric ester
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
3',5'-cyclic-nucleotide 5'-nucleotidohydrolase
Acts on 3',5'-cyclic AMP, 3',5'-cyclic dAMP, 3',5'-cyclic IMP, 3',5'-cyclic GMP and 3',5'-cyclic CMP.
CAS REGISTRY NUMBER
COMMENTARY
9040-59-9
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
additional information
?
-
-
muscarinic antagonists acting possibly as inverse agonists on M2/M3 muscarinic acetylcholine receptors anchored to sarcolemma membranes can initiate a new signal transducing cascade leading to inhibition of PDEI, which produces a simultaneous rise in both cAMP and cGMP intracellular levels in tracheal smooth muscle
-
-
?
additional information
?
-
-
real-time monitoring of PDE2 activity by a fluorescent cAMP sensor shows that activation of PDE2 results in a rapid decrease of intracellular cAMP from high micromolar to sub-micromolar range within a few seconds. High catalytic activity and fast action in regulating cAMP signaling in a physiological system
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
-
muscarinic antagonists acting possibly as inverse agonists on M2/M3 muscarinic acetylcholine receptors anchored to sarcolemma membranes can initiate a new signal transducing cascade leading to inhibition of PDEI, which produces a simultaneous rise in both cAMP and cGMP intracellular levels in tracheal smooth muscle
-
-
?
additional information
?
-
-
real-time monitoring of PDE2 activity by a fluorescent cAMP sensor shows that activation of PDE2 results in a rapid decrease of intracellular cAMP from high micromolar to sub-micromolar range within a few seconds. High catalytic activity and fast action in regulating cAMP signaling in a physiological system
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
Mg2+
Ca2+
-
differential effect on isozymes, activation only in complex with calimodulin, overeview
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0001 mM, PDE3A; IC50: 0.00028 mM, PDE3B
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000019 mM, PDE3B; IC50: 0.0.0209 mM, PDE2; IC50: 0.1129 mM, PDE1
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000015 mM, PDE3B; IC50: 0.0429 mM, PDE1; IC50: 0.0523 mM, PDE2
8-methoxymethyl-isobutylmethylxanthine
-
inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5, is 3times more potent in inhibiting PDE5 than PDE1
Cilostamide
-
IC50: 0.000027 mM, PDE3A; IC50: 0.00005 mM, PDE3B; IC50: 0.0125 mM, PDE2
cilostazol
-
IC50: 0.0002 mM, PDE3A; IC50: 0.00038 mM, PDE3B; IC50: 0.0452 mM, PDE2
dioclein
-
potent selective and calmodulin-independent inhibitor of PDE1, competitive inhibitor for cGMP hydrolysis by PDE1 in basal-activated (1 mM EGTA) and calmodulin-activated (18 nM calmodulin with 0.01 mM CaCl2) states. Dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold), PDE3 (19fold), PDE4 (11fold), and PDE5 (16fold)
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Calmodulin
-
differential effect on isozymes, activation only in complex with Ca2+, overview
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000062
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
-
0.0000003
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
-
0.00000022
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
-
0.00055
dioclein
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
0.00062
dioclein
-
isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0001 - 0.00028
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.00000034 - 0.1129
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
0.00000032 - 0.0523
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0152
8-methoxymethyl-isobutylmethylxanthine
Bos taurus
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
0.0032
nimodipine
Bos taurus
-
isoform PDE1, pH and temperature not specified in the publication
0.0001
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0001 mM, PDE3A
0.00028
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.00028 mM, PDE3B
0.00000034
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor
0.0000019
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0000019 mM, PDE3B
0.0209
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0.0209 mM, PDE2
0.1129
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.1129 mM, PDE1
0.00000032
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor
0.0000015
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0000015 mM, PDE3B
0.0429
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0429 mM, PDE1
0.0523
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0523 mM, PDE2
0.00144
dioclein
Bos taurus
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
0.00247
dioclein
Bos taurus
-
isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication
0.185
vinpocetine
Bos taurus
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
assay procedure of calmodulin-dependent cyclic nucleotide phosphodiesterase
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
-
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
real-time monitoring of PDE2 activity by a fluorescent cAMP sensor shows that activation of PDE2 results in a rapid decrease of intracellular cAMP from high micromolar to sub-micromolar range within a few seconds
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
inhibition of PDE1 is involved in the cGMP-dependent protein kinase-mediated vasorelaxant effect of dioclein in human saphenous vein
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). PDE2A_BOVIN
921
0
103228
Swiss-Prot
other Location (Reliability: 4)
PDE1A_BOVIN
530
0
60843
Swiss-Prot
other Location (Reliability: 1)
PDE1B_BOVIN
534
0
61006
Swiss-Prot
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
60000
63000
additional information
60000
-
x * 63000, bovine brain, x * 60000, bovine heart, lung and brain, SDS-PAGE
63000
-
x * 63000, bovine brain, x * 60000, bovine heart, lung and brain, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
oligomer
-
x * 63000, bovine brain, x * 60000, bovine heart, lung and brain, SDS-PAGE
additional information
-
PDE1 exists as tissue-specific and immunological distinct isozymes, overview
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
0°C, EGTA, rapid loss of activity, inactivation retarded by bovine serum albumin, stability of Ca2+-dependent enzyme
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
molecular biology
-
assay procedure of calmodulin-dependent cyclic nucleotide phosphodiesterase
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Yamamoto, T.; Manganiello, V.C.; Vaughan, M.
Purification and characterization of cyclic GMP-stimulated cyclic nucleotide phosphodiesterase from calf liver. Effects of divalent cations on activity
J. Biol. Chem.
258
12526-12533
1983
Bos taurus
Sharma, R.K.; Wang, J.H.
Isolation of bovine brain calmodulin-dependent cyclic nucleotide phosphodiesterase isozymes
Methods Enzymol.
159
582-594
1988
Bos taurus
Kincaid, R.L.; Vaughan, M.
Purification and properties of calmodulin-activated cyclic nucleotide phosphodiesterase from mammalian brain
Methods Enzymol.
159
557-573
1988
Bos taurus, Mammalia
Hansen, R.S.; Charbonneau, H.; Beavo, J.A.
Purification of calmodulin-stimulated cyclic nucleotide phosphodiesterase by monoclonal antibody affinity chromatography
Methods Enzymol.
159
543-557
1988
Bos taurus, Rattus norvegicus
Chaudry, P.S.; Casillas, E.R.
Calmodulin-stimulated cyclic nucleotide phosphodiesterases in plasma membranes of bovine epididymal spermatozoa
Arch. Biochem. Biophys.
262
439-444
1988
Bos taurus
Pannbacker, R.G.; Fleischman, D.E.; Reed, D.W.
Cyclic nucleotide phosphodiesterase: high activity in a mammalian photoreceptor
Science
175
757-758
1972
Bos taurus
Sharma, R.K.; Kalra, J.
Characterization of calmodulin-dependent cyclic nucleotide phosphodiesterase isoenzymes
Biochem. J.
299
97-100
1994
Bos taurus
Sudo, T.; Tachibana, K.; Toga, K.; Tochizawa, S.; Inoue, Y.; Kimura, Y.; Hidaka, H.
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity
Biochem. Pharmacol.
59
347-356
2000
Bos taurus
Sharma, R.K.
Diversity of calcium action in regulation of mammalian calmodulin-dependent cyclic nucleotide phosphodiesterase
Indian J. Biochem. Biophys.
40
77-91
2003
Bos taurus, Mammalia
Guerra de Gonzalez, L.; Gonzalez de Alfonzo, R.; Lippo de Becemberg, I.; Alfonzo, M.J.
Cyclic nucleotide-dependent phosphodiesterases (PDEI) inhibition by muscarinic antagonists in bovine tracheal smooth muscle
Biochem. Pharmacol.
68
651-658
2004
Bos taurus
Nikolaev, V.O.; Gambaryan, S.; Engelhardt, S.; Walter, U.; Lohse, M.J.
Real-time monitoring of the PDE2 activity of live cells: hormone-stimulated cAMP hydrolysis is faster than hormone-stimulated cAMP synthesis
J. Biol. Chem.
280
1716-1719
2005
Bos taurus
Sharma, R.K.
Assay and purification of calmodulin-dependent cyclic nucleotide phosphodiesterase and isozyme separation
Methods Mol. Biol.
312
325-342
2006
Bos taurus
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
Eur. J. Pharmacol.
620
78-83
2009
Bos taurus, Homo sapiens
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