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Information on EC 3.1.4.17 - 3',5'-cyclic-nucleotide phosphodiesterase and Organism(s) Homo sapiens and UniProt Accession O00408

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EC Tree
     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.4 Phosphoric-diester hydrolases
                3.1.4.17 3',5'-cyclic-nucleotide phosphodiesterase
IUBMB 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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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: O00408
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
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
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
PDE2A
3',5'-cyclic nucleoside monophosphate phosphodiesterase
-
-
-
-
3',5'-cyclic nucleotide phosphodiesterase
-
-
3',5'-cyclic nucleotide phosphodiesterase 11A
-
-
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
-
-
-
-
cAMP phosphodiesterase
-
-
cAMP-PDE
-
-
cAMP-specific PDE
-
-
CGB-PDE
-
-
-
-
CGIP1
-
-
-
-
CGIPDE1
-
-
-
-
cGMP-binding cGMP-specific phosphodiesterase
-
-
-
-
cGMP-inhibited PDE
-
-
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
cyclic nucleotide phosphodiesterase PDE3
-
-
DPDE1
-
-
-
-
DPDE2
-
-
-
-
DPDE3
-
-
-
-
DPDE4
-
-
-
-
Dunce protein
-
-
-
-
GMP-PDE alpha
-
-
-
-
GMP-PDE beta
-
-
-
-
GMP-PDE delta
-
-
-
-
GMP-PDE gamma
-
-
-
-
h-prune
-
-
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
-
-
-
-
PDE10
-
-
PDE10A
PDE11
-
-
PDE11A
PDE11A1
-
-
PDE11A2
-
-
PDE11A3
-
-
PDE11A4
-
-
PDE1A
PDE1B
PDE1C
PDE21
-
-
-
-
PDE2A1
-
-
PDE2A2
-
-
PDE2A3
-
-
PDE32
-
-
-
-
PDE3A
PDE3B
PDE4
-
-
PDE43
-
-
-
-
PDE46
-
-
-
-
PDE5
-
-
PDE9A6
-
isoform
PDE9X-100
-
isoform
PDE9X-120
-
isoform
PDE9X-175
-
isoform
PDEase
-
-
-
-
PDEase regA
-
-
-
-
phosphodiesterase 10
-
-
phosphodiesterase 11
-
-
phosphodiesterase 2A
-
-
phosphodiesterase 3
-
-
phosphodiesterase type 3A
-
-
phosphodiesterase, cyclic 3',5'-nucleotide
-
-
-
-
TM22
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
-
-
-
-
PATHWAY SOURCE
PATHWAYS
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 hide
9040-59-9
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
show the reaction diagram
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
3',5'-cGMP + H2O
5'-GMP
show the reaction diagram
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
show the reaction diagram
-
-
-
-
?
cAMP + H2O
AMP
show the reaction diagram
-
-
?
cGMP + H2O
GMP
show the reaction diagram
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
show the reaction diagram
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
3',5'-cGMP + H2O
5'-GMP
show the reaction diagram
-
highest affinity for 3',5'-cGMP
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Calmodulin
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
required
Zn2+
-
is coordinated to His529, His563, Asp564, Asp674, and two phosphate oxygen atoms
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3-isobutyl-1-methylxanthine
broad-spectrum PDE inhibitor
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
-
IC50: 0.0043 mM, PDE2
(2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol
-
-
(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
(6aS,9aR)-3-benzyl-2-(biphenyl-4-ylmethyl)-5-methyl-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(3H)-one
-
comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context
(Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate
-
time-dependent and irreversible inactivation of PDE3A
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
1-(2-chlorophenyl)-4-methyl-8-[(morpholin-4-yl)methyl][1,2,4]triazolo[4,3-a]quinoxaline
-
compound shows good combined potency, acceptable brain uptake and high selectivity for both PDE2 and PDE10 enzymes. In microdosing experiment in rats, the compound shows preferential distribution in brain areas
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
3',5'-cGMP
-
-
3'-benzyl-2'-(biphenyl-4-ylmethyl)-5'-methyl-3'H-spiro[cyclopentane-1,7'-imidazo[2,1-b]purin]-4'(5'H)-one
-
comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
3-isobutyl-1-methylxanthine
3-isobutyl-8-(methoxymethyl)-1-methyl-3,9-dihydro-1H-purine-2,6-dione
-
i.e. 8MM-IBMX, comparison of inhibitory effect on several recombinant human PDE isoforms
5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
5-methyl-2-[4-(trifluoromethyl)benzyl]-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(1H)-one
-
i.e. SCH51866, comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
8-methoxymethyl(-3-isobutyl-1-)methylxanthine
-
8-methoxymethyl-3-isobutyl-1-methylxanthine
0.02 mM selectively inhibits PDE1
adenosine
-
-
Cilostamide
cilostazol
dioclein
-
dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold)
dipyridamole
EHNA
-
a selective PDE2 inhibitor
erythro-9-(2-hydroxy-3-nonyl)adenine
-
IC50: 0.00061 mM for wild-type enzyme
isobutylmethylxanthine
-
inhibits with micromolar potency
Milrinone
-
MP-10
-
-
N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
-
TAK-915
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
-
-
N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
papaverine
PQ-10
-
-
quinazolinamine
rolipram
RP-73401
sildenafil
tadalafil
TAK-915
-
i.e. 2 N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
TP-10
-
-
vardenafil
vinpocetine
zaprinast
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cGMP
PDE2 is stimulated by cGMP
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000079 - 0.032
3',5'-cAMP
0.00002 - 0.034
3',5'-cGMP
0.0017 - 1.6
cAMP
0.0013 - 1
cGMP
additional information
additional information
-
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.3 - 0.52
3',5'-cAMP
4.2
3',5'-cGMP
-
catalytic domain of PDE2A (PDE2A residues 578-919), enzyme expressed in Escherichia coli
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0434
(Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate
-
in 45 mM HEPES (pH 7.2), 20 mM MgCl2, and 4 mM MES, at 25°C
0.00002 - 0.00003
3',5'-cGMP
0.000039 - 0.000056
cilostazol
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0043
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
Homo sapiens
-
IC50: 0.0043 mM, PDE2
0.0023
(2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol
Homo sapiens
-
isoform PDE2, pH and temperature not specified in the publication
0.000006 - 0.015
(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
0.0000071
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000031
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000028
1-(2-chlorophenyl)-4-methyl-8-[(morpholin-4-yl)methyl][1,2,4]triazolo[4,3-a]quinoxaline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.005 - 0.037
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
0.02654 - 0.0402
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
0.0000017
5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000024
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0012
cAMP
Homo sapiens
-
IC50: 1200 nM, PDE11A4
0.000059 - 0.00056
cGMP
0.00013 - 0.221
Cilostamide
0.0382 - 0.1
dioclein
0.00034 - 0.00084
dipyridamole
0.00061
erythro-9-(2-hydroxy-3-nonyl)adenine
Homo sapiens
-
IC50: 0.00061 mM for wild-type enzyme
0.0127
IBMX
Homo sapiens
-
0.007
Milrinone
Homo sapiens
-
0.000061
N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000054
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000077
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000011
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000054
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000012
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000098
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000012
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00001
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000034
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000051
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000051
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000066
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0038
N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000024
N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00048
N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.01 - 0.241
quinazolinamine
0.15
rolipram
Homo sapiens
-
IC50: 0.15 mM for wild-type enzyme
0.05 - 0.13
RP-73401
0.00035 - 0.0038
sildenafil
0.000015 - 0.01
tadalafil
0.000061
TAK-915
Homo sapiens
-
at pH 7.4 and 25°C
0.000121 - 0.00084
vardenafil
0.0223
vinpocetine
Homo sapiens
-
IC50: 0.0223 mM
0.00816
zaprinast
Homo sapiens
-
IC50: 0.00816 mM, PDE4A4
0.01
additional information
Homo sapiens
-
IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
PDE2A
UniProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
parietal, frontal, temporal cortex, hippocampus, striatum, thalamus, hypothalamus, substantia nigra, nucleus accumbens, cerebellum
Manually annotated by BRENDA team
-
glioblastoma cell, expression of isoform PDE1C and lower levels of isoforms PDE2, PDE3, PDE4, and PDE5
Manually annotated by BRENDA team
-
lung epithelial cell
Manually annotated by BRENDA team
-
activity is one-tenth compared to normal tissue
Manually annotated by BRENDA team
-
phosphodiesterase 3 is exclusively detected in smooth muscle cells of the wall, no activity in vascular endothelial layer
Manually annotated by BRENDA team
-
external layer of
Manually annotated by BRENDA team
-
predominant expression of isoform PDE1A
Manually annotated by BRENDA team
-
epithelial cells and macrophages
Manually annotated by BRENDA team
-
myometrial cell, level of isoform PDE1C decreases in all conditions that inhibit proliferation
Manually annotated by BRENDA team
-
main distribution in glandular and subglandular areas
Manually annotated by BRENDA team
-
of central cavernous arteries
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
PDE9A localizes to the cytosol in the bladder
Manually annotated by BRENDA team
-
PDE9A localizes to the nucleus in the brain
Manually annotated by BRENDA team
-
PDE2A1
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
-
in adipocytes, insulin induces formation of macromolecular complexes containing signaling molecules such as IRS-1, PI3K and PKB, proteins involved in PDE3B activation/phosphorylation
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
PDE2A_HUMAN
941
0
105717
Swiss-Prot
Mitochondrion (Reliability: 5)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
100000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
105000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
110000
-
isoform PDE11A2, gel filtration
124000
-
-
140000
190000
-
isoform PDE11A4, gel filtration
220000
-
isoform PDE11A1, gel filtration
55000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
56000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
60000
-
2 * 60000
61000
-
2 * 61000
64000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
65800
x * 65800, deduced from gene sequence
66000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
72000
-
x * 72000, splice variant PDE1C1, x * 75000, splice variant PDE1C3
75000
78000
-
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1
78100
x * 78100, deduced from gene sequence
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
-
in adipocytes, insulin induces formation of macromolecular complexes containing signaling molecules such as IRS-1, PI3K and PKB, proteins involved in PDE3B activation/phosphorylation
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
hanging drop vapor diffusion method, using 30% (w/v) PEG 3350, 0.1 M Tris pH 7.5, and 0.2 M MgCl2
-
vapor diffusion method, crystal structure of the catalytic domain of PDE2A (PDE2A residues 578-919) determined at 1.7 A resolution
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D106A
-
mutation does not influence h-prune phosphodiesterase activity
D811A
-
activity towards 3',5'-cGMP is similar to wild-type activity, activity towards 3',5'-cAMP is less than 50% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram
D811A/Q812I
-
activity towards 3',5'-cGMP and 3',5'-cAMP is less than 50% of wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram
I826V
-
activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram
L858M
-
activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram
L858S
-
activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity
L907A
-
activity towards 3',5'-cGMP is less than 10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity
M847L
-
activity towards 3',5'-cGMP is less than10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity
Q812I
-
activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity towards 3',5'-cAMP is similar to wild-type activity. Slight increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine, decrease in IC50-value for rolipram
Q812P
-
activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity
Q812P/T819Y
-
activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity
T819Y
-
activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram
Y827A
-
activity towards 3',5'-cGMP is less than 10% of wild-type activity, activity with 3',5'-cAMP is less than 20% of wild-type activity
Y827F
-
activity towards 3',5'-cGMP is less than 50% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity. Increase in IC50-value for erythro-9-(2-hydroxy-3-nonyl)adenine and rolipram
Y827F/L907A
-
activity towards 3',5'-cGMP is less than 20% of wild-type activity, activity with 3',5'-cAMP is less than 10% of wild-type activity
Y827M
-
activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity
Y827V
-
activity towards 3',5'-cAMP and 3',5'-cGMP is less than 10% of wild-type activity
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
2500-3000fold
-
anion exchange chromatography
-
Mono Q column chromatography and Superdex 200 gel filtration
-
nickel resin column chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
baculovirus expression system, PDE11A4
-
Epac1-camps-PDE3A fusion protein is expressed in HEK-293 cells
expressed in a baculovirus/insect cell Sf9 system
-
expression by using a baculovirus expression system
-
expression in COS-7 cells
-
expression in insect cells or in Escherichia coli
-
expression in NIH3006 murine fibroblasts and baculovirus-infected Sf9 insect cells
-
expression in Saccharomyces cerevisiae
PDE3A expression in HEK-293 cells on the plasma membrane
-
the catalytic domain is expressed in Sf9 insect cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
epinephrine infusion stimulates skeletal muscle PDE2A expression
-
PDE9A mRNA is elevated in the aged human hippocampus with dementia when there is a history of traumatic brain injury
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Grant, P.G.; Colman, R.W.
Purification and characterization of a human platelet cyclic nucleotide phosphodiesterase
Biochemistry
23
1801-1807
1984
Homo sapiens
Manually annotated by BRENDA team
Yu, J.; Wolda, S.L.; Frazier, A.L.B.; Florio, V.A.; Martins, T.J.; Snyder, P.B.; Harris, E.A.S.; McCaw, K.N.; Farrell, C.A.; Steiner, B.; Bentley J.K.; Beavo, J.A.; Ferguson, K.; Gelinas, R.
Identification and characterization of a human calmodulin-stimulated phosphodiesterase PDE1B1
Cell. Signal.
9
519-529
1997
Homo sapiens (Q01064), Homo sapiens
Manually annotated by BRENDA team
Kotera, J.; Fujishige, K.; Yuasa, K.; Omori, K.
Characterization and phosphorylation of PDE10A2, a novel alternative splice variant of human phosphodiesterase that hydrolyzes cAMP and cGMP
Biochem. Biophys. Res. Commun.
261
551-557
1999
Homo sapiens
Manually annotated by BRENDA team
Leroy, M.J.; Degerman, E.; Taira, M.; Murata, T.; Wang, L.H.; Movsesian, M.A.; Meacci, E.; Manganiello, V.C.
Characterization of two recombinant PDE3 (cGMP inhibited cyclic nucleotide phosphodiesterase) isoforms, RcGIP1 and HcGIP2, expressed in NIH 3006 murine fibroblasts and Sf9 insect cells
Biochemistry
35
10194-10202
1996
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
O'Grady, S.M.; Jiang, X.; Maniak, P.J.; Birmachu, W.; Scribner, L.R.; Bulbulian, B.; Gullikson, G.W.
Cyclic AMP-dependent Cl secretion is regulated by multiple phosphodiesterase subtypes in human colonic epithelial cells
J. Membr. Biol.
185
137-144
2002
Homo sapiens
Manually annotated by BRENDA team
Hetman, J.M.; Robas, N.; Baxendale, R.; Fidock, M.; Phillips, S.C.; Soderling, S.H.; Beavo, J.A.
Cloning and characterization of two splice variants of human phosphodiesterase 11A
Proc. Natl. Acad. Sci. USA
97
12891-12895
2000
Homo sapiens (Q9HCR9), Homo sapiens
Manually annotated by BRENDA team
Dolci, S.; Belmonte, A.; Santone, R.; Giorgi, M.; Pellegrini, M.; Carosa, E.; Piccione, E.; Lenzi, A.; Jannini, E.A.
Subcellular localization and regulation of type-1C and type-5 phosphodiesterases
Biochem. Biophys. Res. Commun.
341
837-846
2006
Homo sapiens
Manually annotated by BRENDA team
Iffland, A.; Kohls, D.; Low, S.; Luan, J.; Zhang, Y.; Kothe, M.; Cao, Q.; Kamath, A.V.; Ding, Y.H.; Ellenberger, T.
Structural determinants for inhibitor specificity and selectivity in PDE2A using the wheat germ in vitro translation system
Biochemistry
44
8312-8325
2005
Homo sapiens
Manually annotated by BRENDA team
D'Angelo, A.; Garzia, L.; Andre, A.; Carotenuto, P.; Aglio, V.; Guardiola, O.; Arrigoni, G.; Cossu, A.; Palmieri, G.; Aravind, L.; Zollo, M.
Prune cAMP phosphodiesterase binds nm23-H1 and promotes cancer metastasis
Cancer Cell
5
137-149
2004
Homo sapiens
Manually annotated by BRENDA team
Ahlstrom, M.; Pekkinen, M.; Huttunen, M.; Lamberg-Allardt, C.
Cyclic nucleotide phosphodiesterases (PDEs) in human osteoblastic cells; the effect of PDE inhibition on cAMP accumulation
Cell. Mol. Biol. Lett.
10
305-319
2005
Homo sapiens
Manually annotated by BRENDA team
Bischoff, E.
Potency, selectivity, and consequences of nonselectivity of PDE inhibition
Int. J. Impot. Res.
16
S11-S14
2004
Homo sapiens
Manually annotated by BRENDA team
Loughney, K.; Taylor, J.; Florio, V.A.
3',5'-cyclic nucleotide phosphodiesterase 11A: localization in human tissues
Int. J. Impot. Res.
17
320-325
2005
Homo sapiens
Manually annotated by BRENDA team
Pomara, G.; Morelli, G.
Inhibition of phosphodiesterase 11 (PDE11) impact on sperm quality
Int. J. Impot. Res.
17
385-386
2005
Homo sapiens
Manually annotated by BRENDA team
Weeks, J.L.; Zoraghi, R.; Beasley, A.; Sekhar, K.R.; Francis, S.H.; Corbin, J.D.
High biochemical selectivity of tadalafil, sildenafil and vardenafil for human phosphodiesterase 5A1 (PDE5) over PDE11A4 suggests the absence of PDE11A4 cross-reaction in patients
Int. J. Impot. Res.
17
5-9
2005
Homo sapiens
Manually annotated by BRENDA team
Hambleton, R.; Krall, J.; Tikishvili, E.; Honeggar, M.; Ahmad, F.; Manganiello, V.C.; Movsesian, M.A.
Isoforms of cyclic nucleotide phosphodiesterase PDE3 and their contribution to cAMP hydrolytic activity in subcellular fractions of human myocardium
J. Biol. Chem.
280
39168-39174
2005
Homo sapiens
Manually annotated by BRENDA team
D'Andrea, M.R.; Qiu, Y.; Haynes-Johnson, D.; Bhattacharjee, S.; Kraft, P.; Lundeen, S.
Expression of PDE11A in normal and malignant human tissues
J. Histochem. Cytochem.
53
895-903
2005
Homo sapiens
Manually annotated by BRENDA team
Das, S.B.; Sharma, R.K.
Potential role of calmodulin-dependent phosphodiesterase in human brain tumor (Review)
Oncol. Rep.
14
1059-1063
2005
Homo sapiens
Manually annotated by BRENDA team
Oelke, M.; Hedlund, P.; Albrecht, K.; Ellinghaus, P.; Stief, C.G.; Jonas, U.; Andersson, K.E.; Uckert, S.
Expression of cAMP and cGMP-phosphodiesterase isoenzymes 3, 4, and 5 in the human clitoris: immunohistochemical and molecular biology study
Urology
67
1111-1116
2006
Homo sapiens
Manually annotated by BRENDA team
Waldkirch, E.; Uckert, S.; Yildirim, H.; Sohn, M.; Jonas, U.; Stief, C.G.; Andersson, K.E.; Hedlund, P.
Cyclic AMP-specific and cyclic GMP-specific phosphodiesterase isoenzymes in human cavernous arteries--immunohistochemical distribution and functional significance
World J. Urol.
23
405-410
2005
Homo sapiens
Manually annotated by BRENDA team
Weeks, J.L.; Zoraghi, R.; Francis, S.H.; Corbin, J.D.
N-terminal domain of phosphodiesterase-11A4 (PDE11A4) decreases affinity of the catalytic site for substrates and tadalafil, and is involved in oligomerization
Biochemistry
46
10353-10364
2007
Homo sapiens
Manually annotated by BRENDA team
Surapisitchat, J.; Jeon, K.I.; Yan, C.; Beavo, J.A.
Differential regulation of endothelial cell permeability by cGMP via phosphodiesterases 2 and 3
Circ. Res.
101
811-818
2007
Homo sapiens
Manually annotated by BRENDA team
Uckert, S.; Oelke, M.; Stief, C.G.; Andersson, K.E.; Jonas, U.; Hedlund, P.
Immunohistochemical distribution of cAMP- and cGMP-phosphodiesterase (PDE) isoenzymes in the human prostate
Eur. Urol.
49
740-745
2006
Homo sapiens
Manually annotated by BRENDA team
Dunkern, T.R.; Hatzelmann, A.
Characterization of inhibitors of phosphodiesterase 1C on a human cellular system
FEBS J.
274
4812-4824
2007
Homo sapiens
Manually annotated by BRENDA team
Gross-Langenhoff, M.; Hofbauer, K.; Weber, J.; Schultz, A.; Schultz, J.E.
cAMP is a ligand for the tandem GAF domain of human phosphodiesterase 10 and cGMP for the tandem GAF domain of phosphodiesterase 11
J. Biol. Chem.
281
2841-2846
2006
Homo sapiens (Q9HCR9), Homo sapiens (Q9Y233), Homo sapiens
Manually annotated by BRENDA team
Bender, A.T.; Beavo, J.A.
PDE1B2 regulates cGMP and a subset of the phenotypic characteristics acquired upon macrophage differentiation from a monocyte
Proc. Natl. Acad. Sci. USA
103
460-465
2006
Homo sapiens
Manually annotated by BRENDA team
Brown, D.M.; Hutchison, L.; Donaldson, K.; MacKenzie, S.J.; Dick, C.A.; Stone, V.
The effect of oxidative stress on macrophages and lung epithelial cells: the role of phosphodiesterases 1 and 4
Toxicol. Lett.
168
1-6
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Hung, S.H.; Liu, A.H.; Pixley, R.A.; Francis, P.; Williams, L.D.; Matsko, C.M.; Barnes, K.D.; Sivendran, S.; Colman, R.F.; Colman, R.W.
A new nonhydrolyzable reactive cGMP analogue, (Rp)-guanosine-3,5-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate, which targets the cGMP binding site of human platelet PDE3A
Bioorg. Chem.
36
141-147
2008
Homo sapiens
Manually annotated by BRENDA team
Herget, S.; Lohse, M.J.; Nikolaev, V.O.
Real-time monitoring of phosphodiesterase inhibition in intact cells
Cell. Signal.
20
1423-1431
2008
Homo sapiens (P27815)
Manually annotated by BRENDA team
Siuciak, J.A.
The role of phosphodiesterases in schizophrenia: therapeutic implications
CNS Drugs
22
983-993
2008
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Santos-Silva, A.J.; Cairrao, E.; Morgado, M.; Alvarez, E.; Verde, I.
PDE4 and PDE5 regulate cyclic nucleotides relaxing effects in human umbilical arteries
Eur. J. Pharmacol.
582
102-109
2008
Homo sapiens (O00408), Homo sapiens (P54750), Homo sapiens (Q01064), Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Keravis, T.; Lugnier, C.
Cyclic nucleotide phosphodiesterases (PDE) and peptide motifs
Curr. Pharm. Des.
16
1114-1125
2010
Homo sapiens
Manually annotated by BRENDA team
Lu, H.; Goren, A.C.; Zhan, C.G.
Characterization of the structures of phosphodiesterase 10 binding with adenosine 3',5'-monophosphate and guanosine 3',5'-monophosphate by hybrid quantum mechanical/molecular mechanical calculations
J. Phys. Chem. B
114
7022-7028
2010
Homo sapiens
Manually annotated by BRENDA team
Penmatsa, H.; Zhang, W.; Yarlagadda, S.; Li, C.; Conoley, V.G.; Yue, J.; Bahouth, S.W.; Buddington, R.K.; Zhang, G.; Nelson, D.J.; Sonecha, M.D.; Manganiello, V.; Wine, J.J.; Naren, A.P.
Compartmentalized cyclic adenosine 3',5'-monophosphate at the plasma membrane clusters PDE3A and cystic fibrosis transmembrane conductance regulator into microdomains
Mol. Biol. Cell
21
1097-1110
2010
Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Lakics, V.; Karran, E.H.; Boess, F.G.
Quantitative comparison of phosphodiesterase mRNA distribution in human brain and peripheral tissues
Neuropharmacology
59
367-374
2010
Homo sapiens (O00408), Homo sapiens (P54750), Homo sapiens (Q01064), Homo sapiens (Q13370), Homo sapiens (Q14123), Homo sapiens (Q14432), Homo sapiens (Q9HCR9), Homo sapiens (Q9Y233), Homo sapiens
Manually annotated by BRENDA team
Adderley, S.P.; Sprague, R.S.; Stephenson, A.H.; Hanson, M.S.
Regulation of cAMP by phosphodiesterases in erythrocytes
Pharmacol. Rep.
62
475-482
2010
Homo sapiens
Manually annotated by BRENDA team
Weninger, S.; Van Craenenbroeck, K.; Cameron, R.T.; Vandeput, F.; Movsesian, M.A.; Baillie, G.S.; Lefebvre, R.A.
Phosphodiesterase 4 interacts with the 5-HT4(b) receptor to regulate cAMP signaling
Cell. Signal.
26
2573-2582
2014
Homo sapiens
Manually annotated by BRENDA team
Andres, J.I.; Buijnsters, P.; De Angelis, M.; Langlois, X.; Rombouts, F.; Trabanco, A.A.; Vanhoof, G.
Discovery of a new series of [1,2,4]triazolo[4,3-a]quinoxalines as dual phosphodiesterase 2/phosphodiesterase 10 (PDE2/PDE10) inhibitors
Bioorg. Med. Chem. Lett.
23
785-790
2013
Homo sapiens
Manually annotated by BRENDA team
Mikami, S.; Kawasaki, M.; Ikeda, S.; Negoro, N.; Nakamura, S.; Nomura, I.; Ashizawa, T.; Kokubo, H.; Hoffman, I.D.; Zou, H.; Oki, H.; Uchiyama, N.; Hiura, Y.; Miyamoto, M.; Itou, Y.; Nakashima, M.; Iwashita, H.; Taniguchi, T.
Discovery of a novel series of pyrazolo[1,5-a]pyrimidine-based phosphodiesterase 2A inhibitors structurally different from N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the treatment of cognitive disorders
Chem. Pharm. Bull.
65
1058-1077
2017
Homo sapiens
Manually annotated by BRENDA team
Patel, N.S.; Klett, J.; Pilarzyk, K.; Lee, D.I.; Kass, D.; Menniti, F.S.; Kelly, M.P.
Identification of new PDE9A isoforms and how their expression and subcellular compartmentalization in the brain change across the life span
Neurobiol. Aging
65
217-234
2018
Homo sapiens, Mus musculus
Manually annotated by BRENDA team