Page last updated: 2024-08-07 15:21:03

cGMP-dependent 3',5'-cyclic phosphodiesterase

A cGMP-dependent 3,5-cyclic phosphodiesterase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00408]

Synonyms

EC 3.1.4.17;
Cyclic GMP-stimulated phosphodiesterase;
CGS-PDE;
cGSPDE

Research

Bioassay Publications (44)

TimeframeStudies on this Protein(%)All Drugs %
pre-19906 (13.64)18.7374
1990's6 (13.64)18.2507
2000's12 (27.27)29.6817
2010's17 (38.64)24.3611
2020's3 (6.82)2.80

Compounds (43)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
my 5445Homo sapiens (human)IC50100.000022
theophyllineHomo sapiens (human)IC50210.000011
cilostamideHomo sapiens (human)IC5050.002512
dipyridamoleHomo sapiens (human)IC503.123346
9-(2-hydroxy-3-nonyl)adenineHomo sapiens (human)IC5066.933313
amrinoneHomo sapiens (human)IC50656.000045
1-methyl-3-isobutylxanthineHomo sapiens (human)IC5028.000033
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)IC5040.000011
milrinoneHomo sapiens (human)IC50162.255689
papaverineHomo sapiens (human)IC5014.766733
pentoxifyllineHomo sapiens (human)IC50100.000011
proxyphyllineHomo sapiens (human)Ki600.000011
pyrimethamineHomo sapiens (human)IC5073.500011
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinoneHomo sapiens (human)IC50390.000011
rolipramHomo sapiens (human)IC50116.8544616
rolipramHomo sapiens (human)Ki200.000011
sulmazoleHomo sapiens (human)IC50200.000011
trequinsinHomo sapiens (human)IC501.950212
zardaverineHomo sapiens (human)IC5084.5246213
2-chloroadenosineHomo sapiens (human)IC5010.000011
cycloguanilHomo sapiens (human)IC505.800011
cladribineHomo sapiens (human)IC5010.000011
enoximoneHomo sapiens (human)IC50520.000011
imazodanHomo sapiens (human)IC50680.000066
bufrolinHomo sapiens (human)IC5080.000011
tadalafilHomo sapiens (human)IC5064.4507616
clofarabineHomo sapiens (human)IC503.120011
9-(2-hydroxy-3-nonyl)adenineHomo sapiens (human)IC502.145033
9-(2-hydroxy-3-nonyl)adenineHomo sapiens (human)Ki1.900022
9-(2-hydroxy-3-nonyl)adenineHomo sapiens (human)IC501.628844
cilomilastHomo sapiens (human)IC5046.9197212
rp 73401Homo sapiens (human)IC5036.7900110
roflumilastHomo sapiens (human)IC50124.2002110
4,5-dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2h)-pyridazinoneHomo sapiens (human)IC50446.666766
1,3-dihydro-7,8-dimethyl-2h-imidazo(4,5-b)quinolin-2-oneHomo sapiens (human)IC5020.000022
N-(1,3-benzodioxol-5-ylmethyl)-6-chloro-4-quinazolinamineHomo sapiens (human)IC50100.000012
(2R,3S)-EHNA hydrochlorideHomo sapiens (human)IC500.800011
pf 04217903Homo sapiens (human)IC5010.000011
an2728Homo sapiens (human)IC503,630.000011
chf6001Homo sapiens (human)IC501.000011
sildenafilHomo sapiens (human)IC5026.3371919
zaprinastHomo sapiens (human)IC5079.250044
vardenafilHomo sapiens (human)IC507.0667312
bl 4162aHomo sapiens (human)IC5034.000022
bay 60-7550Homo sapiens (human)IC500.00321010

Enables

This protein enables 11 target(s):

TargetCategoryDefinition
magnesium ion bindingmolecular functionBinding to a magnesium (Mg) ion. [GOC:ai]
3',5'-cyclic-AMP phosphodiesterase activitymolecular functionCatalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277]
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitymolecular functionCatalysis of the reaction: nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate; catalytic activity is increased in the presence of cGMP. [GOC:mah]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
zinc ion bindingmolecular functionBinding to a zinc ion (Zn). [GOC:ai]
cAMP bindingmolecular functionBinding to cAMP, the nucleotide cyclic AMP (adenosine 3',5'-cyclophosphate). [GOC:ai]
cGMP bindingmolecular functionBinding to cGMP, the nucleotide cyclic GMP (guanosine 3',5'-cyclophosphate). [GOC:ai]
TPR domain bindingmolecular functionBinding to a tetratricopeptide repeat (TPR) domain of a protein, the consensus sequence of which is defined by a pattern of small and large hydrophobic amino acids and a structure composed of helices. [GOC:mah]
phosphate ion bindingmolecular functionBinding to a phosphate ion. [GOC:jl]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [GOC:jl]
3',5'-cyclic-GMP phosphodiesterase activitymolecular functionCatalysis of the reaction: 3',5'-cyclic GMP + H2O = GMP + H+. [RHEA:16957]

Located In

This protein is located in 10 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
mitochondrial outer membranecellular componentThe outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai]
mitochondrial inner membranecellular componentThe inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai]
endoplasmic reticulumcellular componentThe irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732]
Golgi apparatuscellular componentA membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
presynaptic membranecellular componentA specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194]
perinuclear region of cytoplasmcellular componentCytoplasm situated near, or occurring around, the nucleus. [GOC:jid]

Active In

This protein is active in 7 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
mitochondrial inner membranecellular componentThe inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai]
perinuclear region of cytoplasmcellular componentCytoplasm situated near, or occurring around, the nucleus. [GOC:jid]
mitochondrial outer membranecellular componentThe outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai]
synaptic membranecellular componentA specialized area of membrane on either the presynaptic or the postsynaptic side of a synapse, the junction between a nerve fiber of one neuron and another neuron or muscle fiber or glial cell. [GOC:BHF, PMID:20410104]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
mitochondrial matrixcellular componentThe gel-like material, with considerable fine structure, that lies in the matrix space, or lumen, of a mitochondrion. It contains the enzymes of the tricarboxylic acid cycle and, in some organisms, the enzymes concerned with fatty acid oxidation. [GOC:as, ISBN:0198506732]

Involved In

This protein is involved in 22 target(s):

TargetCategoryDefinition
negative regulation of transcription by RNA polymerase IIbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH]
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
regulation of cGMP-mediated signalingbiological processAny process that modulates the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, GOC:dph, GOC:tb]
cAMP-mediated signalingbiological processAn intracellular signaling cassette that starts with production of cyclic AMP (cAMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling]
cGMP-mediated signalingbiological processAn intracellular signaling cassette that starts with production of cyclic GMP (cGMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling]
cellular response to macrophage colony-stimulating factor stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a macrophage colony-stimulating factor stimulus. [GOC:yaf, PMID:14687666]
negative regulation of vascular permeabilitybiological processAny process that reduces the extent to which blood vessels can be pervaded by fluid. [GOC:jl]
positive regulation of vascular permeabilitybiological processAny process that increases the extent to which blood vessels can be pervaded by fluid. [GOC:jl]
regulation of cAMP-mediated signalingbiological processAny process which modulates the frequency, rate or extent of cAMP-mediated signaling. [GOC:jl]
cGMP catabolic processbiological processThe chemical reactions and pathways resulting in the breakdown of cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators]
positive regulation of inflammatory responsebiological processAny process that activates or increases the frequency, rate or extent of the inflammatory response. [GOC:ai]
establishment of endothelial barrierbiological processThe establishment of a barrier between endothelial cell layers, such as those in the brain, lung or intestine, to exert specific and selective control over the passage of water and solutes, thus allowing formation and maintenance of compartments that differ in fluid and solute composition. [GOC:dph]
cellular response to mechanical stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mechanical stimulus. [GOC:mah]
cellular response to cAMPbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:mah]
cellular response to cGMPbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cGMP (cyclic GMP, guanosine 3',5'-cyclophosphate) stimulus. [GOC:mah]
cellular response to transforming growth factor beta stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a transforming growth factor beta stimulus. [GOC:ecd, PMID:15451575]
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaybiological processAny process that stops, prevents or reduces the frequency, rate or extent of an adenylate cyclase-activating G protein-coupled receptor signaling pathway. [GOC:hjd, PMID:19246489]
cellular response to 2,3,7,8-tetrachlorodibenzodioxinebiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a 2,3,7,8-tetrachlorodibenzodioxine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23196670]
positive regulation of gene expressionbiological processAny process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018]
negative regulation of cGMP-mediated signalingbiological processAny process that decreases the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, GOC:dph, GOC:tb]
negative regulation of cAMP-mediated signalingbiological processAny process which stops, prevents, or reduces the frequency, rate or extent of cAMP-mediated signaling. [GOC:jl]
regulation of mitochondrion organizationbiological processAny process that modulates the frequency, rate or extent of a process involved in the formation, arrangement of constituent parts, or disassembly of a mitochondrion. [GOC:dph, GOC:tb]