A high affinity cAMP-specific and IBMX-insensitive 3,5-cyclic phosphodiesterase 8A that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60658]
EC 3.1.4.53
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (30.00) | 29.6817 |
| 2010's | 7 (70.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| cilostamide | Homo sapiens (human) | IC50 | 50.0025 | 1 | 2 |
| dipyridamole | Homo sapiens (human) | IC50 | 2.6333 | 1 | 3 |
| 9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | IC50 | 66.9333 | 1 | 3 |
| 1-methyl-3-isobutylxanthine | Homo sapiens (human) | IC50 | 384.0000 | 2 | 2 |
| milrinone | Homo sapiens (human) | IC50 | 50.1500 | 1 | 2 |
| papaverine | Homo sapiens (human) | IC50 | 25.0000 | 1 | 1 |
| pentoxifylline | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| rolipram | Homo sapiens (human) | IC50 | 127.6669 | 3 | 13 |
| trequinsin | Homo sapiens (human) | IC50 | 1.9502 | 1 | 2 |
| zardaverine | Homo sapiens (human) | IC50 | 84.5246 | 2 | 13 |
| tadalafil | Homo sapiens (human) | IC50 | 72.2294 | 4 | 14 |
| 9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| cilomilast | Homo sapiens (human) | IC50 | 50.2760 | 1 | 11 |
| rp 73401 | Homo sapiens (human) | IC50 | 36.7900 | 1 | 10 |
| roflumilast | Homo sapiens (human) | IC50 | 124.2002 | 1 | 10 |
| sildenafil | Homo sapiens (human) | IC50 | 31.7128 | 6 | 16 |
| vardenafil | Homo sapiens (human) | IC50 | 7.4274 | 2 | 11 |
This protein enables 5 target(s):
| Target | Category | Definition |
|---|---|---|
| 3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
| kinase binding | molecular function | Binding to a kinase, any enzyme that catalyzes the transfer of a phosphate group. [GOC:jl] |
| protein kinase activator activity | molecular function | Binds to and increases the activity of a protein kinase, an enzyme which phosphorylates a protein. [GOC:ai] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| 3',5'-cyclic-GMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic GMP + H2O = GMP + H+. [RHEA:16957] |
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|---|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|---|---|
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| nucleus | cellular component | A 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] |
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|---|---|
| cAMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of the nucleotide cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate). [ISBN:0198506732] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
| cellular response to epidermal growth factor stimulus | biological process | Any 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 an epidermal growth factor stimulus. [GOC:mah] |
| cAMP-mediated signaling | biological process | An 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] |