Proteins > High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A
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High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A
A high affinity cGMP-specific 3,5-cyclic phosphodiesterase 9A that is encoded in the genome of human. [PRO:DNx, UniProtKB:O76083]
Synonyms
EC 3.1.4.35
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (27.78) | 29.6817 |
| 2010's | 11 (61.11) | 24.3611 |
| 2020's | 2 (11.11) | 2.80 |
Compounds (12)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pf-2545920 | Homo sapiens (human) | Activity | 0.0021 | 1 | 1 |
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Insight into binding of phosphodiesterase-9A selective inhibitors by crystal structures and mutagenesis.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
(±)-Torreyunlignans A-D, rare 8-9' linked neolignan enantiomers as phosphodiesterase-9A inhibitors from Torreya yunnanensis.Journal of natural products, , Dec-26, Volume: 77, Issue:12, 2014
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Elucidation of fluorine's impact on pMedChemComm, , May-01, Volume: 9, Issue:5, 2018
Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorJournal of medicinal chemistry, , Nov-08, Volume: 55, Issue:21, 2012
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| 3',5'-cyclic-nucleotide phosphodiesterase activity | molecular function | Catalysis of the reaction: a nucleoside 3',5'-cyclic phosphate + H2O = a nucleoside 5'-phosphate. [RHEA:14653] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| 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] |
| 3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
Located In
This protein is located in 9 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| endoplasmic reticulum | cellular component | The 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 apparatus | cellular component | A 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] |
| 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] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| ruffle membrane | cellular component | The portion of the plasma membrane surrounding a ruffle. [GOC:mah] |
| sarcolemma | cellular component | The outer membrane of a muscle cell, consisting of the plasma membrane, a covering basement membrane (about 100 nm thick and sometimes common to more than one fiber), and the associated loose network of collagen fibers. [ISBN:0198506732] |
| perikaryon | cellular component | The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| positive regulation of cardiac muscle hypertrophy | biological process | Any process that increases the rate, frequency or extent of the enlargement or overgrowth of all or part of the heart due to an increase in size (not length) of individual cardiac muscle fibers, without cell division. [GOC:BHF, GOC:dph, GOC:tb] |
| cGMP metabolic process | biological process | The chemical reactions and pathways involving cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators] |
| cGMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators] |
| positive regulation of long-term synaptic potentiation | biological process | Any process that activates or increases the frequency, rate or extent of long-term synaptic potentiation. [GOC:BHF, GOC:TermGenie] |
| negative regulation of neural precursor cell proliferation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of neural precursor cell proliferation. [GOC:dph, GOC:yaf] |
| 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] |