Proteins > Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
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Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
A cone cGMP-specific 3,5-cyclic phosphodiesterase subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P51160]
Synonyms
EC 3.1.4.35;
cGMP phosphodiesterase 6C
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (38.46) | 29.6817 |
| 2010's | 6 (46.15) | 24.3611 |
| 2020's | 2 (15.38) | 2.80 |
Compounds (7)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| evodiamine | Homo sapiens (human) | EC50 | 20.0000 | 1 | 1 |
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
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
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
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
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 13, Issue:8, 2003
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
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
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
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
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.Journal of natural products, , Volume: 71, Issue:9, 2008
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
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
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
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
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
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| cGMP binding | molecular function | Binding to cGMP, the nucleotide cyclic GMP (guanosine 3',5'-cyclophosphate). [GOC:ai] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| 3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
| 3',5'-cyclic-GMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic GMP + H2O = GMP + H+. [RHEA:16957] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| 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] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| phototransduction, visible light | biological process | The sequence of reactions within a cell required to convert absorbed photons from visible light into a molecular signal. A visible light stimulus is electromagnetic radiation that can be perceived visually by an organism; for organisms lacking a visual system, this can be defined as light with a wavelength within the range 380 to 780 nm. [GOC:go_curators, ISBN:0198506732] |
| retinal cone cell development | biological process | Development of a cone cell, one of the sensory cells in the eye that reacts to the presence of light. Cone cells contain the photopigment iodopsin or cyanopsin and are responsible for photopic (daylight) vision. [ISBN:0198506732] |
| 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] |
| visual perception | biological process | The series of events required for an organism to receive a visual stimulus, convert it to a molecular signal, and recognize and characterize the signal. Visual stimuli are detected in the form of photons and are processed to form an image. [GOC:ai] |