Proteins > Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta
Page last updated: 2024-08-07 15:25:49
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta
A retinal rod rhodopsin-sensitive cGMP 3,5-cyclic phosphodiesterase subunit delta that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43924]
Synonyms
GMP-PDE delta;
Protein p17
Research
Bioassay Publications (11)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (36.36) | 29.6817 |
| 2010's | 5 (45.45) | 24.3611 |
| 2020's | 2 (18.18) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dipyridamole | Homo sapiens (human) | Ki | 0.1250 | 1 | 1 |
| tadalafil | Homo sapiens (human) | IC50 | 2.9280 | 5 | 5 |
| fluconazole | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
| sildenafil | Homo sapiens (human) | IC50 | 0.0188 | 4 | 4 |
| sildenafil | Homo sapiens (human) | Ki | 0.0500 | 1 | 1 |
| zaprinast | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| vardenafil | Homo sapiens (human) | IC50 | 0.0077 | 3 | 3 |
Drugs with Activation Measurements
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
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
Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer.Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.European journal of medicinal chemistry, , Feb-01, Volume: 163, 2019
Structural Biology-Inspired Discovery of Novel KRAS-PDEδ Inhibitors.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.Journal of medicinal chemistry, , Jun-26, Volume: 57, 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
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
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 3 target(s):
| Target | Category | Definition |
|---|
| GTPase inhibitor activity | molecular function | Stops, prevents or reduces the activity of any enzyme that catalyzes the hydrolysis of GTP to GDP and orthophosphate. [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| small GTPase binding | molecular function | Binding to a small monomeric GTPase. [GOC:mah, PMID:27218782] |
Located In
This protein is located in 5 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] |
| cytoskeleton | cellular component | A cellular structure that forms the internal framework of eukaryotic and prokaryotic cells. The cytoskeleton includes intermediate filaments, microfilaments, microtubules, the microtrabecular lattice, and other structures characterized by a polymeric filamentous nature and long-range order within the cell. The various elements of the cytoskeleton not only serve in the maintenance of cellular shape but also have roles in other cellular functions, including cellular movement, cell division, endocytosis, and movement of organelles. [GOC:mah, PMID:16959967, PMID:27419875] |
| cilium | cellular component | A specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998] |
| cytoplasmic vesicle membrane | cellular component | The lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah] |
| cytoplasmic vesicle | cellular component | A vesicle found in the cytoplasm of a cell. [GOC:ai, GOC:mah, GOC:vesicles] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 1 target(s):
| Target | Category | Definition |
|---|
| 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] |