Page last updated: 2024-08-07 16:48:13
P2Y purinoceptor 4
A P2Y purinoceptor 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P51582]
Synonyms
P2Y4;
P2P;
Uridine nucleotide receptor;
UNR
Research
Bioassay Publications (17)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 8 (47.06) | 29.6817 |
| 2010's | 9 (52.94) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| acid blue 25 | Homo sapiens (human) | IC50 | 17.8567 | 3 | 3 |
Drugs with Activation Measurements
Boranophosphate isoster controls P2Y-receptor subtype selectivity and metabolic stability of dinucleoside polyphosphate analogues.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
UDP made a highly promising stable, potent, and selective P2Y6-receptor agonist upon introduction of a boranophosphate moiety.Bioorganic & medicinal chemistry, , Sep-15, Volume: 20, Issue:18, 2012
Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.European journal of medicinal chemistry, , Volume: 44, Issue:4, 2009
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Novel nucleotide triphosphates as potent P2Y2 agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Purine and pyrimidine (P2) receptors as drug targets.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphate δ-ester modifications as selective agonists of the P2Y(4) receptor.Journal of medicinal chemistry, , Jun-23, Volume: 54, Issue:12, 2011
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 16, Issue:12, 2008
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors.Journal of medicinal chemistry, , Nov-30, Volume: 49, Issue:24, 2006
Development of Potent and Selective Antagonists for the UTP-Activated P2YJournal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| G protein-coupled purinergic nucleotide receptor activity | molecular function | Combining with a purine nucleotide and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:mah, PMID:9755289] |
| G protein-coupled UTP receptor activity | molecular function | Combining with a nucleotide and transmitting the signal to a heterotrimeric G-protein complex to initiate a change in cell activity, activated by UTP. [GOC:mah] |
Located In
This protein is located in 5 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] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| presynaptic active zone membrane | cellular component | The membrane portion of the presynaptic active zone; it is the site where docking and fusion of synaptic vesicles occurs for the release of neurotransmitters. [PMID:12812759, PMID:12923177, PMID:3152289] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active 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 9 target(s):
| Target | Category | Definition |
|---|
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| transepithelial chloride transport | biological process | The directed movement of chloride ions from one side of an epithelium to the other. [GOC:mah] |
| G protein-coupled purinergic nucleotide receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by an extracellular purine nucleotide binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:BHF, PMID:9755289] |
| cellular response to ATP | 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 ATP (adenosine 5'-triphosphate) stimulus. [GOC:mah] |
| cellular response to prostaglandin E 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 a prostagladin E stimulus. [GOC:mah] |
| regulation of presynaptic cytosolic calcium ion concentration | biological process | Any process that regulates the concentration of calcium in the presynaptic cytosol. [GOC:dos] |
| regulation of synaptic vesicle exocytosis | biological process | Any process that modulates the frequency, rate or extent of synaptic vesicle exocytosis. [GOC:obol] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |