Page last updated: 2024-08-07 13:32:57
P2Y purinoceptor 6
A P2Y purinoceptor 6 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15077]
Synonyms
P2Y6
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 | 10 (55.56) | 29.6817 |
| 2010's | 8 (44.44) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| suramin | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
| acid blue 25 | Homo sapiens (human) | IC50 | 43.6950 | 2 | 2 |
Drugs with Activation Measurements
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
5-OMe-UDP is a potent and selective P2Y(6)-receptor agonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 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
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
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
Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
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
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
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 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
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
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
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled ADP receptor activity | molecular function | Combining with ADP 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, GOC:signaling, PMID:11196645] |
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal 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:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| G protein-coupled UDP 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 UDP. [GOC:mah] |
| 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 3 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] |
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 14 target(s):
| Target | Category | Definition |
|---|
| phagocytosis | biological process | A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732] |
| 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] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| positive regulation of smooth muscle cell migration | biological process | Any process that activates, maintains or increases the frequency, rate or extent of smooth muscle cell migration. [CL:0000192, GOC:mtg_muscle] |
| transepithelial chloride transport | biological process | The directed movement of chloride ions from one side of an epithelium to the other. [GOC:mah] |
| positive regulation of inositol 1,4,5-trisphosphate-sensitive calcium-release channel activity | biological process | Any process that activates or increases the frequency, rate or extent of the activity of the inositol 1,4,5-trisphosphate-sensitive calcium-release channel. [GOC:dph, GOC:mah, GOC:signaling] |
| positive regulation of inositol trisphosphate biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of inositol trisphosphate. [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] |
| 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 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] |
| cellular response to purine-containing compound | 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 purine-containing compound stimulus. [GOC:mah] |
| positive regulation of vascular associated smooth muscle cell proliferation | biological process | Any process that activates or increases the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467] |
| cellular response to pyrimidine ribonucleotide | 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 pyrimidine ribonucleotide stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:22065602] |
| 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] |