Page last updated: 2024-08-07 17:26:05
P2Y purinoceptor 12
A P2Y purinoceptor 12 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9H244]
Synonyms
P2Y12;
ADP-glucose receptor;
ADPG-R;
P2T(AC);
P2Y(AC);
P2Y(cyc);
P2Y12 platelet ADP receptor;
P2Y(ADP);
SP1999
Research
Bioassay Publications (21)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (4.76) | 18.2507 |
| 2000's | 6 (28.57) | 29.6817 |
| 2010's | 9 (42.86) | 24.3611 |
| 2020's | 5 (23.81) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| leukotriene e4 | Homo sapiens (human) | EC50 | 0.0013 | 1 | 1 |
| ar c67085mx | Homo sapiens (human) | EC50 | 0.0013 | 1 | 1 |
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Purine and pyrimidine (P2) receptors as drug targets.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Strategies for targeting the P2YBioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.European journal of medicinal chemistry, , Jan-01, Volume: 107, 2016
GPCR crystal structures: Medicinal chemistry in the pocket.Bioorganic & medicinal chemistry, , Jul-15, Volume: 23, Issue:14, 2015
Purine and pyrimidine (P2) receptors as drug targets.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Strategies for targeting the P2YBioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
Synthesis and biological evaluation of RSC medicinal chemistry, , Aug-18, Volume: 12, Issue:8, 2021
Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2YJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Facile alkylation of 4-nitrobenzotriazole and its platelet aggregation inhibitory activity.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
[no title available]European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Strategies for targeting the P2YBioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
State of affairs: Design and structure-activity relationships of reversible P2Y12 receptor antagonists.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 26, Issue:12, 2016
Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.Bioorganic & medicinal chemistry, , 02-15, Volume: 56, 2022
Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
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
High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled adenosine receptor activity | molecular function | Combining with adenosine 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, GOC:mah, PMID:9755289] |
| 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] |
| guanyl-nucleotide exchange factor activity | molecular function | Stimulates the exchange of GDP to GTP on a signaling GTPase, changing its conformation to its active form. Guanine nucleotide exchange factors (GEFs) act by stimulating the release of guanosine diphosphate (GDP) to allow binding of guanosine triphosphate (GTP), which is more abundant in the cell under normal cellular physiological conditions. [GOC:kd, GOC:mah, PMID:23303910, PMID:27218782] |
| 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] |
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] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| cell projection membrane | cellular component | The portion of the plasma membrane surrounding a plasma membrane bounded cell surface projection. [GOC:krc, GOC:mah] |
| cell body membrane | cellular component | The plasma membrane of a cell that bears surface projections such as axons, dendrites, cilia, or flagella, excluding the plasma membrane on cell projections. [GOC:ecd] |
Involved In
This protein is involved in 27 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled adenosine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a receptor binding to extracellular adenosine and transmitting the signal to a heterotrimeric G-protein complex to initiate a change in cell activity. [GOC:dph] |
| monoatomic ion transport | biological process | The directed movement of a monoatomic ion into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:ai] |
| substrate-dependent cell migration, cell extension | biological process | The formation of a cell surface protrusion, such as a lamellipodium or filopodium, at the leading edge of a migrating cell. [ISBN:0815316194, PMID:11944043, PMID:14657486] |
| 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] |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| 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] |
| hemostasis | biological process | The stopping of bleeding (loss of body fluid) or the arrest of the circulation to an organ or part. [ISBN:0198506732] |
| calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
| cerebral cortex radial glia-guided migration | biological process | The radial migration of neuronal or glial precursor cells along radial glial cells during the development of the cerebral cortex. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, PMID:12626695] |
| cell projection organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a prolongation or process extending from a cell, e.g. a flagellum or axon. [GOC:jl, GOC:mah, http://www.cogsci.princeton.edu/~wn/] |
| lamellipodium assembly | biological process | Formation of a lamellipodium, a thin sheetlike extension of the surface of a migrating cell. [GOC:mah, ISBN:0815316194] |
| platelet activation | biological process | A series of progressive, overlapping events triggered by exposure of the platelets to subendothelial tissue. These events include shape change, adhesiveness, aggregation, and release reactions. When carried through to completion, these events lead to the formation of a stable hemostatic plug. [http://www.graylab.ac.uk/omd/] |
| positive regulation of integrin activation by cell surface receptor linked signal transduction | biological process | Any process that activates or increases the frequency, rate, or extent of integrin activation by cell surface receptor linked signal transduction. This can occur by increased affinity of an integrin for its extracellular ligands. [GOC:add, PMID:12213832, PMID:14754902] |
| positive regulation of cell adhesion mediated by integrin | biological process | Any process that activates or increases the frequency, rate, or extent of cell adhesion mediated by integrin. [GOC:add] |
| 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 monoatomic ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of charged atoms or small charged molecules into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:jl] |
| response to axon injury | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an axon injury stimulus. [GOC:dgh, GOC:dph, GOC:jid, GOC:lm] |
| regulation of chemotaxis | biological process | Any process that modulates the frequency, rate or extent of the directed movement of a motile cell or organism in response to a specific chemical concentration gradient. [GOC:ai] |
| positive regulation of chemotaxis | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of a motile cell or organism in response to a specific chemical concentration gradient. [GOC:ai] |
| establishment of localization in cell | biological process | Any process, occuring in a cell, that localizes a substance or cellular component. This may occur via movement, tethering or selective degradation. [GOC:ai, GOC:dos, GOC:dph, GOC:tb] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| platelet aggregation | biological process | The adhesion of one platelet to one or more other platelets via adhesion molecules. [GOC:BHF, GOC:vk] |
| 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] |
| visual system development | biological process | The process whose specific outcome is the progression of the visual system over time, from its formation to the mature structure, including the eye, parts of the central nervous system (CNS) involved in processing of visual inputs, and connecting nerve pathways. [GOC:aruk, GOC:bc, GOC:krc, PMID:15004427, PMID:20647017, PMID:22632727] |
| positive regulation of ruffle assembly | biological process | Any process that activates or increases the frequency, rate or extent of ruffle assembly. [GOC:TermGenie, GOC:yaf] |
| regulation of microglial cell migration | biological process | Any process that modulates the frequency, rate or extent of microglial cell migration. [GO_REF:0000058, GOC:BHF, GOC:nc, GOC:TermGenie, PMID:19100238] |
| positive regulation of microglial cell migration | biological process | Any process that activates or increases the frequency, rate or extent of microglial cell migration. [GO_REF:0000058, GOC:BHF, GOC:nc, GOC:TermGenie, PMID:19100238] |