Page last updated: 2024-08-07 17:33:00
Prostaglandin D2 receptor 2
A prostaglandin D2 receptor DP2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9Y5Y4]
Synonyms
Chemoattractant receptor-homologous molecule expressed on Th2 cells;
G-protein coupled receptor 44
Research
Bioassay Publications (27)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 11 (40.74) | 29.6817 |
| 2010's | 16 (59.26) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| indomethacin | Homo sapiens (human) | EC50 | 0.3890 | 1 | 2 |
| oc000459 | Homo sapiens (human) | EC50 | 0.0240 | 1 | 1 |
| fevipiprant | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| duloxetine | Homo sapiens (human) | IC20 | 17.0000 | 1 | 1 |
| amg 009 | Homo sapiens (human) | Kb | 0.0004 | 3 | 3 |
| amg 853 | Homo sapiens (human) | Kb | 0.0002 | 1 | 1 |
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.Journal of medicinal chemistry, , Oct-06, Volume: 48, Issue:20, 2005
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Zwitterionic CRTh2 antagonists.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.ACS medicinal chemistry letters, , May-12, Volume: 2, Issue:5, 2011
Discovery and optimization of CRTH2 and DP dual antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
New indole amide derivatives as potent CRTH2 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Azaindoles as potent CRTH2 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
[no title available],
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| prostaglandin J receptor activity | molecular function | Combining with prostaglandin J (PGJ(2)), a metabolite of prostaglandin D (PGD(2)) to initiate a change in cell activity. [PMID:12878180] |
| 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] |
| prostaglandin D receptor activity | molecular function | Combining with prostaglandin D (PGD(2)) to initiate a change in cell activity. [ISBN:0198506732] |
| prostaglandin F receptor activity | molecular function | Combining with prostaglandin F (PGF (2-alpha)) to initiate a change in cell activity. [ISBN:0198506732] |
| neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
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] |
Active In
This protein is active in 2 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] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| chemotaxis | biological process | The directed movement of a motile cell or organism, or the directed growth of a cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [ISBN:0198506732] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| 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] |
| calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
| positive regulation of G protein-coupled receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of G protein-coupled receptor signaling pathway activity. [GOC:go_curators] |
| negative regulation of male germ cell proliferation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of male germ cell proliferation. [GOC:obol] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |