Page last updated: 2024-08-07 17:05:08
Prostaglandin D2 receptor
A prostaglandin D2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q13258]
Synonyms
PGD receptor;
PGD2 receptor;
Prostanoid DP receptor
Research
Bioassay Publications (22)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 12 (54.55) | 29.6817 |
| 2010's | 9 (40.91) | 24.3611 |
| 2020's | 1 (4.55) | 2.80 |
Compounds (22)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| iloprost | Homo sapiens (human) | EC50 | 1.1030 | 2 | 2 |
| u 62840 | Homo sapiens (human) | EC50 | 0.0006 | 1 | 1 |
| mk-0524 | Homo sapiens (human) | Kd | 0.0000 | 1 | 1 |
| selexipag | Homo sapiens (human) | EC50 | 0.1000 | 1 | 1 |
| mre 269 | Homo sapiens (human) | EC50 | 0.1540 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tg4-155 | Homo sapiens (human) | Kb | 0.0345 | 2 | 2 |
| pf-04418948 | Homo sapiens (human) | Kb | 10.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | Kb | 0.1665 | 2 | 2 |
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
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
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
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Building on endogenous lipid mediators to design synthetic receptor ligands.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 02-09, Volume: 60, Issue:3, 2017
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Lead optimization studies of cinnamic amide EP2 antagonists.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
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 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
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
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
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Lead optimization studies of cinnamic amide EP2 antagonists.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Enables
This protein enables 3 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] |
| prostaglandin D receptor activity | molecular function | Combining with prostaglandin D (PGD(2)) to initiate a change in cell activity. [ISBN:0198506732] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located 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] |
| 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] |
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 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| male sex determination | biological process | The specification of male sex of an individual organism. [GOC:mah] |
| sleep | biological process | Any process in which an organism enters and maintains a periodic, readily reversible state of reduced awareness and metabolic activity. Usually accompanied by physical relaxation, the onset of sleep in humans and other mammals is marked by a change in the electrical activity of the brain. [ISBN:0192800981] |
| mast cell degranulation | biological process | The regulated exocytosis of secretory granules containing preformed mediators such as histamine, serotonin, and neutral proteases by a mast cell. [ISBN:0781735149] |
| adenosine metabolic process | biological process | The chemical reactions and pathways involving adenosine, adenine riboside, a ribonucleoside found widely distributed in cells of every type as the free nucleoside and in combination in nucleic acids and various nucleoside coenzymes. [GOC:go_curators] |
| cellular response to prostaglandin D 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 D stimulus. [GOC:sl] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |