Proteins > Prostaglandin E2 receptor EP4 subtype
Page last updated: 2024-08-07 18:34:15
Prostaglandin E2 receptor EP4 subtype
A prostaglandin E2 receptor EP4 subtype that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35408]
Synonyms
PGE receptor EP4 subtype;
PGE2 receptor EP4 subtype;
Prostanoid EP4 receptor
Research
Bioassay Publications (32)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 14 (43.75) | 29.6817 |
| 2010's | 18 (56.25) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dinoprostone | Homo sapiens (human) | EC50 | 0.0028 | 5 | 5 |
| cj-042794 | Homo sapiens (human) | Kd | 0.0018 | 1 | 1 |
| cj-023,423 | Homo sapiens (human) | Kd | 0.0048 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| metergoline | Homo sapiens (human) | Activity | 0.0152 | 1 | 1 |
| tg4-155 | Homo sapiens (human) | Kb | 7.6038 | 3 | 3 |
| pf-04418948 | Homo sapiens (human) | Kb | 10.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | Kb | 8.6056 | 2 | 2 |
Difluoromethylene at the γ-Lactam α-Position Improves 11-Deoxy-8-aza-PGEJournal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Discovery of G Protein-Biased EP2 Receptor Agonists.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
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
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
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
Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 27, Issue:5, 2017
Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 27, Issue:5, 2017
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 26, Issue:9, 2016
Discovery and characterization of a potent and selective EP4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 25, Issue:16, 2015
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 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
Lead optimization studies of cinnamic amide EP2 antagonists.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Prostanoid receptor EP2 as a therapeutic target.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| prostaglandin E receptor activity | molecular function | Combining with prostaglandin E (PGE(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 22 target(s):
| Target | Category | Definition |
|---|
| negative regulation of cytokine production | biological process | Any process that stops, prevents, or reduces the rate of production of a cytokine. [GOC:add, ISBN:0781735149] |
| positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
| 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] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| JNK cascade | biological process | A MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017] |
| response to mechanical stimulus | 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 a mechanical stimulus. [GOC:hb] |
| response to nematode | 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 a stimulus from a nematode. [GOC:hb] |
| regulation of ossification | biological process | Any process that modulates the frequency, rate or extent of ossification, the formation of bone or of a bony substance or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:go_curators] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| negative regulation of integrin activation | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of integrin activation. [GOC:add] |
| T-helper cell differentiation | biological process | The process in which a relatively unspecialized thymocyte acquires specialized features of a T-helper cell. [GOC:ebc] |
| negative regulation of inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| positive regulation of inflammatory response | biological process | Any process that activates or increases the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| regulation of stress fiber assembly | biological process | Any process that modulates the frequency, rate or extent of the assembly of a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| bone development | biological process | The process whose specific outcome is the progression of bone over time, from its formation to the mature structure. Bone is the hard skeletal connective tissue consisting of both mineral and cellular components. [GOC:dph] |
| ERK1 and ERK2 cascade | biological process | A MAPK cascade containing at least the ERK1 or ERK2 MAP kinases. It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK1 or ERK2. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier. The ERK1/ERK2 cascade is activated by mitogens, growth factors, G protein-coupled receptors, and results in cellular responses such as cell proliferation, cell differentiation and development. [PMID:20811974, PMID:23125017, PMID:28903453] |
| cellular response to mechanical 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 mechanical stimulus. [GOC:mah] |
| negative regulation of eosinophil extravasation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of eosinophil extravasation. [GOC:BHF, 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] |
| adenylate cyclase-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 adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [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] |
| 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] |