Proteins > Prostaglandin E2 receptor EP3 subtype
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Prostaglandin E2 receptor EP3 subtype
A prostaglandin E2 receptor EP3 subtype that is encoded in the genome of human. [PRO:WCB, UniProtKB:P43115]
Synonyms
PGE receptor EP3 subtype;
PGE2 receptor EP3 subtype;
PGE2-R;
Prostanoid EP3 receptor
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 13 (54.17) | 29.6817 |
| 2010's | 11 (45.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| metergoline | Homo sapiens (human) | Activity | 0.0217 | 1 | 1 |
| tg4-155 | Homo sapiens (human) | Kb | 10.0000 | 1 | 1 |
| l-798106 | Homo sapiens (human) | Kb | 0.0006 | 1 | 1 |
| pf-04418948 | Homo sapiens (human) | Kb | 100.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | Kb | 5.3000 | 1 | 1 |
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
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
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
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 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
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
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
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor anJournal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 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
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 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
Enables
This protein enables 1 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] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
| 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 9 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] |
| cell death | biological process | Any biological process that results in permanent cessation of all vital functions of a cell. A cell should be considered dead when any one of the following molecular or morphological criteria is met: (1) the cell has lost the integrity of its plasma membrane; (2) the cell, including its nucleus, has undergone complete fragmentation into discrete bodies (frequently referred to as apoptotic bodies). The cell corpse (or its fragments) may be engulfed by an adjacent cell in vivo, but engulfment of whole cells should not be considered a strict criteria to define cell death as, under some circumstances, live engulfed cells can be released from phagosomes (see PMID:18045538). [GOC:mah, GOC:mtg_apoptosis, PMID:25236395] |
| positive regulation of fever generation | biological process | Any process that activates or increases the frequency, rate, or extent of fever generation. [GOC:add] |
| intestine smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. This process occurs in the intestine. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. The intestine is the section of the alimentary canal from the stomach to the anal canal. It includes the large intestine and small intestine. [GOC:mtg_muscle, MA:0001539, MSH:D007422] |
| 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] |
| 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] |
| 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] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| negative regulation of gastric acid secretion | biological process | Any process that decreases the rate frequency or extent of gastric secretion. Gastric secretion is the regulated release of gastric acid (hydrochloric acid) by parietal or oxyntic cells during digestion. [GOC:dph, GOC:tb] |