Page last updated: 2024-08-07 16:40:19
Prostacyclin receptor
A prostacyclin receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P43119]
Synonyms
Prostaglandin I2 receptor;
PGI receptor;
PGI2 receptor;
Prostanoid IP receptor
Research
Bioassay Publications (29)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 16 (55.17) | 29.6817 |
| 2010's | 12 (41.38) | 24.3611 |
| 2020's | 1 (3.45) | 2.80 |
Compounds (25)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dinoprostone | Homo sapiens (human) | EC50 | 0.3470 | 1 | 1 |
| alprostadil | Homo sapiens (human) | EC50 | 0.0018 | 1 | 1 |
| fluprostenol | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| iloprost | Homo sapiens (human) | EC50 | 0.0014 | 2 | 2 |
| u 62840 | Homo sapiens (human) | EC50 | 0.0019 | 1 | 1 |
| selexipag | Homo sapiens (human) | EC50 | 0.0060 | 1 | 1 |
| mre 269 | Homo sapiens (human) | EC50 | 0.0220 | 1 | 1 |
| fevipiprant | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tg4-155 | Homo sapiens (human) | Kb | 31.6600 | 2 | 2 |
| pf-04418948 | Homo sapiens (human) | Kb | 10.0000 | 1 | 1 |
| tg6-10-1 | Homo sapiens (human) | Kb | 8.2850 | 2 | 2 |
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
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
Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity.Bioorganic & medicinal chemistry letters, , Aug-06, Volume: 11, Issue:15, 2001
Design and synthesis of a highly selective EP4-receptor agonist. Part 2: 5-thia and 9beta-haloPG derivatives with improved stability.Bioorganic & medicinal chemistry letters, , Aug-06, Volume: 11, Issue:15, 2001
Design and synthesis of a highly selective EP2-receptor agonist.Bioorganic & medicinal chemistry letters, , Aug-06, Volume: 11, Issue:15, 2001
Building on endogenous lipid mediators to design synthetic receptor ligands.European journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
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 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
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 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
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 new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
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
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
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 new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2.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
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
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 |
|---|
| 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] |
| prostacyclin receptor activity | molecular function | Combining with prostacyclin (PGI(2)) to initiate a change in cell activity. [ISBN:0198506732] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| 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 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, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, 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] |
| cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
| negative regulation of platelet-derived growth factor receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the platelet-derived growth factor receptor signaling pathway. [GOC:dph, GOC:hjd, GOC:tb] |
| 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 smooth muscle cell proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| 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] |