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prostaglandin J receptor activity

Definition

Target type: molecularfunction

Combining with prostaglandin J (PGJ(2)), a metabolite of prostaglandin D (PGD(2)) to initiate a change in cell activity. [PMID:12878180]

Prostaglandin J receptor activity is a molecular function associated with the binding and recognition of prostaglandin J2 (PGJ2) by its specific receptor, known as the peroxisome proliferator-activated receptor gamma (PPARγ). This interaction triggers a cascade of events that ultimately regulate gene expression and cellular processes.

PGJ2, a potent lipid mediator derived from arachidonic acid, exhibits a wide range of biological activities, including anti-inflammatory, anti-proliferative, and pro-apoptotic effects. These effects are mediated through its binding to PPARγ, a nuclear receptor that plays a crucial role in regulating lipid metabolism, glucose homeostasis, and immune responses.

Upon binding to PPARγ, PGJ2 undergoes a conformational change, which facilitates the recruitment of coactivator proteins. These coactivators, in turn, interact with specific DNA sequences known as peroxisome proliferator response elements (PPREs) located in the promoters of target genes. The binding of PPARγ to PPREs initiates the transcription of genes involved in various physiological processes.

The molecular function of prostaglandin J receptor activity is characterized by the following key features:

1. **Ligand Recognition:** PPARγ exhibits high affinity and selectivity for PGJ2, demonstrating its ability to distinguish PGJ2 from other prostaglandins and lipids.
2. **Conformational Change:** Binding of PGJ2 induces a conformational shift in PPARγ, exposing its DNA-binding domain and facilitating the recruitment of coactivator proteins.
3. **Transcriptional Regulation:** The interaction of PPARγ with coactivators promotes the transcription of target genes by facilitating the binding of the receptor to PPREs within their promoters.
4. **Biological Effects:** The transcriptional regulation mediated by PPARγ activation by PGJ2 results in a wide range of biological effects, including modulation of inflammation, cell growth, and apoptosis.

In summary, prostaglandin J receptor activity encompasses the specific recognition, binding, and signal transduction of PGJ2 by PPARγ, ultimately leading to the regulation of gene expression and diverse biological processes.'
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Proteins (2)

ProteinDefinitionTaxonomy
Prostaglandin D2 receptor 2A prostaglandin D2 receptor DP2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9Y5Y4]Homo sapiens (human)
Prostaglandin D2 receptorA prostaglandin D2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q13258]Homo sapiens (human)

Compounds (32)

CompoundDefinitionClassesRoles
indomethacinindometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.

Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.
aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole
analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic;
xenobiotic metabolite
lomerizinelomerizine: used to treat migrainesdiarylmethane
phlorhizinaryl beta-D-glucoside;
dihydrochalcones;
monosaccharide derivative
antioxidant;
plant metabolite
2-methyl-4-chlorophenoxyacetic acid(4-chloro-2-methylphenoxy)acetic acid : A chlorophenoxyacetic acid that is (4-chlorophenoxy)acetic acid substituted by a methyl group at position 2.

2-Methyl-4-chlorophenoxyacetic Acid: A powerful herbicide used as a selective weed killer.
chlorophenoxyacetic acid;
monochlorobenzenes
environmental contaminant;
phenoxy herbicide;
synthetic auxin
fentiazacthiazoles
duloxetineduloxetine
ah 68096-isopropoxy-9-oxoxanthene-2-carboxylic acid: structure given in UDxanthones
ramatrobanorganic molecular entity
agatoxin-489agatoxin-489: structure given in first source; anhydrous MW 489 Da; isolated from Agelenopsis aperta
flunarizineFlunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.diarylmethane
np 1188091-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one: an N-type calcium channel blocker; structure in first source
dinoprostDinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.

prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.
monocarboxylic acid;
prostaglandins Falpha
human metabolite;
mouse metabolite
cloprostenolCloprostenol: A synthetic prostaglandin F2alpha analog. The compound has luteolytic effects and is used for the synchronization of estrus in cattle.prostanoid
iloprostiloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.

Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.
carbobicyclic compound;
monocarboxylic acid;
secondary alcohol
platelet aggregation inhibitor;
vasodilator agent
sulindac sulfidesulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.

sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source
aryl sulfide;
monocarboxylic acid;
organofluorine compound
antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug
tg4-155TG4-155: an EP2 receptor antagonist; structure in first source
u 62840U 62840: stereoisomeric benzindene prostaglandin analog; structure given in first sourcecarbotricyclic compound;
carboxylic acid
antihypertensive agent;
cardiovascular drug;
human blood serum metabolite;
platelet aggregation inhibitor;
vasodilator agent;
vitamin K antagonist
mk-0524MK-0524: a potent orally active human prostaglandin D(2) receptor 1 antagonist; structure in first sourceindolyl carboxylic acid
selexipagselexipag : A member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid).

selexipag: prostacyclin receptor agonist
aromatic amine;
ether;
monocarboxylic acid amide;
N-sulfonylcarboxamide;
pyrazines;
tertiary amino compound
orphan drug;
platelet aggregation inhibitor;
prodrug;
prostacyclin receptor agonist;
vasodilator agent
mre 269(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid: active form of NS-304

ACT-333679 : A member of the class of pyrazines that is {4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetic acid carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. The active metabolite of selexipag, an orphan drug used for the treatment of pulmonary arterial hypertension.
aromatic amine;
ether;
monocarboxylic acid;
pyrazines;
sulfonamide;
tertiary amino compound
drug metabolite;
orphan drug;
platelet aggregation inhibitor;
prostacyclin receptor agonist;
vasodilator agent
amg 009AMG 009: an anti-inflammatory agent; structure in first source
azd1981
cay 10471CAY 10471: a prostaglandin D2 receptor antagonist; structure in first source
oc000459
l-798106L-798106 : An N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of o-naphthalen-2-ylcinnamic acid with the sulfonamide group of 5-bromo-2-methoxybenzenesulfonamide. It is a selective antagonist for the prostanoid receptor EP3, a prostaglandin receptor for prostaglandin E2 (PGE2).aromatic ether;
bromobenzenes;
N-sulfonylcarboxamide
prostaglandin receptor antagonist
fevipiprantfevipiprant: a CRTh2 antagonist; structure in first source
fr181157
pf-044189481-(4-fluorobenzoyl)-3-(((6-methoxy-2-naphthyl)oxy)methyl)azetidine-3-carboxylic acid: structure in first source
amg 853vidupiprant: structure in first source
cay 105802-(3-hydroxyoctyl)-5-oxo-1-pyrrolidineheptanoic acid : A pyrrolidin-2-one substituted by 6-carboxyhexyl and 3-hydroxyoctyl groups at positions 1 and 2, respectively. It is a potent prostaglandin EP4 receptor agonist (Ki=35 nM).

CAY 10580: a E-prostanoid EP4 receptor agonist
hydroxy monocarboxylic acid;
pyrrolidin-2-ones;
secondary alcohol
prostaglandin receptor agonist
mk-7246
tg6-10-1TG6-10-1: brain-permeant prostaglandin E receptor 2 antagonist; structure in first source