Biological Information
Background Information:
Prostanoid receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Prostanoid EP4 receptors are present in brain and many peripheral tissues (e.g., ileum>thymus>spleen>lung>heart>stomach).
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.
Family:
GPCR
Sub Family:
Prostanoid
Class:
Class A
Coupling:
Gs
Protein Name:
EP4
Uniprot Number:
P35408
Protein Aliases:
PGE2 receptor EP4 subtype|Prostanoid EP4 receptor
Gene Name:
PTGER4
Gene ID:
5734
Gene Aliases:
EP4
Accession Number:
AY429109
Organism:
Human
Cell Type:
HEK293
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
β-Arrestin Isoform:
β-Arrestin-2
Testing Information
Control Activator:
Prostaglandin E2
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
Adverse / Beneficial Action:
EP4 receptor agonism may exhibit intestinal cytoprotection, suppress hypermotility and colon cancer, reduce inflammatory activity (ulcerative colitis) and fever as well as increase wakefulness; use in the treatment of endotoxin shock and acute myocardial infarction have also been suggested. EP4 receptor antgonism may reduce intestinal mucosal and bronchopulmonary epithelial healing.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA