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