DP2 Human Prostanoid GPCR Cell Based Antagonist Arrestin LeadHunter Assay - US

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. Prostaglandin D2 (PGD2), detected in brain, lung, skin, and mast cells, is implicated in the regulation of body temperature, sleep, hormone secretion, ion transport and pain. Prostanoid CRTH2 (Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells) receptor is activated by PGD2 and leads to increase in eosinophils and Th2 cell motility. CRTH2 receptor antagonism may be useful in the treatment of allergic inflammation.

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:

Gi/Go

Protein Name:

DP2

Uniprot Number:

Q9Y5Y4

Protein Aliases:

chemoattractant receptor homologous molecule expressed on T helper type 2 cells|G-protein coupled receptor 44|CD antigen CD294

Gene Name:

PTGDR2

Gene ID:

11251

Gene Aliases:

CRTH2|CD294|DP2|DL1R|GPR44

Accession Number:

AY507142

Organism:

Human

Cell Type:

U2OS