B1 Human Bradykinin GPCR Cell Based Agonist Arrestin LeadHunter Assay - US

Background Information:

Bradykinin 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. Bradykinin receptors are found in most peripheral tissue and within the central nervous system. Bradykinin B1 receptor agonism may result in cough, algesia, inflammation and vasodilation. Bradykinin B1 receptor antagonism may find therapeutic use in the treatment of chronic pain and 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 enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Bradykinin

Class:

Class A

Coupling:

Gq

Protein Name:

B1

Uniprot Number:

P46663

Protein Aliases:

BK-1 receptor

Gene Name:

BDKRB1

Gene ID:

623

Gene Aliases:

BKR1|B1BKR|bradyb1

Accession Number:

NM_000710.2

Organism:

Human

Cell Type:

CHO-K1