GPR139 Human Class A Orphan GPCR Cell Based Antagonist Calcium Flux Assay (in Arrestin Cell Line) LeadHunter Assay - US

Background Information:

GPR139 is an orphan receptor that is expressed primarily in the brain. It potentially acts through a G(q/11)-mediated pathway and negatively regulates μ opioid receptor signaling. https://www.uniprot.org/uniprotkb/Q6DWJ6/entry.
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Calcium mobilization in PathHunter β-Arrestin GPCR cell lines expressing Gq-coupled GPCRs is monitored using a calcium sensitive dye that is loaded into cells. The esterified (inactive) calcium dye (probe) penetrates the cell membrane and becomes active after binding to intracellular calcium. Ligand binding stimulates GPCR activation, resulting in release of intracellular calcium stores from the ER, which leads to an increase in fluorescence in the presence of the activated calcium dye.

Family:

GPCR

Sub Family:

Class A Orphan

Class:

Orphan and other 7TM

Protein Name:

GPR139

Uniprot Number:

Q6DWJ6

Protein Aliases:

Gq-coupled orphan receptor GPRg1|G-protein-coupled receptor PGR3

Gene Name:

GPR139

Gene ID:

124274

Gene Aliases:

GPRG1|PGR3

Accession Number:

NM_001002911.2

Organism:

Human

Cell Type:

CHO-K1