GPR68 Human GPCR Cell Based NAM Calcium Flux (Gα15 coupling) LeadHunter Assay - US

Background Information:

GPR68 is a proton-sensing receptor involved in pH homeostasis (PMID: 12955148). May represents an osteoblastic pH sensor regulating cell-mediated responses to acidosis in bone. Mediates its action by association with G proteins that stimulates inositol phosphate (IP) production or Ca2+ mobilization. The receptor is almost silent at pH 7.8 but fully activated at pH 6.8. Also functions as a metastasis suppressor gene in prostate cancer (By similarity). (https://www.uniprot.org/uniprotkb/Q15743/entry) ChemiScreen cell lines are engineered for high levels of receptor expression and contain high leves of the promiscuous G-protein Gα15 to couple the receptor to the calcium signaling pathway. Calcium mobilization in ChemiScreen GPCR cell lines 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

Coupling:

Ga

Protein Name:

OGR1

Uniprot Number:

Q15743

Protein Aliases:

ovarian cancer G protein-coupled receptor 1|G-protein coupled receptor 68|GPR12A|sphingosylphosphorylcholine receptor

Gene Name:

GPR68

Gene ID:

8111

Gene Aliases:

OGR1; AI2A6; GPR12A

Accession Number:

NM_003485

Organism:

Human

Cell Type:

Chem-1