Biochem/physiol Actions

Target Sub-Family: SPC/LPC /proton-sensor

GPCR Class: A

Protein Target: GPR68/OGR1

Cell Line Description

GPCR Cell Lines

Host cells: Chem-1

Components

Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial.Fifty (50) mL of Media Component.

General description

Millipore’s Ready-to-Assay GPCR frozen cells are designed for simple, rapid calcium assays with no requirement for intensive cell culturing. Millipore has optimized the freezing conditions to provide cells with high viability and functionality post-thaw. The user simply thaws the cells and resuspends them in media, dispenses cell suspension into assay plates and, following over night recovery, assays for calcium response.

GPR68, also known as OGR1 (ovarian cancer G-protein-coupled receptor 1), was initially thought to be a receptor for sphingosylphosphorylcholine, although these results are controversial. Subsequent studies indicated that GPR68/OGR1 functions as a Gq-coupled sensor for extracellular pH, with maximal signaling occurring at pH of 7 or below (Ludwig et al., 2003; Tomura et al., 2005). Expression of GPR68/OGR1 is upregulated during RANKL-induced osteoclast differentiation, and knockdown of GPR68/OGR1 expression inhibits this differentiation process (Yang et al., 2006). Millipore’s cloned human GPR68-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant GPR68 expression on the cell surface and contains high levels of the promiscuous G protein G15 to enhance coupling of the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between GPR68 and its ligands.