mProX™ Human GPR68 Stable Cell Line

Sub Cat	Product Name	Target Protein Species	Host Cell Type	Assay Types	Inquiry	Datasheet
S01YF-1122-KX808	Magic™ Mouse GPR68 in Vitro cAMP Assay	Mouse	1321N1	cAMP Assay
S01YF-1122-KX809	Magic™ Rat GPR68 in Vitro cAMP Assay	Rat	1321N1	cAMP Assay

Product Information

Target Protein

GPR68

Target Family

SPC/LPC/Proton-sensor Family

Target Protein Species

Human

Host Cell Type

Caco-2; CHO-K1; HEK293

Target Classification

GPCR Cell Lines

Target Research Area

CNS Research; Orphan Receptor Research

Related Diseases

Amelogenesis Imperfecta

Gene ID

8111

UniProt ID

Q15743

Product Properties

Biosafety Level

Level 1

Activity

Yes

Quantity

10⁶ cells per vial

Applications

GPR68 was identified as a proton-sensing GPCR that affects the function of many different cell types in response to extracellular acidity. GPR68 sensing of H+ is assumed to occur through protonation of histidine residues, which results in conformational changes and receptor activation, in contrast to the ligand-receptor binding pocket interaction of other GPCRs. The mRNA expression of GPR68 is elevated in many cancers, and it is expressed in a variety of organs. New evidence suggests that GPR68 plays important functions in tumor biology. GPR68 was first discovered to be a metastasis suppressor gene in prostate cancer, but it has also been shown to support carcinogenesis in melanoma and prostate cancer. Additionally, GPR68 controls the growth and proliferation of medulloblastoma cells and may be a mediator of lenalidomide response in MDS. The customized GPR68 stable cell line can be used in antibody discovery and development, potential drug candidate screening and signaling pathway researches.

Protocols

Please visit our protocols page.

Customer Reviews

chat Eartha

I customized a GPR68 cell line and it's very good. Aug 16 2023

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chat Vanessa

This cell line is very suitable for studying the GPR68 signaling pathway. Jul 11 2023

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FAQ

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Published Data

Fig.1 ER stress is induced by acidosis activated OGR1-mediated signalling.

After 4-6 hours of incubation in pH 7.6 serum free medium, Caco-2 cells were exposed to varied pH medium. Tunicamycin was applied to vector control Caco-2 (VC) and OGR1 overexpressing Caco-2 cells for 24 hours at the given doses. Western blotting was done after total protein was extracted.

Ref: Maeyashiki, Chiaki, et al. "Activation of pH-Sensing Receptor OGR1 (GPR68) Induces ER Stress Via the IRE1 α/JNK Pathway in an Intestinal Epithelial Cell Model." Scientific reports 10.1 (2020): 1438.

Pubmed: 31996710

DOI: 10.1038/s41598-020-57657-9

Research Highlights

A number of cellular processes are controlled by GPR68, a proton-sensing G-protein-coupled receptor (GPCR) that reacts to extracellular acidity. One distinctive feature of the tumor microenvironment (TME) is acidosis. The expression of GPR68 is markedly increased in many different cancers.
Wiley, Shu Z., et al. "GPR68: an emerging drug target in cancer." International journal of molecular sciences 20.3 (2019): 559.
Pubmed: 30696114 DOI: 10.3390/ijms20030559

One of these is the proton receptor GPR68, which is lacking the small chemical modulators needed to examine its biology. Here, we identified the benzodiazepine medication lorazepam as a non-selective GPR68 positive allosteric modulator using yeast-based screens against GPR68.
Huang, Xi-Ping, et al. "Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65." Nature 527.7579 (2015): 477-483.
Pubmed: 26550826 DOI: 10.1038/nature15699