HUMAN RECOMBINANT GPR91 RECEPTOR
MULTISCREEN™ DIVISION ARRESTED CELL LINE
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human GPR91 cDNA (GenBank Accession umber: NM_033050.3) with FLAG tag sequence at N- terminus.
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS
Stable for 1-2 days after thawing
GPR91, also known as SUCNR1, is a G Protein-Coupled Receptor with 339 amino acids. It has been characterized as a receptor for Succinate, a citric acid cycle intermediate. Succinate plays a key role in energy metabolism. Local interstitial accumulation of Succinate has recently been reported to serve as an indicator of ischemic or diabetic organ damage in the brain, liver, and kidney. In diabetes patients, the accumulation of Succinate is detectable in the plasma, and more significantly in the renal tubular fluid and urine. It is therefore considered a potential new biomarker of local tissue damage. It has also been shown that Succinate increases blood pressure in animals. The Succinate-induced hypertensive effect involves the renin-angiotensin
system that is shown to be absent in GPR91-deficient mice. There is a possible role for GPR91 in renovascular hypertension, a disease closely linked to atherosclerosis, diabetes and renal failure. In a recombinant system overexpressing GPR91, Succinate was shown to not only stimulate calcium mobilization and inositol phosphate (IP) accumulation through the stimulation of Gαq pathway but also to activate the Erk1/2 MAPK pathway and inhibit forskolin-stimulated cAMP accumulation through Gαi pathway
Application: Functional assays
Figure 1. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP accumulation upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01).
He, W., Miao, F. J., Lin, D. C., Schwandner, R. T., Wang, Z., Gao, J., Chen, J. L., Tian, H. and Ling, L. (2004) Citric acid cycle intermediates as ligands for orphan G-protein- coupled receptors. Nature, 429: 188-193.
Peti-Peterdi, J. (2010) “High glucose and renin release: the role of succinate and GPR91.” Kidney International, 78(12):1214-7