HUMAN RECOMBINANT GPR52 RECEPTOR
MULTISCREENTM β-ARRESTIN2 STABLE CELL LINE
Catalog Number: CA1112BA2
Lot Number: C1112BA2-082821
Quantity: 1 vial (2 x 106) frozen cells
Freeze Medium: Cellbanker 2 (Amsbio)
Host cell: HEK293T β-Arrestin2
Transfection: Expression vector containing full-length human GPR52 cDNA (GenBank accession number NM_005684) with FLAG tag sequence at N-terminus and ARRB2 cDNA (GenBank Accession Number NM_004313.3)
Recommended Storage: Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin, 50 μg/mL hygromycin
Stability: In progress
Background: GPR52 is a class-A orphan G-protein-coupled receptor that can be found in human and mice, and is highly expressed in the brain and represents a promising therapeutic target for the treatment of Huntington’s disease and several psychiatric disorders. Once activated by antipsychotics reserpine, an increase of intracellular cAMP and its internalization is resulted. Members of this protein family contain transmembrane domain and may play a role in locomotor activity through modulation of dopamine, NMDA and ADORA2A-induced locomotor activity. They represent a promising therapeutic target for the treatment of Huntington’s disease and several psychiatric disorders.
Application: Functional assays
Figure 1. Dose-dependent stimulation from arrestin recruitment upon treatment with ligand, measured with MultiScreenTM β-Arrestin Assay Kit (Multispan MSBA01). Figure 2. Dose- dependent stimulation of intracellular cAMP level upon treatment with ligand, measured with MultiScreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01) Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Yao, Y et al. (2015). A striatal-enriched intronic GPCR modulates huntingtin levels and toxicity. eLife, 4, e05449.
Komatsu, H. et al. (2014). Anatomical transcriptome of G protein-coupled receptors leads to the identification of a novel therapeutic candidate GPR52 for psychiatric disorders. PloS one, 9(2), e9013
Nishiyama, K. et al. (2017). FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia. The Journal of pharmacology and experimental therapeutics, 363(2), 253–264.
Southern, Craig et al. “Screening β-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors.” Journal of biomolecular screening vol. 18,5 (2013): 599-609
Hatzipantelis, Cassandra J et al. “β-Arrestin-2-Dependent Mechanism of GPR52 Signaling in Frontal Cortical Neurons.” ACS chemical neuroscience vol. 11,14 (2020): 2077-2084.