The G-protein coupled receptor (GPCR) family represents the largest and most versatile group of cell surface receptors, and are targets of approximately 30%-40% of marketed drugs currently. Identifying key modulators or compounds of GPCRs is now at the crux of drug discovery efforts. Incorporated with a special biosensor system, Creative Biolabs now launches the Magic™ GPCR stable cell line platform for function validation & screening against various GPCR targets. Here, we proudly introduce the popular Magic™ AVPR2 stable cell line to our global clients.
Introduction to AVPR2 Receptor
Arginine Vasopressin receptor 2 (AVPR2) belongs to the subfamily of G-protein coupled receptors. The binding of arginine vasopressin (AVP) to the V2 vasopressin receptor (V2R) stimulates a Gs-coupled protein that activates adenylyl cyclase (AC), in turn catalyzing the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate. The cAMP has been shown to activate protein kinase A (PKA). This pathway increases the exocytosis of aquaporin water channel-containing vesicles (AQMCV) and inhibits endocytosis of the vesicles, both resulting in increases in aquaporin 2 (AQ2) channel formation and apical membrane insertion. This allows an increase in the permeability of water from the collecting duct (CD).
Fig.1 Mechanisms of action of the peptide hormone system-related drugs in hormone-resistant cancer.1,2
Magic™ AVPR2 Stable Cell Line
Magic™ AVPR2 stable cell line is constructed by co-transfection of human arginine vasopressin receptor 2 (AVPR2) and cAMP-activated, membrane-associated fluorescent biosensor in U2OS cells. Upon AVPR2 activation/inhibition, changes in cAMP concentration will elicit rapid translocation of biosensor (from plasma membrane to cytosolic vesicles). This way, AVPR2 activities will be real-time translated into cellular fluorescence signals, which can be easily monitored and quantified. The AVPR2 cell line has been applied to assay compounds and characterize their AVPR2-modulating activities. It has been proved to be high-efficient, convenient and sensitive, providing an attractive strategy for receptor function validation/screening in early stage.
Featured Advantages of Magic™ AVPR2 Stable Cell Lines
In addition to AVPR2, Creative Biolabs now offers a comprehensive portfolio of Magic™ GPCR stable cell lines engineered with cAMP-activated biosensors, including but not limited to:
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Meanwhile, we also provide well-established Magic™ biosensor cell line options to assess calcium-, DAG-related as well as multiplex pathway events of various GPCRs. If you cannot find your desired target in the catalog, we are always happy to establish a specific cell line upon custom request. Please contact us for more information and a detailed quote.
References
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