AAV ACTOne Gs-GPCR Assay Kit-TGR5

Takeda G protein-coupled receptor 5 (TGR5), also known as the G protein-coupled bile acid receptor 1 (GPBAR1), G-protein coupled receptor 19 (GPCR19), or membrane-type receptor for bile acids (M-BAR), is a protein that in humans is encoded by the GPBAR1 gene. Upon activation by bile acids, TGR5 primarily couples with Gs proteins, leading to an increase in cyclic AMP (cAMP) levels. This receptor is widely expressed in tissues such as the liver, intestines, and immune cells, where it plays key roles in regulating metabolic processes, including energy expenditure, glucose homeostasis, and immune responses. TGR5 has garnered significant interest for its potential therapeutic applications in treating metabolic disorders, including obesity and type 2 diabetes, as well as inflammatory diseases. By modulating bile acid signaling through TGR5, researchers aim to develop novel treatments that can improve metabolic health and reduce inflammation, highlighting the receptor's importance in both basic physiology and potential clinical interventions.
This kit uses AAV vectors with a CMV promoter to co-express the TGR5 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential TGR5-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of TGR5 drugs, such as agonists and antagonists, in a live-cell environment.

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Background

ACTOne™ is the only high-throughput GPCR screening technology that can directly measure the intracellular changes of the secondary messenger cyclic AMP (cAMP) in living cells, in real-time. It uses a proprietary modified cyclic nucleotide-gated (CNG) channel, which is co-localized with adenylate cyclase at the plasma membrane, as a biosensor of cAMP activity. The CNG channel opens when the cAMP level near the plasma membrane increases, resulting in ion flux and cell membrane depolarization. The influx of cations through the CNG channel can be quantified using fluorescent ion indicators or membrane potential (MP) dyes. It provides information on real time intracellular cAMP changes and is highly sensitive. By combining kinetic and endpoint readouts, we are able to capture and analyze transient responses from endogenous GPCRs and weak responses caused by weak Gs or Gi coupled GPCR activities. Using ACTOne, we are able to detect the subcellular cAMP concentration changes directly caused by GPCR activation. Real-time kinetic readouts minimize artifacts, and provide greater content and more statistically relevant data. The intensity of signal increase caused by GPCR activation is directly related to the receptor number on cell surface. Using ACTOne assay, we were able to detect activities of some endogenous Gs coupled receptors in HEK293 cells that have not been reported in literature. In addition, we have also detected weak Gs coupled activity of a GPCR that was widely considered to be only linked to Gq coupled pathway. The ACTOne assay also provides a useful tool for GPCR de-orphanization.