AAV ACTOne Gs-GPCR Assay Kit-GPR119

GPR119 is a G protein-coupled receptor (GPCR) primarily expressed in the pancreas and gastrointestinal tract. It plays a significant role in glucose homeostasis by stimulating insulin secretion and promoting the release of incretin hormones such as GLP-1 and GIP in response to food intake. GPR119 is activated by endogenous lipids, including oleoylethanolamide (OEA). Due to its involvement in regulating glucose levels, GPR119 is a target for developing treatments for type 2 diabetes and obesity. GPR119, along with GPR55 and GPR18, has been implicated as a novel cannabinoid receptor. These receptors are part of the G protein-coupled receptor family and are thought to interact with cannabinoids, including endogenous ligands and potentially exogenous compounds like those found in cannabis. While GPR119 is primarily involved in metabolic processes such as glucose homeostasis, GPR55 and GPR18 are more directly linked to cannabinoid-like activities, making them potential targets for cannabinoid-related research and therapeutic development.
This kit uses AAV vectors with a CMV promoter to co-express the GPR119 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential GPR119-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of GPR119 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.