AAV ACTOne GI-GPCR Assay Kit-NPY4R

Neuropeptide Y Receptor Y4 (NPY4R), also known as Pancreatic Polypeptide Receptor 1 (PPR1), is a G protein-coupled receptor (GPCR) that primarily binds to pancreatic polypeptide (PP), although it can also bind to neuropeptide Y (NPY) and peptide YY (PYY) with lower affinity. NPY4R is primarily coupled with the Gi/Go class of G proteins, which inhibit adenylate cyclase activity, leading to a reduction in cyclic AMP (cAMP) levels. This signaling pathway influences various physiological processes, including the regulation of appetite, energy homeostasis, and gastrointestinal function. NPY4R is expressed in several tissues, including the brain, particularly the hypothalamus, as well as in the gastrointestinal tract, pancreas, and adipose tissue. In the central nervous system, NPY4R plays a role in regulating food intake and energy balance. Activation of NPY4R by pancreatic polypeptide has been shown to reduce food intake, making it an important receptor in the control of appetite and body weight. In addition to its role in feeding behavior, NPY4R is also involved in gastrointestinal motility and secretion, as well as in the regulation of cardiovascular function. Due to its involvement in appetite suppression and energy homeostasis, NPY4R is a target of interest for developing treatments for obesity and related metabolic disorders. Ongoing research into NPY4R aims to better understand its role in regulating appetite and metabolism, with the potential for developing new therapeutic approaches for weight management and metabolic health.
This kit uses AAV vectors with a CMV promoter to co-express the NPY4R and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential NPY4R-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of NPY4R 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.