AAV ACTOne Gi-GPCR Assay Kit-NPY5R

Neuropeptide Y Receptor Y5 (NPY5R) is a G protein-coupled receptor (GPCR) that primarily binds to neuropeptide Y (NPY), peptide YY (PYY), and pancreatic polypeptide (PP). NPY5R is coupled with the Gi/Go class of G proteins, leading to the inhibition of adenylate cyclase and a subsequent reduction in cyclic AMP (cAMP) levels. This signaling pathway influences a variety of physiological processes, particularly those related to energy balance, appetite regulation, and food intake. NPY5R is predominantly expressed in the hypothalamus, a region of the brain that plays a key role in controlling feeding behavior and energy homeostasis. Activation of NPY5R has been associated with the stimulation of appetite and the promotion of food intake, making it an important player in the regulation of body weight and metabolism. The receptor is believed to work in conjunction with other neuropeptide Y receptors, particularly NPY1R, to mediate the effects of NPY on feeding behavior. Due to its role in promoting food intake, NPY5R has been a target of interest for the development of anti-obesity therapies. By blocking or modulating NPY5R activity, it may be possible to reduce appetite and food intake, thus aiding in weight management. Research continues to explore the role of NPY5R in energy homeostasis, with ongoing studies aimed at better understanding its potential as a therapeutic target for obesity and other metabolic disorders.
This kit uses AAV vectors with a CMV promoter to co-express the NPY5R and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential NPY5R-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of NPY5R 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.