AAV ACTOne Gi-GPCR Assay Kit-MCHR1

Melanin-Concentrating Hormone Receptor 1 (MCHR1) is a G protein-coupled receptor (GPCR) that binds to melanin-concentrating hormone (MCH), a neuropeptide primarily involved in the regulation of energy homeostasis, feeding behavior, and emotional responses. MCHR1 is primarily coupled with the Gi/Go class of G proteins, which inhibit adenylate cyclase, leading to a reduction in cyclic AMP (cAMP) levels. This signaling pathway influences various physiological processes, including appetite regulation, mood, and sleep. MCHR1 is widely expressed in the brain, particularly in regions such as the hypothalamus, which is crucial for controlling feeding behavior and energy balance. The receptor is also found in other brain areas associated with emotion and reward, such as the limbic system. Activation of MCHR1 by MCH promotes feeding behavior and energy storage, making it a key player in the regulation of body weight and metabolism. Because of its role in these processes, MCHR1 is a target of interest for developing treatments for obesity and metabolic disorders. Additionally, MCHR1 has been implicated in mood regulation, and research suggests it may also play a role in anxiety and depression. Given its involvement in energy balance, mood, and other physiological processes, MCHR1 continues to be a focus of research aimed at developing new therapeutic approaches for metabolic diseases, mood disorders, and other conditions related to dysregulated MCH signaling.
This kit uses AAV vectors with a CMV promoter to co-express the MCHR1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential MCHR1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of MCHR1 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.