AAV ACTOne Gi-GPCR Assay Kit-SSTR5

Somatostatin Receptor 5 (SSTR5) is a G protein-coupled receptor (GPCR) that belongs to the somatostatin receptor family, which consists of five subtypes: SSTR1, SSTR2, SSTR3, SSTR4, and SSTR5. These receptors are activated by the peptide hormone somatostatin, which plays a key role in regulating endocrine and exocrine secretions, as well as cell proliferation and neurotransmission. SSTR5 is primarily coupled with the Gi/Go class of G proteins, leading to inhibition of adenylate cyclase, a reduction in cyclic AMP (cAMP) levels, and modulation of ion channels. This signaling cascade results in decreased hormone secretion, cell growth inhibition, and other regulatory effects, depending on the tissue and cell type involved. SSTR5 is expressed in various tissues, including the pancreas, pituitary gland, gastrointestinal tract, and central nervous system. In the pancreas, SSTR5 is involved in the regulation of insulin and glucagon secretion, making it an important player in glucose homeostasis. In the pituitary gland, SSTR5 helps regulate the secretion of growth hormone and other pituitary hormones. Due to its regulatory functions, SSTR5 has been implicated in several physiological and pathological conditions, including endocrine tumors, acromegaly (a condition characterized by excessive growth hormone secretion), and neuroendocrine tumors. Somatostatin analogs, which can target SSTR5 and other somatostatin receptors, are used therapeutically to treat these conditions by inhibiting excessive hormone secretion and controlling tumor growth. Research into SSTR5 continues to explore its broader role in disease mechanisms, particularly in the context of cancer and metabolic disorders, with the aim of developing more targeted therapies that exploit its inhibitory effects on hormone secretion and cell proliferation.
This kit uses AAV vectors with a CMV promoter to co-express the SSTR5 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential SSTR5-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of SSTR5 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.