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Overview
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Sphingosine-1-Phosphate Receptor 5 (S1PR5) is a G protein-coupled receptor (GPCR) that binds to sphingosine-1-phosphate (S1P), a bioactive lipid that regulates various physiological processes, including cell migration, survival, and immune function. S1PR5 is one of the five receptors in the S1P receptor family (S1PR1-5), each of which has distinct but overlapping roles in modulating cellular responses to S1P. S1PR5 is primarily coupled with Gi and G12/13 class G proteins. Through these G proteins, S1PR5 can influence a variety of intracellular signaling pathways, including those involved in cytoskeletal rearrangement, cell migration, and survival. Activation of S1PR5 by S1P can result in diverse cellular outcomes depending on the context, including changes in cell shape, motility, and intercellular communication. S1PR5 is expressed in several tissues, with notable expression in the central nervous system, particularly in oligodendrocytes (the cells responsible for forming myelin sheaths around neurons) and some regions of the brain. It is also expressed in natural killer (NK) cells and other immune cells, where it plays a role in their trafficking and function. In the central nervous system, S1PR5 is involved in the regulation of myelination and oligodendrocyte survival, making it relevant in the context of neurodegenerative diseases like multiple sclerosis (MS). In the immune system, S1PR5 contributes to the migration and function of NK cells, which are important for the body's defense against infections and tumors. Given its roles in myelination and immune cell trafficking, S1PR5 is a target of interest in research related to neuroinflammatory and neurodegenerative diseases, as well as cancer. Therapeutic modulation of S1PR5 may hold potential for treating conditions where abnormal myelination, immune cell dysfunction, or improper cell migration plays a key role.
This kit uses AAV vectors with a CMV promoter to co-express the S1PR5 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential S1PR5-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of S1PR5 drugs, such as agonists and antagonists, in a live-cell environment.Please contact us at for specific academic pricing.
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.
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Overview