AAV ACTOne Gi-GPCR Assay Kit-FPR1

Formyl Peptide Receptor 1 (FPR1) is a G protein-coupled receptor (GPCR) that is primarily involved in the immune response. FPR1 is expressed on the surface of various immune cells, including neutrophils, monocytes, and macrophages. It is best known for its role in detecting and responding to formyl peptides, which are molecules derived from bacteria and mitochondria. These formyl peptides act as powerful chemoattractants, guiding immune cells to sites of infection or tissue damage. When FPR1 binds to formyl peptides, it activates signaling pathways through its coupling with Gi-type G proteins, leading to the inhibition of adenylate cyclase, a decrease in cyclic AMP (cAMP) levels, and the activation of downstream effectors such as phospholipase C (PLC). This signaling cascade results in various cellular responses, including chemotaxis (directed movement of immune cells toward the source of the formyl peptides), degranulation, and the production of reactive oxygen species (ROS), which are crucial for the immune system's ability to fight infections. FPR1 plays a critical role in the body's defense against bacterial infections by rapidly mobilizing neutrophils to the site of infection. However, it is also involved in non-infectious inflammatory responses and has been implicated in chronic inflammatory diseases, cancer, and tissue injury. Because of its central role in immune cell recruitment and activation, FPR1 is a potential target for therapeutic interventions aimed at modulating immune responses in various diseases.
This kit uses AAV vectors with a CMV promoter to co-express the FPR1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential FPR1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of FPR1 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.