G-Protein-Coupled Receptors (GPCR)

G-Protein Coupled Receptors (GPCRs) are known as seven transmembrane spanning receptors or metabotropic receptors. They are the largest family of membrane receptors in the entire human genome. As the name suggests, it functions by coupling itself with G-protein to regulate intracellular signalling pathways. G-proteins possess GTPase activity and controls the function of these receptors. The structure of GPCRs consists of a single polypeptide chain comprising of seven transmembrane helices, where N-terminal domain is extracellular and C-terminal is located intracellularly.

GPCRs works in a manner where agonist binds with the receptors and that causes receptors to undergo conformational change, activating G-protein heterodimer. This leads to activation of its downstream signalling pathways. Ligand-induced ?-arrestin recruitment plays a critical role in GPCR regulation through receptor desensitization and internalization and also mediates G-protein independent signal transduction. The GPCRs works via secondary messengers such as cAMP, which is generated by Adenylyl Cyclase, a target for GPCRs, or DAG and IP3, which uses Phospholipase C, another target of GPCRs.

Study of GPCRs has so much potential uncovering lot of physiological processes inside the cells. One third of the drugs available on the market to date is based on targeting GPCRs shows the importance of GPCRs research. At AAT bioquest we offer a wide variety of the products.

Figure 1.Nociceptin-stimulated calcium response was measured in CHO-Ga16-NOP cells with Cal-520®, AM (Cat#21130). CHO-Ga16-NOP cells were seeded overnight at 60,000 cells/100 µL/well in a Costar black wall/clear bottom 96-well plate. The cells were incubated with equal volume (100 µL) of 10 µM Cal-520®, AM with 2 mM probenecid in Hanks with 20 mM Hepes buffer (HHBS) at 37 °C for 1 hour. The Cal-520®, AM loading solution was replaced with HHBS and 1 mM probenecid. Nociceptin was added by FlexStation® (Molecular Devices) to achieve the final indicated concentrations.

Product Ordering Information

Table 1. Ordering Info for ScreenQuest GPCR Cell Lines Products

Cat# Product Name Unit Size
38000 Screen Quest™ HEK-CNGC-Amylin 3 Receptor Cells Each
38001 Screen Quest™ HEK-CNGC-Cannabinoid Receptor 1 Cells Each
38002 Screen Quest™ CHO-Ga16- Chemokine (C-C) Receptor 2B Cells Each
38003 Screen Quest™ HEK-CNGC-Chemokine (C-X-C motif) Receptor 4 Cells Each
38004 Screen Quest™ HEK-CNGC-Dopamine Receptor 1 (DRD1) Cells Each
38005 Screen Quest™ HEK-CNGC-Glucagon-like Receptor 1 (GLP1R) Cells Each
38006 Screen Quest™ HEK-CNGC-Opiate Receptor-like 1 (ORL1) Cells Each
38100 Screen Quest™ Human Nociceptin Receptor Ga16 coupled CHO Cells (NOP-Ga16) Each
38101 Screen Quest™ CHO-Gqi Chimera Cell line Each
38102 Screen Quest™ CHO-Gqo Chimera Cell line Each
38103 Screen Quest™ CHO-Gqz Chimera Cell line Each
38104 Screen Quest™ CHO-Gqs Chimera Cell line Each
38105 Screen Quest™ CHO-Ga16 Chimera Cell line Each


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