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GPCRs (G protein-coupled receptors) are important proteins in cell signaling that bind the nucleotides guanosine triphosphate (GTP) and guanosine diphosphate (GDP). GPCRs play a role in an incredible array of functions in the human body, from sensation to growth to hormone responses. Among the more than 500 drug targets that have been discovered, GPCRs account for the majority. The increased understanding of these receptors has greatly influenced modern medicine. GPCRs have been widely used to screen drugs and study the etiology and pathogenesis of autoimmune diseases. Therefore, it is necessary for researchers to construct cell lines that stably overexpress GPCRs.
So far, Creative Biogene has successfully constructed GPCR over-expressing stable cell lines of various species, which has become one of the world's largest banks of GPCR cells. These cell lines have been verified in the functionality and stability through reporter gene assay or intracellular calcium assay, to satisfy our customers' requirements for screening GPCR-target drugs and final evaluation.
Advantages of Our GPCR Stable Cell Lines
G protein-coupled receptor (GPCR), with approximately 800-1000 members, is the largest receptor superfamily in organisms. What this type of receptors has in common is that they all have seven transmembrane α-helices in their three-dimensional structure, and there are G protein binding sites on the C-terminus of the peptide chain and the inner loop connecting the 5th and 6th transmembrane helices. Their main function is to transmit extracellular information into cells by interacting with G proteins. GPCRs are involved in the regulation of a variety of physiological processes, including olfaction, cognition, muscle contraction, endocrine and exocrine secretions, metabolism, inflammation, and immunity.
Due to the large number and important physiological functions of GPCRs, GPCRs have become important targets for medical research and drug development. However, studying GPCRs can be challenging due to their complex nature and the need for stable and reliable cell lines for experimentation. In recent years, the application of GPCR stable cell lines has become increasingly prevalent in research, offering scientists a valuable tool to unravel the intricacies of cellular signaling pathways.
Applications for GPCR stable cell lines include:
Case Study 1
GPR84 is an orphan G protein-coupled receptor expressed on monocytes, macrophages, and neutrophils and is significantly upregulated in response to inflammatory stimuli. The researchers conducted a comprehensive study of GPR84 receptor signaling and function in recombinant and primary immune cells using GPR84 cell lines to decipher how GPR84 activation regulates important physiological functions of these cells.
Figure 1. GPR84 did not couple to Gq proteins, since embelin failed to induce calcium flux in a GPR84 expressing cell line. Also, no increase in cAMP was observed when embelin was tested in GPR84 expressing cells in the absence of forskolin, indicating no signaling of GPR84 through the Gs pathway. (Gaidarov I, et al., 2018)
Case Study 2
Colorectal cancer (CRC) responds poorly to immune-mediated cytotoxicity. Low expression of corticotropin-releasing hormone receptor 2 (CRHR2) in CRC promotes tumor survival, growth, and epithelial-mesenchymal transition (EMT) in vitro and in vivo. Researchers compared the sensitivity of CRC cells to CH11-induced apoptosis between Urocortin-2 (Ucn2)-stimulated parental and CRHR2-overexpressing CRC cell lines and and identified targets of CRHR2/Ucn2 signaling through in vitro and ex vivo analyses.
Figure 2. CRHR2/Ucn2 signaling specifically promotes Fas upregulation in CRC. CRHR2 overexpressing cell line and EV CRC cell lines were treated for 24 h with 0.1 mM Ucn2 before evaluation of Fas expression at the mRNA and protein level. (Pothoulakis C, et al., 2018)
Q: What are GPCRs?
A: G-protein coupled receptors (GPCRs) are transmembrane proteins that play a crucial role in mediating a wide range of cellular responses to external stimuli. They are involved in various physiological processes such as neurotransmission, hormone secretion, immune response, and sensory perception.
Q: What are GPCR Cell Lines?
A: GPCR cell lines are artificially engineered cell systems that express a specific GPCR of interest. These cell lines serve as valuable tools for research, enabling scientists to investigate the functional properties of GPCRs, study signaling pathways, and facilitate drug discovery efforts.
Q: How are GPCR cell lines generated?
A: GPCR cell lines are generated by introducing the GPCR gene into a host cell line. This gene expression results in stable cell populations that express the receptor on their surface.
Q: What are some functional assays that can be performed using GPCR cell lines?
A: GPCR cell lines can be used for ligand binding studies, measuring receptor activation and desensitization kinetics, evaluating downstream signaling events, and conducting drug screening.
Q: What are fluorescent and bioluminescent tags used for in GPCR research?
A: Fluorescent and bioluminescent tags are used to monitor GPCR activity in real-time, allowing researchers to visualize GPCR localization, trafficking, ligand binding, and dynamic processes such as internalization and receptor recycling.
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