GPCR Functional Cell Lines
G protein-coupled receptors (GPCRs), a large family of seven transmembrane protein receptors, represent the largest class of mammalian cell surface receptors. Although they are the targets of many approved drugs, only few GPCRs have been developed. This field still has tremendous potential for disease research and drug discovery.
Figure 1. The number of GPCRs targeted by approved drugs. (Sriram K & Insel P A, 2018)
Engineered cell lines are powerful tools for GPCR research and drug discovery. With experienced scientists and advanced techniques, Creative Biolabs can provide a variety of GPCR functional cell lines to meet different needs of our customers toward the exploration of GPCR. Our cell lines have been functionally validated by downstream assays.
β-Arrestin GPCR Cell Lines
β-arrestin GPCR cell lines are designed to co-express the enzyme accepter (EA)-fused β-arrestin and a PK-tagged GPCR. The activation of PK-tagged GPCR can induce the recruitment of EA-fused β-arrestin, which results in the generation of chemiluminescent signals.
Calcium Gq Cell Lines
Calcium Gq cell lines are designed to overexpress naturally Gq coupled GPCRs. In response to agonist stimulation of receptors, these cell lines can be used to detect calcium mobilization.
cAMP-Activated GPCR Cell Lines
cAMP-activated GPCR cell lines are designed to co-express a membrane-associated cAMP biosensor and GPCRs. They can be used as a sensitive tool to study the molecular mechanism and kinetics underlying the GPCR activation by real-time monitoring the fluorescence intensity changes.
cAMP-Gs/Gi Cell Lines
cAMP-Gs/Gi cell lines are designed to overexpress naturally Gs or Gi coupled GPCRs. In response to agonist stimulation of receptors, these cell lines can be used to detect the increase of intracellular cAMP levels. These cell lines can also help expedite drug screening.
ChemiScreening GPCR Cell Lines
ChemiScreening GPCR cell lines contain high levels of the promiscuous G protein. They are designed to couple the receptor to the calcium signaling pathway. These cell lines are ideal tools for GPCR screening.
ChemiLuminal GPCR Cell Lines
ChemiLuminal GPCR cell lines are designed to express a photoprotein that can be activated by calcium. The ligand-induced calcium flux can produce sensitive luminescence. These cell lines are ideal for luminescent analysis of agonists and antagonists at the target protein.
GPCR Internalization Cell Lines
GPCR internalization cell lines are designed to co-express an enzyme accepter (EA)-tag localized to the endosomes and PK-tagged GPCR. The activation of PK-tagged GPCR can induce the internalization of receptor in EA-tagged endosomes, which results in the generation of chemiluminescent signals.
Pharmacotrafficking Cell Lines
Pharmacological chaperones are drugs acting as protein chaperones. Pharmacotrafficking cell lines are designed as a chemiluminescent-based quantitative tool. By facilitating the proper folding of misfolded proteins and assisting in their transport to an intended location, the compounds that act as pharmacological chaperones can be identified and optimized.
More GPCR functional cell lines are under development. If you are interested in our cell lines or have any specific needs, please feel free to contact us.
References
- Sriram K & Insel P A. G protein-coupled receptors as targets for approved drugs: how many targets and how many drugs?. Molecular pharmacology, 2018, 93(4): 251-258.
- Cook J L. G Protein–coupled receptors as disease targets: Emerging paradigms. The Ochsner Journal, 2010, 10(1): 2.