G Protein Independent Functional Assays

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G Protein Independent Functional Assays

For Research Use Only. Not For Clinical Use.

Creative Biolabs provides G protein independent functional assay services based on multiple assay formats to accelerate GPCR research and drug development. We can further help speed up your drug discovery by combining high-throughput technology.

Introduction of G Protein Independent Functional Assays

G protein-coupled receptors (GPCRs) play an important role in health and disease. They represent the largest family of druggable targets. The development of GPCR assays has always been the focus of drug discovery research. Efforts have been made to develop functional assays to provide more comprehensive information for GPCR drug discovery. Choosing the right assay is important for the early stage of drug discovery.

As the activation of G protein by GPCRs is the basis of transmembrane signal transduction, early GPCR functional assays mainly depend on G proteins. With further understanding of GPCR signal transduction, many G protein independent assays have been developed to detect GPCR activity. These assays can also be combined with high-throughput technology, automation technology, label-free technology and other technologies to provide more additional valuable information for drug development and improve the success rate in drug discovery.

Examples of G protein- and β-arrestin-mediated downstream signaling pathways on GPCRs.Figure 1. Examples of G protein- and β-arrestin-mediated downstream signaling pathways on GPCRs. (Bologna Z, et al., 2017)

G Protein Independent Functional Assay Services

We offer our customers with a comprehensive selection of G protein independent functional assays to meet their different research needs.

Assays Suitable GPCRs Description
GPCR internalization assay Any GPCR
  • GPCR internalization is closely related to signal transduction.
  • Robust and sensitive to follow and quantify GPCR internalization.
  • Applicable to living cells.
  • High-content screening format is available.
β-arrestin recruitment assay Any GPCR
  • β-arrestin recruitment independent of G protein signaling is a powerful tracker for GPCR activation.
  • Useful in the study of ligand pharmacology, antagonist mode screening, and GPCR deorphanization.
  • Applicable to living cells.
Label free assay Any GPCR
  • Capable of capturing the integrated cell response.
  • Biosensors are generally employed in label-free cell-based assays to monitor cell response.
  • Applicable to native live cells.
GPCR dimerization assay Any GPCR
  • GPCR dimers are considered operative pharmacological targets.
  • Protein complementation assays (PCAs) based on either fluorescence or luminescence are widely used.
  • Compatible with high throughput screening

Our Advantages

  • Customized services based on multiple assays formats.
  • One-stop solutions for all your problems.
  • High-quality and reliable results under strict quality control conditions.
  • Fast turnaround time and competitive price.

Creative Biolabs provides our customers with customized G protein independent functional assay services in a time- and cost-effective manner. Our experts will work closely with you to fully meet your requirements.

If you are interested in our services or have any specific needs, please feel free to contact us for more details.

References

  1. Bologna Z, et al. Biased G protein-coupled receptor signaling: new player in modulating physiology and pathology. Biomolecules & therapeutics, 2017, 25(1): 12.
  2. Zhang R & Xie X. Tools for GPCR drug discovery. Acta Pharmacologica Sinica, 2012, 33(3): 372-384.
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