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Webinar: Application of β-Arrestin Assays to the Orphan GPCR World

Kinase dendrogram

Wednesday, December 6, 2017

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(25-minute seminar, 5-minute Q&A)

University Paris Descartes, INSERM, CNRS Presenters:

Ralf Jockers, Ph.D., Research Director
Atsuro Oishi, M.D., Ph.D., Postdoctoral Research Fellow

GPCRs are privileged drug targets. Approximately 100 receptors still escape from the drug discovery process as they are orphans, without any known cognate ligand. To setup deorphanization assays, spontaneous receptor activity can be instrumental. Here we will present the various aspects to be considered when determining constitutive and allosteric β-arrestin recruitment of orphan GPCRs.

Recent phylogenetic studies proposed three orphan receptors, GPR61, GPR62, and GPR135, to belong to the melatonin receptor subfamily, but their capacity to bind melatonin and their biochemical functions were not well characterized. We revealed that melatonin is not the cognate ligand of these orphan GPRs, but they have distinct spontaneous activities including β-arrestin recruitment. Interestingly, by forming heteromers with the melatonin MT2 receptor, these orphan GPRs inhibit melatonin induced β-arrestin recruitment allosterically (Oishi, Sci. Rep., 2017).

In this webinar, we will highlight the application of several β-arrestin assays to analyze orphan GPCRs, and discuss the advantages and characteristics of each assay.

What will be covered?

  • How to apply β-arrestin assays to the characterization of orphan GPCRs
  • How to design β-arrestin assays for receptors with spontaneous activity
  • Comparison and complementary properties of different β-arrestin assay formats
  • Allosteric modulation of the β-arrestin pathway in GPCR heteromers

Who should attend?

  • GPCR scientists
  • Researchers discovering new ligands to orphan GPCRs
  • Basic researchers, assay developers, and lead identification drug discovery scientists