Monitoring gpcr-β-arrestin1/2 interactions in real time living systems to accelerate drug discovery

Arfaxad Reyes-Alcaraz*, Yoo Na Lee, Seongsik Yun, Jong Ik Hwang, Jae Young Seong

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


Interactions between G-protein coupled receptors (GPCRs) and β-arrestins are vital processes with physiological implications of great importance. Currently, the characterization of novel drugs towards their interactions with β-arrestins and other cytosolic proteins is extremely valuable in the field of GPCR drug discovery particularly during the study of GPCR biased agonism. Here, we show the application of a novel structural complementation assay to accurately monitor receptor-β-arrestin interactions in real time living systems. This method is simple, accurate and can be easily extended to any GPCR of interest and also it has the advantage that it overcomes unspecific interactions due to the presence of a low expression promoter present in each vector system. This structural complementation assay provides key features that allow an accurate and precise monitoring of receptor-β-arrestin interactions, making it suitable in the study of biased agonism of any GPCR system as well as GPCR c-terminus ‘phosphorylation codes’ written by different GPCR-kinases (GRKs) and post-translational modifications of arrestins that stabilize or destabilize the receptor-β-arrestin complex.

Original languageEnglish (US)
Article numbere59994
JournalJournal of Visualized Experiments
Issue number148
StatePublished - Jun 2019


  • Biochemistry
  • Drug development
  • Drug discovery
  • G-protein coupled receptors
  • Issue 148
  • Living systems
  • Real time
  • Structural complementation assay
  • β-arrestins

ASJC Scopus subject areas

  • General Neuroscience
  • General Chemical Engineering
  • General Biochemistry, Genetics and Molecular Biology
  • General Immunology and Microbiology


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