Assays for detecting arrestin interaction with GPCRs

Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  • Nicole A. Perry-Hauser
  • Wesley B. Asher
  • Maria Hauge Pedersen
  • Jonathan A. Javitch

The four vertebrate arrestins play a key role in the desensitization and internalization of G protein-coupled receptors (GPCRs) and also mediate receptor-dependent signaling. Recent work has shown that bias for arrestin vs G protein signaling could offer certain therapeutic advantages (or disadvantages) in different systems, making assays that measure arrestin binding to receptors important for drug discovery efforts. Herein, we briefly review several commonly used techniques for measuring arrestin binding to receptors, as well as provide an in-depth and methodologically focused review of two methods that do not require receptor modification. The first approach measures direct binding between purified arrestin and rhodopsin, and the second measures the recruitment of arrestin to receptors in living cells.

Original languageEnglish
Title of host publicationBiomolecular Interactions Part A
EditorsArun K. Shukla
Number of pages23
PublisherAcademic Press
Publication date2021
Pages43-65
Chapter3
ISBN (Print)9780128233511
DOIs
Publication statusPublished - 2021
SeriesMethods in Cell Biology
Volume166
ISSN0091-679X

Bibliographical note

Publisher Copyright:
© 2021 Elsevier Inc.

    Research areas

  • Arrestin, Cell signaling, G protein-coupled receptors (GPCRs), Unmodified receptor

ID: 298039741