MultiScreen™ Beta-Arrestin Sensor Technology

High Throughput Detection of Biased Cell Signaling by Unmodified GPCRs

The First HTS β-Arrestin Assay for Native GPCRs in Recombinant or Primary Cells

  • No GPCR tagging required – assess true receptor pharmacology
  • No wash, homogeneous assay in 96- or 384-well microplate formats
  • Fully validated for transiently or stably transfected cells
  • No GRK2 co-transfection required
  • Available as assay kits, reagents, cell lines, and services

CHO-K1 cells stably expressing the µ opioid receptor were stimulated with known agonists and the MultiScreen β-arrestin assay run in a 384-well format.

Developing Candidates with Improved Efficacy & Safety Profiles

With the expanding importance of β arrestin-mediated signaling and the role of biased signaling in GPCR physiology, robust β-arrestin cell-based assays have become a critical piece of GPCR -targeted drug development.

First generation β-Arrestin assays rely on tagging both the GPCR-of-interest and β-arrestin with fusion proteins that when brought together mediate production of light. Multispan’s proprietary MultiScreen β-Arrestin sensor technology relies on unmodified GPCRS and thus overcomes receptor-tagging drawback of first-generation technologies, enabling high-throughput detection of beta-arrestin translocation induced by native GPCRs in vitro and in vivo.

Don’t let GPCR tagging bias your results. Find out how to unbias your GPCR signaling research.

MultiScreen β-Arrestin Assays –The Next Generation

MultiScreen β-Arrestin assays use translocation of β-arrestin as the assay readout; however, it is β-arrestin and a membrane ‘sensor’ that are tagged rather than the GPCR of interest. Upon recruitment, tagged arrestin comes within proximity of a membrane sensor which in turns results in a functional luciferase enzyme.

This scheme overcomes receptor tagging drawbacks and importantly offers a means to examine β-arrestin activation via
endogenous or orphan GPCRs using an assay format well suited for high throughput, cell-based screening.

Why are Unmodified GPCRs so Important?

GPCR tagging, required by other β-Arrestin assays can be deleterious, induce receptor conformational changes, lead to
steric hinderance, or modify receptor pharmacology – all of which impact the identification and optimization of highly
qualified drug candidates. MultiScreen β-Arrestin Sensor Technology enables researchers to:

  • Assess GPCRs in their native form for true pharmacology
  • Assay endogenously expressed GPCRs for more relevant data
  • Characterize orphan GPCRs to expand your target pool
  • Use a single cell line for multiple GPCR assays for accelerated drug development

MultiScreen™ β-Arrestin Assay Solutions

β-arrestin sensor technology is available as a portfolio of reagents, kits, and service to meet your specific assay needs:

  • MultiScreen™ β-Arrestin reagent options
    • HSV and Bacmam viral particles carrying MultiScreen™ β-Arrestin sensor genes
    • β-Arrestin sensors plasmids
    • MultiScreen™ β-Arrestin Assay Kits (Catalog MSBAK01)
    • MultiScreen™ β-Arrestin BacMam or HSV Assay Kits (Catalog MSBAKBM01-1, MSBAKHSV01-1)
  • Cell Lines
    • HEK293 and CHO parental cell lines stably expressing MultiScreen™ β-Arrestin sensors
    • 20+ GPCR stable cell lines co-expressing β-Arrestin sensor
    • > 1000 GPCR-expressing cell lines
  • Services
    • Custom stable cell line generation co-expression β-Arrestin sensor and GPCR
    • Development of MultiScreen™ β-Arrestin HTS assays
    • GPCR screening and profiling services using β-Arrestin assays

MultiScreen™ β-Arrestin Assay Protocols:

MultiScreen™ β-Arrestin Assay Kit
MultiScreen™ β-Arrestin BacMam Assay Kit
MultiScreen™ β-Arrestin HSV Assay Kit
MultiScreen™ Calcium 1.0 No Wash Assay Kit
MultiScreen™ TR-FRET cAMP 1.0 No Wash Assay Kit

Ready To Order A β-Arrestin Reagent Or Kit?