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.

GPCR assay kits used in compound screening

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:

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