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MULTISCREEN™ Beta-Arrestin Assay Technology

High Throughput Detection of Biased Cell Signaling by Unmodified GPCRs

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The First HTS Beta-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

Example: Beta-Arrestin Sensor Application in CXCR7 Assay Solution

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 Enhanced Efficacy & Safety Profiles Using Beta-Arrestin Assays

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

First generation Beta-Arrestin assays rely on tagging both the GPCR-of-interest and Beta-Arrestin with fusion proteins that when brought together mediate production of light. Multispan’s proprietary MULTISCREENTM Beta-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.

MULTISCREENTM Beta-Arrestin Assays: Pioneering Next-Gen GPCR Assays

MULTISCREENTM Beta-Arrestin assays utilize the translocation of Beta-Arrestin for the assay readout, a process distinct due to the tagging of Beta-Arrestin and a membrane sensor instead of the GPCR itself. This approach facilitates closer proximity between the tagged arrestin and the membrane sensor, initiating a functional luciferase enzyme reaction.

By avoiding GPCR tagging, it sidesteps the associated drawbacks, offering a viable method to study Beta-Arrestin activation in endogenous or orphan GPCRs. This technique is designed for high throughput, cell-based screening, promising efficiency and accuracy in GPCR research.

For detailed insights, consult with our technical team or request a quote. 

Beta Arrestin Assay Workflow

Poster: Technical Poster on Beta-Arrestin Assay Measuring Native GPCRs

Why are Unmodified GPCRs so Important?

In the highly specialized domain of GPCR-targeted drug development, the importance of working with unmodified GPCRs cannot be overstated. Traditional Beta-Arrestin assays necessitate GPCR tagging, a process that has been shown to potentially induce deleterious receptor conformational changes, promote steric hindrance, or even alter receptor pharmacology. Such modifications not only compromise the physiological relevance of the data generated but can significantly impact the identification and optimization of highly qualified drug candidates.

Recognizing these challenges, the advanced MULTISCREENTM Beta-Arrestin Sensor Technology stands out as a reliable and precise solution. Here are the prominent ways this technology is shaping the future of GPCR research:

True Pharmacology: By enabling the assessment of GPCRs in their native form, it safeguards the integrity of receptor pharmacology, paving the way for data that mirrors the true physiological interactions more closely.

Relevance in Data: The technology allows for the assay of endogenously expressed GPCRs, ensuring that the data generated is highly relevant and reflective of the in-vivo conditions, thus enhancing the accuracy of preliminary screenings in drug development processes.

Expanding Target Pool: The MULTISCREENTM Beta-Arrestin Sensor Technology facilitates the characterization of orphan GPCRs, broadening the scope of potential targets and advancing opportunities in GPCR research and drug development.

Accelerated Drug Development: Perhaps one of the most remarkable features is its compatibility with a single cell line for conducting multiple GPCR assays. This not only streamlines the operational workflow but remarkably accelerates the pace of drug development, saving both time and resources while maintaining a high standard of reliability and efficiency.

By prioritizing unmodified GPCRs, the MULTISCREENTM Beta-Arrestin Sensor Technology stands as a formidable tool in the researcher’s arsenal, promising a revolution in GPCR-targeted drug development through enhanced efficacy and the true realization of the potentials hidden in GPCR signaling pathways.

MULTISCREEN™ Beta-Arrestin Assay Solutions

Beta-Arrestin sensor technology is available as a portfolio of reagents, kits, and services to meet your specific assay needs:

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

GPCR-Arrestin Co-Expressed MULTISCREENTM Stable Cell lines

Receptor FamilyReceptorSpeciesParentalStable Cell LinesDivision-Arrested Cells Membranes
Adrenergicbeta2humanHEK293T β-Arrestin1CA1438BA1DCA1438BA1MCA1438BA1
beta2humanHEK293T β-Arrestin2CA1438BA2DCA1438BA2MCA1438BA2
AngiotensinAT1humanHEK293T β-Arrestin1HA1417- BA1DHA1417- BA1MHA1417- BA1
AT1humanHEK293T β-Arrestin2HA1417-BA2DHA1417-BA2MHA1417-BA2
CannabinoidCB1 MUTANT BhumanCHO-K1 β-Arrestin2CA1513BA2-1DCA1513BA2-1MCA1513BA2-1
CB2humanCHO-K1 β-Arrestin2CA1230BA2-1DCA1230BA2-1MCA1230BA2-1
CB2mouseCHO-K1 β-Arrestin2CAm1230BA2-1DCAm1230BA2-1MCAm1230BA2-1
CB2ratCHO-K1 β-Arrestin2CAr1230BA2-1DCAr1230BA2-1MCAr1230BA2-1
CB2ratCHO-K1 β-Arrestin2CAr1230BA2-1aDCAr1230BA2-1aMCAr1230BA2-1a
ChemokineCXCR7humanHEK293T β-Arrestin2CA1150-BA2DCA1150-BA2MCA1150-BA2
Citric Acid Cycle IntermediatesGPR91humanCHO-K1 B-Arrestin2CA1141BA2-1DCA1141BA2-1MCA1141BA2-1
Free Fatty AcidGPR120LhumanHEK293T β-Arrestin2CA1522DCA1522MCA1522
GPR40humanCHO-K1 β-Arrestin2CA1101-1DCA1101-1MCA1101-1
GPR40ratCHO-K1 β-Arrestin2CAr1101-1DCAr1101-1MCAr1101-1
GPR40cynomolgus monkeyCHO-K1 β-Arrestin2CApc1101-1DCApc1101-1MCApc1101-1
GlucagonGIPhumanHEK293T β-Arrestin2CA1290DCA1290MCA1290
GIPhumanHEK293T β-Arrestin2CA1290BA1DCA1290BA1MCA1290BA1
GLP-1humanCHO-K1 β-Arrestin2CA1267-1DCA1267-1MCA1267-1
GLP-1humanHEK293T β-Arrestin2CA1267BA2DCA1267BA2MCA1267BA2
GlucagonhumanCHO-K1 β-Arrestin2CA1266-1DCA1266-1MCA1266-1
HistamineH4humanHEK293T β-Arrestin2CA1030BA2DCA1030BA2MCA1030BA2
OpioiddeltahumanCHO-K1 β-Arrestin2CA1351-1DCA1351-1MCA1351-1
kappahumanCHO-K1 β-Arrestin2CA1352-1aDCA1352-1aMCA1352-1a
kappahumanCHO-K1 β-Arrestin2CA1352BA2-1DCA1352BA2-1MCA1352BA2-1
muhumanCHO-K1 β-Arrestin2CA1350-1aDCA1350-1aMCA1350-1a
NOPhumanCHO-K1 β-Arrestin2CA1354-1DCA1354-1MCA1354-1
OrphanGPR35 (short form)humanCHO-K1 β-Arrestin2CA1096-1DCA1096-1MCA1096-1
GPR35 (long form)humanCHO-K1 β-Arrestin2CA1523-1DCA1523-1MCA1523-1
GPR35 (long form) T108M MutanthumanCHO-K1 β-Arrestin2CA1524-1DCA1524-1MCA1524-1
GPRC5AhumanHEK293T β-Arrestin2CA1525DCA1525MCA1525
MRGX2humanHEK293T β-Arrestin2CA1257aBA2DCA1257aBA2MCA1257aBA2
Proton-Sensing ReceptorsGPR4humanHEK293T β-Arrestin2CA1100DCA1100MCA1100
GPR65humanHEK293T β-Arrestin2CA1121DCA1121MCA1121
GPR68humanHEK293T β-Arrestin2CA1123DCA1123MCA1123
GPR132humanHEK293T β-Arrestin2CA1066DCA1066MCA1066
Parental CellsHEK293T β-Arrestin2CA0001MCA0001
CHO-K1 β-Arrestin2CA0001-1MCA0001-1

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