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Updated: Feb 10, 2026
13:14
Genetic Barcoding with Fluorescent Proteins for Multiplexed Applications
Published on: April 14, 2015
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Multiplexed profiling of GPCR activities by combining split TEV assays and EXT-based barcoded readouts.
Sabrina Galinski1, Sven P Wichert1,2, Moritz J Rossner3
1Molecular Neurobiology, Department of Psychiatry, Ludwig Maximilian University of Munich, Germany, Nussbaumstr. 7, Munich, 80336, Germany.
Scientific Reports
|May 27, 2018
Summary
A new assay, GPCRprofiler, enables simultaneous measurement of drug effects on multiple G protein-coupled receptors (GPCRs). This technology aids in developing selective therapeutics by assessing compound activity across related and unrelated GPCR targets.
Area of Science:
- Pharmacology
- Molecular Biology
- Assay Development
Background:
- G protein-coupled receptors (GPCRs) are crucial for physiological regulation and are major drug targets.
- Developing selective drugs is challenging due to structural similarities among GPCR subfamilies.
- Simultaneous assessment of GPCR activity is needed to evaluate compound selectivity.
Purpose of the Study:
- To present GPCRprofiler, a novel cell-based multiplexed assay for measuring GPCR activity.
- To enable simultaneous profiling of compound effects on multiple GPCRs.
- To demonstrate the utility of GPCRprofiler in assessing drug selectivity and polypharmacology.
Main Methods:
- Utilizes a β-arrestin recruitment strategy combined with split TEV protein-protein interaction and EXT-based barcode technologies.
- Employs massively parallelized reporter assays for simultaneous measurements.
- Incorporates normalization of barcode reporters for quantitative, parallelized assays.
Main Results:
- Successfully demonstrated the specificity of endogenous agonists across 19 different GPCRs.
- Revealed polypharmacological effects of two antipsychotic drugs on GPCR activities.
- Validated the quantitative and parallelized nature of the assay.
Conclusions:
- GPCRprofiler is a flexible and scalable assay for simultaneous GPCR activity profiling.
- The assay facilitates the assessment of compound selectivity and polypharmacology in living cells.
- This technique supports the development of novel therapeutics targeting GPCRs.
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