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Updated: Dec 15, 2025
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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
Published on: December 2, 2022
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Advances in G protein-coupled receptor high-throughput screening
Emily A Yasi1, Nicholas S Kruyer2, Pamela Peralta-Yahya3
1School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA, 30332, United States.
Current Opinion in Biotechnology
|July 13, 2020
Summary
High-throughput screening (HTS) of G protein-coupled receptors (GPCRs) accelerates drug discovery and deorphanization. Advances in cell-based, in vitro, and computational methods are key for personalized medicine.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- G protein-coupled receptors (GPCRs) are crucial cell surface proteins initiating signaling cascades.
- Over 30% of FDA-approved drugs target GPCRs, highlighting their significance in medicine.
Purpose of the Study:
- To review recent advancements in high-throughput screening (HTS) for G protein-coupled receptors (GPCRs).
- To focus on cell-based and in vitro assays, alongside computational approaches for GPCR HTS.
Main Methods:
- Review of recent literature on cell-based assays for GPCR HTS.
- Highlighting advances in in vitro assays using purified receptors.
- Discussion of computational strategies employed in GPCR HTS.
Main Results:
- GPCR HTS has successfully identified novel drugs and repurposed existing ones.
- HTS has facilitated the deorphanization of GPCRs with previously unknown ligands.
- Advancements are driving the use of GPCR HTS beyond drug discovery into basic biological research.
Conclusions:
- High-throughput screening is a vital tool for G protein-coupled receptor drug discovery.
- Emerging automation and computational methods enhance GPCR HTS capabilities.
- GPCR HTS is poised to significantly impact personalized medicine by probing biological processes.
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