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Updated: Nov 22, 2025
07:41
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
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G protein-coupled receptors: structure- and function-based drug discovery.
Dehua Yang1,2, Qingtong Zhou3, Viktorija Labroska1,4
1The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203, Shanghai, China.
Signal Transduction and Targeted Therapy
|January 8, 2021
Summary
G protein-coupled receptors (GPCRs) are key drug targets. Recent advances in understanding GPCR structure-function relationships accelerate drug discovery, shifting from random screening to knowledge-driven design.
Area of Science:
- Pharmacology
- Biochemistry
- Medicinal Chemistry
Background:
- G protein-coupled receptors (GPCRs) represent a major class of drug targets.
- Historically, drug discovery relied on random ligand screening.
- Recent breakthroughs have revolutionized GPCR-focused drug development.
Purpose of the Study:
- To provide a comprehensive overview of recent advancements in GPCR research.
- To highlight the transition towards knowledge-driven drug design for GPCRs.
- To inform a broad audience interested in drug discovery.
Main Methods:
- Review of recent scientific literature on GPCR structure-function relationships.
- Analysis of emerging trends in GPCR-targeted drug design.
- Synthesis of information on accelerated drug development facilitated by GPCR understanding.
Main Results:
- Significant progress in elucidating GPCR structure-function relationships.
- Demonstration of accelerated drug development timelines.
- Shift from random screening to structure-based and knowledge-driven approaches.
Conclusions:
- Understanding GPCR structure-function is crucial for efficient drug discovery.
- Knowledge-driven design significantly enhances the pace of therapeutic development.
- GPCRs remain a highly promising target family for novel therapeutics.
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