Related Experiment Video
Updated: May 21, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
G-protein coupled receptor resensitization-appreciating the balancing act of receptor function
Maradumane L Mohan1, Neelakantan T Vasudevan, Manveen K Gupta
1Department of Molecular Cardiology, Lerner Research Institute, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, OH, 44195. prasads2@ccf.org.
G-protein coupled receptors (GPCRs) regulate cellular functions through activation, desensitization, and resensitization. This review emphasizes resensitization as a critical, dynamic process in GPCR regulation, often overlooked in drug discovery.
Area of Science:
- Cellular Biology
- Pharmacology
- Biochemistry
Background:
- G-protein coupled receptors (GPCRs) are crucial for cellular signaling, impacting vision, cardiac function, and more.
- GPCRs are key drug targets due to their roles in numerous physiological and pathological processes.
- GPCRs function cyclically through activation, desensitization, and resensitization.
Purpose of the Study:
- To highlight the critical, yet underappreciated, role of GPCR resensitization.
- To discuss resensitization as a dynamic and mechanistic regulator of GPCR function.
- To provide a comprehensive overview of GPCR activation, desensitization, and resensitization.
Main Methods:
- Literature review focusing on GPCR signaling pathways.
- Analysis of existing research on receptor activation, desensitization, and resensitization.
- Utilizing the beta-adrenergic receptor as a model system for mechanistic insights.
Main Results:
- Significant research has focused on GPCR activation and desensitization, with less attention paid to resensitization.
- Evidence suggests resensitization is not merely homeostatic but an acutely regulated process.
- Mechanisms of resensitization are crucial for sustained GPCR signaling and cellular responses.
Conclusions:
- Resensitization is a vital component of GPCR regulation, influencing downstream signaling.
- Understanding resensitization dynamics is essential for comprehensive GPCR research and drug development.
- The principles governing resensitization in beta-adrenergic receptors may apply broadly across other GPCRs.
More Related Videos
09:21BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
Published on: November 7, 2025
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Related Concept Videos
GPCR Desensitization
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G-protein Coupled Receptors
G-protein Coupled Receptors
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...