Related Experiment Video
Updated: Jun 25, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Modelling the activation of G-protein coupled receptors by a single drug
P J Woodroffe1, L J Bridge, J R King
1Centre for Mathematical Medicine, Division of Theoretical Mechanics, School of Mathematical Sciences, University of Nottingham, Nottingham NG72RD, UK.
Abstract:
In this paper, the most popular proposed mechanism for activation of G-protein coupled receptors (GPCRs)--the shuttling mechanism--is modelled mathematically. An asymptotic analysis of this model clarifies the dynamics of the system in the presence of a drug, in particular identifying which reactions dominate during the different timescales. The modelling also reveals challenging behaviour in the form of a peak response. This new mechanism gives simple explanations for complex, possibly misunderstood, behaviour.
Related Concept Videos
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
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...
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
Activation and Inactivation of G Proteins
G-protein Coupled Receptors

