Related Experiment Video
Updated: Jun 10, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Heterodimerization of the GABAB receptor-implications for GPCR signaling and drug discovery
Fiona H Marshall1, Steven M Foord
1Heptares Therapeutics, Biopark, Welwyn Garden City, Hertfordshire, UK.
Abstract:
The identification of the molecular nature of the GABA(B) receptor and the demonstration of its heterodimeric structure has led to extensive studies investigating the mechanism of activation and signaling. Phylogenetic studies suggest that the formation of the heterodimer is a relatively recent event arising in conjunction with the evolution of the central nervous system. Heterodimerization has now been demonstrated for many other G-protein-coupled receptors (GPCRs) and plays a role in signaling and trafficking. This presents both challenges and opportunities for GPCR drug discovery. In the case of the GABA(B) receptor the best hope for the development of new drugs directed at this receptor is from allosteric modulators. This chapter summarizes our current understanding of the molecular function of the GABA(B) receptor and recent developments in the identification of allosteric modulators. The broader implication of heterodimerization on GPCR function and drug discovery is also discussed.
More Related Videos
Related Concept Videos
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
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...
Activation and Inactivation of G Proteins
GPCR Desensitization
GPCRs Regulate Adenylyl Cylase Activity
Two...

