title: Compartmentalization of GPCR signalling controls unique cellular responses.
abstract: With >800 members, G protein-coupled receptors (GPCRs) are the largest class of cell-surface signalling proteins, and their activation mediates diverse physiological processes. GPCRs are ubiquitously distributed across all cell types, involved in many diseases and are major drug targets. However, GPCR drug discovery is still characterized by very high attrition rates. New avenues for GPCR drug discovery may be provided by a recent shift away from the traditional view of signal transduction as a simple chain of events initiated from the plasma membrane. It is now apparent that GPCR signalling is restricted to highly organized compartments within the cell, and that GPCRs activate distinct signalling pathways once internalized. A high-resolution understanding of how compartmentalized signalling is controlled will probably provide unique opportunities to selectively and therapeutically target GPCRs.
authors.affiliation: Department of Biochemistry and Molecular Biology, Biomedicine Discovery Institute, Monash University, Wellington Rd, Clayton 3800, Australia Australian Research Council Centre of Excellence in Advanced Molecular Imaging, Monash University, Wellington Rd, Clayton 3800, Australia.
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Ellisdon
authors.affiliation: Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia michelle.halls@monash.edu.
authors.forename: Michelle L
authors.initials: ML
authors.lastname: Halls
mesh_terms: D002451:Cell Compartmentation; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D043562:Receptors, G-Protein-Coupled
keywords: G protein; G protein-coupled receptor (GPCR); cAMP; compartmentalization; protein complex; signalosome