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.
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April 2016
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Cover Image
Endoplasmic reticulumendosome contact sites. This pseudo-colored electron microscopy image shows the formation of inter-organelle membrane contact sites between late endosomes (magenta) and the endoplasmic reticulum (ER; green). This tethering results from the interaction between two ER-anchored proteins (VAP-A and VAP-B) and the late endosomeanchored protein STARD3NL. Mitochondria: brown; nucleus: blue. For further details see pp. 493-498. Image kindly provided by Fabien Alpy. - PDF Icon PDF LinkTable of Contents
Review Article|
April 11 2016
Compartmentalization of GPCR signalling controls unique cellular responses
Andrew M. Ellisdon;
Andrew M. Ellisdon
*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
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Michelle L. Halls
Michelle L. Halls
1
‡Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia
1To whom correspondence should be addressed (michelle.halls@monash.edu).
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Publisher: Portland Press Ltd
Received:
November 25 2015
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2016 Authors; published by Portland Press Limited
2016
Biochem Soc Trans (2016) 44 (2): 562–567.
Article history
Received:
November 25 2015
Citation
Andrew M. Ellisdon, Michelle L. Halls; Compartmentalization of GPCR signalling controls unique cellular responses. Biochem Soc Trans 15 April 2016; 44 (2): 562–567. doi: https://doi.org/10.1042/BST20150236
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