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.

journal_name

Biochem Soc Trans

authors

Ellisdon AM,Halls ML

doi

10.1042/BST20150236

subject

Has Abstract

pub_date

2016-04-15 00:00:00

pages

562-7

issue

2

eissn

0300-5127

issn

1470-8752

pii

BST20150236

journal_volume

44

pub_type

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