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 Transjournal_title
Biochemical Society transactionsauthors
Ellisdon AM,Halls MLdoi
10.1042/BST20150236subject
Has Abstractpub_date
2016-04-15 00:00:00pages
562-7issue
2eissn
0300-5127issn
1470-8752pii
BST20150236journal_volume
44pub_type
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