Compartmentalization of GPCR signalling controls unique cellular responses

Research output: Contribution to journalArticleResearchpeer-review

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.

Original languageEnglish
Pages (from-to)562-567
Number of pages6
JournalBiochemical Society Transactions
Volume44
Issue number2
DOIs
Publication statusPublished - 15 Apr 2016

Keywords

  • cAMP
  • Compartmentalization
  • G protein
  • G protein-coupled receptor (GPCR)
  • Protein complex
  • Signalosome

Cite this

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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.",
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Compartmentalization of GPCR signalling controls unique cellular responses. / Ellisdon, Andrew M.; Halls, Michelle L.

In: Biochemical Society Transactions, Vol. 44, No. 2, 15.04.2016, p. 562-567.

Research output: Contribution to journalArticleResearchpeer-review

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