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Cell Signal. 2017 May;33:1-9. doi: 10.1016/j.cellsig.2017.02.004. Epub 2017 Feb 8.

The G protein-coupled receptor N-terminus and receptor signalling: N-tering a new era.

Author information

1
Molecular Pharmacology Group, Victor Chang Cardiac Research Institute, Darlinghurst, NSW 2010, Australia; St Vincent's Clinical School, University of New South Wales, Darlinghurst, NSW 2010, Australia. Electronic address: j.coleman@victorchang.edu.au.
2
Molecular Pharmacology Group, Victor Chang Cardiac Research Institute, Darlinghurst, NSW 2010, Australia; St Vincent's Clinical School, University of New South Wales, Darlinghurst, NSW 2010, Australia.
3
Molecular Pharmacology Group, Victor Chang Cardiac Research Institute, Darlinghurst, NSW 2010, Australia; St Vincent's Clinical School, University of New South Wales, Darlinghurst, NSW 2010, Australia. Electronic address: n.smith@victorchang.edu.au.

Abstract

G protein-coupled receptors (GPCRs) are a vast family of membrane-traversing proteins, essential to the ability of eukaryotic life to detect, and mount an intracellular response to, a diverse range of extracellular stimuli. GPCRs have evolved with archetypal features including an extracellular N-terminus and intracellular C-terminus that flank a transmembrane structure of seven sequential helices joined by intracellular and extracellular loops. These structural domains contribute to the ability of a GPCR to be correctly synthesised and inserted into the cell membrane, to interact with its cognate ligand(s) and to couple with signal-transducing heterotrimeric G proteins, allowing the activated receptor to selectively modulate a number of signalling cascades. Whilst well known for its importance in receptor translation and trafficking, the GPCR N-terminus is underexplored as a participant in receptor signalling. This review aims to discuss and integrate recent advances in knowledge of the vital roles of the GPCR N-terminus in receptor signalling.

KEYWORDS:

G protein-coupled receptor; GPCR; N-terminus; Proteolysis; Signalling

PMID:
28188824
DOI:
10.1016/j.cellsig.2017.02.004
[Indexed for MEDLINE]

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