The glucagon-like peptide-1 receptor (GLP-1R) is a class B GPCR that is a major therapeutic target for the treatment of type 2 diabetes. The receptor is activated by the incretin peptide GLP-1 promoting a broad range of physiological effects including glucose-dependent insulin secretion and biosynthesis, improved insulin sensitivity of peripheral tissues, preservation of β-cell mass and weight loss, all of which are beneficial in the treatment of type 2 diabetes. Despite this, existing knowledge surrounding the underlying signalling mechanisms responsible for the physiological actions downstream of GLP-1R activation is limited. Here, we review the current understanding around GLP-1R-mediated signalling, in particular highlighting recent contributions to the field on biased agonism, the spatial and temporal aspects for the control of signalling and how these concepts may influence future drug development.
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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
The complexity of signalling mediated by the glucagon-like peptide-1 receptor
Madeleine M. Fletcher;
Madeleine M. Fletcher
*Monash Institute of Pharmaceutical Sciences, Monash University, Royal Parade, Parkville, Melbourne, 3052, Australia
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Michelle L. Halls;
Michelle L. Halls
*Monash Institute of Pharmaceutical Sciences, Monash University, Royal Parade, Parkville, Melbourne, 3052, Australia
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Arthur Christopoulos;
Arthur Christopoulos
*Monash Institute of Pharmaceutical Sciences, Monash University, Royal Parade, Parkville, Melbourne, 3052, Australia
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Patrick M. Sexton;
Patrick M. Sexton
*Monash Institute of Pharmaceutical Sciences, Monash University, Royal Parade, Parkville, Melbourne, 3052, Australia
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Denise Wootten
Denise Wootten
1
*Monash Institute of Pharmaceutical Sciences, Monash University, Royal Parade, Parkville, Melbourne, 3052, Australia
1To whom correspondence should be addressed (email denise.wootten@monash.edu).
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Publisher: Portland Press Ltd
Received:
January 07 2016
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2016 Authors; published by Portland Press Limited
2016
Biochem Soc Trans (2016) 44 (2): 582–588.
Article history
Received:
January 07 2016
Citation
Madeleine M. Fletcher, Michelle L. Halls, Arthur Christopoulos, Patrick M. Sexton, Denise Wootten; The complexity of signalling mediated by the glucagon-like peptide-1 receptor. Biochem Soc Trans 15 April 2016; 44 (2): 582–588. doi: https://doi.org/10.1042/BST20150244
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