Type 2 diabetes is a major global health problem and there is ongoing research for new treatments to manage the disease. The GLP-1R (glucagon-like peptide-1 receptor) controls the physiological response to the incretin peptide, GLP-1, and is currently a major target for the development of therapeutics owing to the broad range of potential beneficial effects in Type 2 diabetes. These include promotion of glucose-dependent insulin secretion, increased insulin biosynthesis, preservation of β-cell mass, improved peripheral insulin sensitivity and promotion of weight loss. Despite this, our understanding of GLP-1R function is still limited, with the desired spectrum of GLP-1R-mediated signalling yet to be determined. We review the current understanding of GLP-1R function, in particular, highlighting recent contributions in the field on allosteric modulation, probe-dependence and ligand-directed signal bias and how these behaviours may influence future drug development.
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February 2013
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Conference Article|
January 29 2013
Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function Available to Purchase
Cassandra Koole;
Cassandra Koole
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Kavita Pabreja;
Kavita Pabreja
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Emilia E. Savage;
Emilia E. Savage
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Denise Wootten;
Denise Wootten
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Sebastian G.B. Furness;
Sebastian G.B. Furness
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Laurence J. Miller;
Laurence J. Miller
†Department of Molecular Pharmacology and Experimental Therapeutics, 13400 E. Shea Blvd., Scottsdale, AZ 85259, U.S.A.
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Arthur Christopoulos;
Arthur Christopoulos
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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Patrick M. Sexton
Patrick M. Sexton
1
*Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
1To whom correspondence should be addressed (email[email protected]).
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Publisher: Portland Press Ltd
Received:
September 24 2012
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2013 Biochemical Society
2013
Biochem Soc Trans (2013) 41 (1): 172–179.
Article history
Received:
September 24 2012
Citation
Cassandra Koole, Kavita Pabreja, Emilia E. Savage, Denise Wootten, Sebastian G.B. Furness, Laurence J. Miller, Arthur Christopoulos, Patrick M. Sexton; Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function. Biochem Soc Trans 1 February 2013; 41 (1): 172–179. doi: https://doi.org/10.1042/BST20120236
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