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G-Protein-Coupled Receptors: from Structural Insights to Functional Mechanisms

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Cassandra Koole, Kavita Pabreja, Emilia E. Savage, Denise Wootten, Sebastian G.B. Furness, Laurence J. Miller, Arthur Christopoulos, Patrick M. Sexton
Biochemical Society Transactions Jan 29, 2013, 41 (1) 172-179; DOI: 10.1042/BST20120236
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
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
Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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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
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
Department of Molecular Pharmacology and Experimental Therapeutics, 13400 E. Shea Blvd., Scottsdale, AZ 85259, U.S.A.
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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
Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, 381 Royal Parade, Parkville 3052, Victoria, Australia
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  • For correspondence: patrick.sexton@monash.edu
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Abstract

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.

  • allosteric modulation
  • biased signalling
  • G-protein-coupled receptor
  • glucagon-like peptide-1 receptor
  • glucagon-like peptide-1
  • probe-dependence

Footnotes

  • G-Protein-Coupled Receptors: from Structural Insights to Functional Mechanisms: A Biochemical Society Focused Meeting co-organized with Monash University held at Monash University Prato Centre, Prato, Italy, 12–14 September 2012. Organized and Edited by Bice Chini (CNR Institute of Neuroscience, Italy), Marco Parenti (University of Milano–Bicocca, Italy), David Poyner (Aston University, U.K.) and Mark Wheatley (University of Birmingham, U.K.)

Abbreviations: BETP, 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine; DM, diabetes mellitus; DPPIV, dipeptidyl peptidase IV; EGFR, epidermal growth factor receptor; ERK1/2, extracellular-signal-regulated kinase 1 and 2; GLP-1R, glucagon-like peptide-1 receptor; GPCR, G-protein-coupled receptor; GRK, G-protein-coupled receptor kinase; PAM, positive allosteric modulator; PI3K, phosphoinositide 3-kinase; PK, protein kinase

  • © The Authors Journal compilation © 2013 Biochemical Society
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February 2013

Volume: 41 Issue: 1

Biochemical Society Transactions: 41 (1)
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Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function
Cassandra Koole, Kavita Pabreja, Emilia E. Savage, Denise Wootten, Sebastian G.B. Furness, Laurence J. Miller, Arthur Christopoulos, Patrick M. Sexton
Biochemical Society Transactions Feb 2013, 41 (1) 172-179; DOI: 10.1042/BST20120236
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Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function
Cassandra Koole, Kavita Pabreja, Emilia E. Savage, Denise Wootten, Sebastian G.B. Furness, Laurence J. Miller, Arthur Christopoulos, Patrick M. Sexton
Biochemical Society Transactions Feb 2013, 41 (1) 172-179; DOI: 10.1042/BST20120236

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  • Article
    • Abstract
    • Introduction
    • Physiology of the incretin system
    • GLP-1 receptor
    • GLP-1R signalling and regulation
    • GLP-1 mimetics in the treatment of Type II DM
    • Biased signalling
    • Allosteric modulation
    • Conclusions
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Keywords

allosteric modulation
biased signalling
G-protein-coupled receptor
glucagon-like peptide-1 receptor
glucagon-like peptide-1
probe-dependence

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