Journal
BIOCHEMICAL SOCIETY TRANSACTIONS
Volume 41, Issue -, Pages 172-179Publisher
PORTLAND PRESS LTD
DOI: 10.1042/BST20120236
Keywords
allosteric modulation; biased signalling; G-protein-coupled receptor; glucagon-like peptide-1 receptor; glucagon-like peptide-1; probe-dependence
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Funding
- National Health and Medical Research Council of Australia (NHMRC) [519461, 1002180]
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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 beta-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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