Journal
BIOCHEMICAL SOCIETY TRANSACTIONS
Volume 44, Issue -, Pages 582-588Publisher
PORTLAND PRESS LTD
DOI: 10.1042/BST20150244
Keywords
biased signalling; G protein-coupled receptor; glucagon-like peptide-1 receptor; ligand-directed signalling bias
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Funding
- National Health and Medical Research Council of Australia [1065410, 1055134]
- National Health and Medical Research Council of Australia [1065410] Funding Source: NHMRC
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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 beta-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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