| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2529732 | Current Opinion in Pharmacology | 2016 | 6 Pages |
•Reviews role of key peptide activators of GPCRs on insulin secretion in pancreatic β-cells.•Overview of mechanisms of action of peptide activated GPCRs in context of diabetes.•Potential of lipid activated GPCRs for improving glycaemic control in diabetes.•Discusses emerging drug developments including dual and multifunctional GPCRs agonists.
Incretin based glucagon-like peptide-1 receptor (GLP-1R) agonists which target a G-protein coupled receptor (GPCR) are currently used in the treatment of type 2 diabetes. This review focuses on GPCRs from pancreatic β-cells, including GLP-1, glucose-dependent insulinotropic polypeptide (GIP), glucagon, somatostatin, pancreatic polypeptide (PP), cholecystokinin (CCK), peptide YY (PYY), oxyntomodulin (OXM) and ghrelin receptors. In addition, fatty acids GPCRs are thought to have an increasing role in regulating peptide secretions namely short fatty acids GPCR (GPR41, GPR43), medium chain fatty acid GPCR (GPR84), long chain fatty acid GPCR (GPR40, GPR120) and cannabinoid-like GPCR (GPR55, GPR119). Several pre-clinical and clinical trials are currently ongoing in peptide GPCR based therapies, including dual and triple agonist peptides which activate two or more GPCRs simultaneously.
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