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Development of novel ligands for peptide GPCRs

Moran, BM, McKillop, Aine and O'Harte, Finbarr (2016) Development of novel ligands for peptide GPCRs. Current Opinion in Pharmacology, 31 . pp. 57-62. [Journal article]

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DOI: 10.1016/j.coph.2016.08.009


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 b-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 preclinical and clinical trials are currently ongoing in peptide GPCR based therapies, including dual and triple agonist peptides which activate two or more GPCRs simultaneously.

Item Type:Journal article
Keywords:GPCR, beta-cells,
Faculties and Schools:Faculty of Life and Health Sciences > School of Biomedical Sciences
Faculty of Life and Health Sciences
Research Institutes and Groups:Biomedical Sciences Research Institute
Biomedical Sciences Research Institute > Diabetes
ID Code:35836
Deposited By: Dr Nigel Irwin
Deposited On:20 Sep 2016 08:43
Last Modified:26 Jul 2017 13:29

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