Development of novel ligands for peptide GPCRs

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)
97 Downloads (Pure)


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.
Original languageEnglish
Pages (from-to)57-62
JournalCurrent Opinion in Pharmacology
Early online date5 Sept 2016
Publication statusPublished (in print/issue) - 1 Dec 2016


  • GPCR
  • beta-cells


Dive into the research topics of 'Development of novel ligands for peptide GPCRs'. Together they form a unique fingerprint.

Cite this