Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Cassandra Koole, Kavita Pabreja, Emilia E. Savage, Denise Wootten, Sebastian G.B. Furness, Laurence J. Miller, Arthur Christopoulos, Patrick M. Sexton

Research output: Contribution to journalArticlepeer-review

49 Scopus citations

Abstract

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 β-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.

Original languageEnglish (US)
Pages (from-to)172-179
Number of pages8
JournalBiochemical Society Transactions
Volume41
Issue number1
DOIs
StatePublished - Feb 1 2013

Keywords

  • Allosteric modulation
  • Biased signalling
  • G-protein-coupled receptor
  • Glucagon-like peptide-1
  • Glucagon-like peptide-1 receptor
  • Probe-dependence

ASJC Scopus subject areas

  • Biochemistry

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