GLP-1 receptor localization in monkey and human tissue: novel distribution revealed with extensively validated monoclonal antibody

Research output: Contribution to journalJournal articleResearchpeer-review

  • Charles Pyke
  • R Scott Heller
  • Rikke K Kirk
  • Ørskov, Cathrine
  • Steffen Reedtz-Runge
  • Peter Kaastrup
  • Anders Hvelplund
  • Linda Bardram
  • Dan Calatayud
  • Lotte Bjerre Knudsen

Glucagon-like peptide 1 (GLP-1) analogs are increasingly being used in the treatment of type 2 diabetes. It is clear that these drugs lower blood glucose through an increase in insulin secretion and a lowering of glucagon secretion; in addition, they lower body weight and systolic blood pressure and increase heart rate. Using a new monoclonal antibody for immunohistochemistry, we detected GLP-1 receptor (GLP-1R) in important target organs in humans and monkeys. In the pancreas, GLP-1R was predominantly localized in β-cells with a markedly weaker expression in acinar cells. Pancreatic ductal epithelial cells did not express GLP-1R. In the kidney and lung, GLP-1R was exclusively expressed in smooth muscle cells in the walls of arteries and arterioles. In the heart, GLP-1R was localized in myocytes of the sinoatrial node. In the gastrointestinal tract, the highest GLP-1R expression was seen in the Brunner's gland in the duodenum, with lower level expression in parietal cells and smooth muscle cells in the muscularis externa in the stomach and in myenteric plexus neurons throughout the gut. No GLP-1R was seen in primate liver and thyroid. GLP-1R expression seen with immunohistochemistry was confirmed by functional expression using in situ ligand binding with (125)I-GLP-1. In conclusion, these results give important new insight into the molecular mode of action of GLP-1 analogs by identifying the exact cellular localization of GLP-1R.

Original languageEnglish
JournalEndocrinology
Volume155
Issue number4
Pages (from-to)1280-90
Number of pages11
ISSN0013-7227
DOIs
Publication statusPublished - Apr 2014
Externally publishedYes

    Research areas

  • Animals, Antibodies, Monoclonal/chemistry, Blood Pressure, Body Weight, Cell Line, Cricetinae, Duodenum/metabolism, Glucagon/secretion, Glucagon-Like Peptide 1/analogs & derivatives, Glucagon-Like Peptide-1 Receptor, Haplorhini, Heart Rate, Humans, Insulin/secretion, Ligands, Liraglutide, Mice, Mice, Inbred C57BL, Mice, Knockout, Peptides/chemistry, Protein Binding, Receptors, Glucagon/metabolism, Tissue Distribution, Transfection, Venoms/chemistry

ID: 194814912