Synthesis, characterization and pharmacodynamics of vitamin-B(12)-conjugated glucagon-like peptide-1

ChemMedChem. 2013 Apr;8(4):582-6. doi: 10.1002/cmdc.201200461. Epub 2012 Nov 30.

Abstract

Clearing the way: Glucagon-like peptide-1 (GLP-1) receptor agonists are proving a potent weapon in the treatment of type II diabetes. A new vitamin B(12)-GLP-1 conjugate is investigated and shown to have insulinotropic properties similar to the unmodified peptide. These results are critical to the exploitation of the vitamin B(12) oral uptake pathway for peptide delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / metabolism
  • Diabetes Mellitus, Type 2 / drug therapy
  • Diabetes Mellitus, Type 2 / metabolism
  • Glucagon-Like Peptide 1 / chemistry*
  • Glucagon-Like Peptide-1 Receptor
  • HEK293 Cells
  • Humans
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use
  • Insulin / metabolism
  • Insulin Secretion
  • Islets of Langerhans / drug effects
  • Islets of Langerhans / metabolism
  • Receptors, Glucagon / genetics
  • Receptors, Glucagon / metabolism
  • Vitamin B 12 / chemistry*

Substances

  • GLP1R protein, human
  • Glucagon-Like Peptide-1 Receptor
  • Hypoglycemic Agents
  • Insulin
  • Receptors, Glucagon
  • Glucagon-Like Peptide 1
  • Vitamin B 12
  • Calcium