title: Synthesis, characterization and pharmacodynamics of vitamin-B(12)-conjugated glucagon-like peptide-1.
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.
authors.affiliation: Department of Chemistry, Syracuse University, 111 College Place Syracuse, NY 13244, USA.
authors.forename: Susan
authors.initials: S
authors.lastname: Clardy-James
authors.forename: Oleg G
authors.initials: OG
authors.lastname: Chepurny
authors.forename: Colin A
authors.initials: CA
authors.lastname: Leech
authors.forename: George G
authors.initials: GG
authors.lastname: Holz
authors.forename: Robert P
authors.initials: RP
authors.lastname: Doyle
mesh_terms: D002118:Calcium / Q000378:metabolism; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy / Q000378:metabolism; D052216:Glucagon-Like Peptide 1 / Q000737:chemistry*; D000067757:Glucagon-Like Peptide-1 Receptor; D057809:HEK293 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000187:drug effects / Q000378:metabolism; D018027:Receptors, Glucagon / Q000235:genetics / Q000378:metabolism; D014805:Vitamin B 12 / Q000737:chemistry*
chemical_list: C000593833:GLP1R protein, human; D000067757:Glucagon-Like Peptide-1 Receptor; D007004:Hypoglycemic Agents; D007328:Insulin; D018027:Receptors, Glucagon; D052216:Glucagon-Like Peptide 1; D014805:Vitamin B 12; D002118:Calcium