title: Peptide complex containing GLP-1 exhibited long-acting properties in the treatment of type 2 diabetes.
abstract: The multiple physiological characterizations of glucagon-like peptide-1 (GLP-1) make it a promising drug candidate for the treatment of type 2 diabetes. However, in vivo, the half-life of GLP-1 is short, which is caused by the degradation of dipeptidyl peptidase-IV (DPP-IV) and renal clearance. Thus, the stabilization of GLP-1 is critical for its utility in drug development. Peptides known as GLP-1 protectors are predicted to increase the half-life of GLP-1 in vivo. Protecting peptides are able to form stable complexes by non-covalent interactions with human GLP-1. In this study, the stability of the complex was investigated, and the physiological functions of the GLP-1/peptide 1 complex were compared to those of exenatide and liraglutide in animals. The results indicated that the GLP-1/peptide 1 complex remarkably raised the half-life of GLP-1 in vivo and showed better glucose tolerance and higher HbA(1c) reduction than exenatide and liraglutide in rodents. Based upon these results, it is suggested that the GLP-1/peptide 1 complex might be utilized as a possible potent anti-diabetic drug in the treatment of type 2 diabetes mellitus.
authors.affiliation: Department of Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, China.
authors.forename: Xuemin
authors.initials: X
authors.lastname: Zheng
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.forename: Lida
authors.initials: L
authors.lastname: Tang
authors.forename: Weiren
authors.initials: W
authors.lastname: Xu
authors.forename: Min
authors.initials: M
authors.lastname: Gong
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D000077270:Exenatide; D052216:Glucagon-Like Peptide 1 / Q000031:analogs & derivatives / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000627:therapeutic use*; D000069450:Liraglutide; D008297:Male; D010455:Peptides / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D021241:Spectrometry, Mass, Electrospray Ionization; D014688:Venoms / Q000627:therapeutic use
chemical_list: D007004:Hypoglycemic Agents; D010455:Peptides; D014688:Venoms; D000069450:Liraglutide; D052216:Glucagon-Like Peptide 1; D000077270:Exenatide