Peptide complex containing GLP-1 exhibited long-acting properties in the treatment of type 2 diabetes |
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| Authors: | Zheng Xuemin Li Ying Li Xin Tang Lida Xu Weiren Gong Min |
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| Affiliation: | aDepartment of Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, China;bSchool of Life Science, University of Birmingham, UK;cDivision of Pharmacology, Tianjin Medical University, China;dTianjin Key Lab of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, China |
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| 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 HbA1c 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. |
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| Keywords: | Abbreviations: AUC, area under the curve DPP-IV, dipeptidylpeptidase IV ELISA, enzyme-linked immunosorbent assay GLP-1, glucagon-like peptide 1 IPGTT, intraperitoneally glucose tolerance test |
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