Application of novel peptide (Pp1) improving the half-life of exendin-4 in vivo |
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Authors: | Zheng Xuemin Li Ying Fu Gang Gong Min |
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Institution: | a Department of Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China b Tianjin Key Lab of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China c School of Life Science, University of Birmingham, B15 2TT, UK |
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Abstract: | AimsThe multiple physiological characterizations of exendin-4 make it as a promising drug candidate for the therapy of type 2 diabetes. Although the longer biological half-life offered the exendin-4 with excellent therapeutic potentials for the clinical utility of type 2 diabetes than glucagon-like peptide-1, the exendin-4 still did not free from the inconveniently frequent injections. Therefore, there are increasing requirements for the long-acting exendin-4.MethodsPp1 regard as a novel exendin-4 protecting peptide, which are predicted to have the ability of increasing the stabilization of exendin-4 in vivo. Protecting peptide is able to form stable complex by non-covalent interaction with human exendin-4.ResultsIn this study, the stability of the exendin-4/Pp1 complex was investigated, and the physiological functions of it were analyzed. Results indicated that exendin-4/Pp1 complex remarkably raised the stabilization of exendin-4 in vivo; it also showed better glucose tolerance and higher HbA1c reduction than exendin-4 which was utilized chronically in rodents.ConclusionBased upon these results, it is suggested that an exendin-4/Pp1 complex might be utilized as a potent anti-diabetic drug in the treatment of type 2 diabetes mellitus. |
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Keywords: | Exendin-4 Long-lasting anti-diabetes HbA1c Biological half-life |
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