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LIU Yan, LI Chengye, CAI Xingguang, SUN Lidan, HUANG Wenlong. Synthesis and preliminary anti-diabetic activity evaluation of novel PEGylated GLP-1 receptor agonists[J]. Journal of China Pharmaceutical University, 2018, 49(5): 558-567. DOI: 10.11665/j.issn.1000-5048.20180507
Citation: LIU Yan, LI Chengye, CAI Xingguang, SUN Lidan, HUANG Wenlong. Synthesis and preliminary anti-diabetic activity evaluation of novel PEGylated GLP-1 receptor agonists[J]. Journal of China Pharmaceutical University, 2018, 49(5): 558-567. DOI: 10.11665/j.issn.1000-5048.20180507
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Synthesis and preliminary anti-diabetic activity evaluation of novel PEGylated GLP-1 receptor agonists

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  • In order to obtain glucagon-like peptide-1(GLP-1)analogs which can sustainedly control the levels of glucose, 12 derivatives were designed and synthesized by coupling monomethoxy polyethylene glycol(mPEG, with average molecular weights of 350, 550 and 750)to GLP-1 analogs. Preliminary pharmacological activities showed that all compounds retained GLP-1 receptor agonist activities, and the hypoglycemic activity of compound I - 12 was similar to those of Ex-4 and Liraglutide, suggesting I - 12 could be a potential long-acting GLP-1 receptor agonist.
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    • References (17)
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