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Bioorg Med Chem. 2019 Apr 15;27(8):1670-1676. doi: 10.1016/j.bmc.2019.03.014. Epub 2019 Mar 7.

Novel nonapeptide GLP (28-36) amide derivatives with improved hypoglycemic and body weight lowering effects.

Author information

1
Integrated Medicine Research Center for Neurological Rehabilitation, College of Medicine, Jiaxing University, Jiaxing 314001, PR China.
2
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
3
School of Chemistry and Materials Science, Jiangsu Normal University, Xuzhou 221116, PR China.
4
Integrated Medicine Research Center for Neurological Rehabilitation, College of Medicine, Jiaxing University, Jiaxing 314001, PR China. Electronic address: slidan89@mail.zjxu.edu.cn.

Abstract

Glucagon-like peptide-1 (GLP-1) has emerged as a major therapeutic target for the treatment of type 2 diabetes. The nonapeptide GLP-1 (28-36) amide is one of the biological C-terminal products of GLP-1 modified by the neutral endopeptidase (NEP) 24.11 with limited hypoglycemic activity. In this study, we focused on the modification of GLP-1 (28-36) amide for the first time and synthesized a series of GLP-1 (28-36) amide analogues. Results of biological activity evaluation in INS-1 cell, STZ-induced diabetic and diet induced obesity (DIO) mice indicated that S3 as a promising candidate to treat type 2 diabetes and obesity.

KEYWORDS:

Diabetes; Glucagon-like peptide-1; Metabolite; Obesity

PMID:
30878191
DOI:
10.1016/j.bmc.2019.03.014

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