Small-molecule GLP-1 secretagogs: challenges and recent advances
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Published on: February 26, 2019
1Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
Abstract:
Glucagon-like peptide-1 (GLP-1) is a potent antihyperglycemic hormone that is an alternative treatment choice for patients with type 2 diabetes mellitus (T2DM). The glucose-dependent mechanism of GLP-1 is particularly important because it does not stimulate insulin secretion and cause hypoglycemia when plasma glucose concentrations are in the normal fasting range. Although several peptide drugs of GLP-1 analogs are clinically available, research on the small molecules that stimulate GLP-1 secretion is still struggling. In this review, we summarize recent updates in the discovery of small-molecule GLP-1 secretagogs targeting the G-protein-coupled receptor (GPCR) family. we also discuss the challenges and strategies for the study and describe the latest developments.
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