Exendin-4-derived glucagon-like peptide-1 receptor (GLP-1R) agonist with in vivo therapeutic efficacy in animal models of type 2 diabetes.
Lixisenatide (AVE0010, ZP10A) is a C-terminal amidated synthetic glucagon-like peptide-1 receptor (GLP-1R) agonist peptide whose sequence corresponds to Pro38 deleted exendin-4 with a C-terminal extension by six Lys residues. Lixisenatide exhibits 4-times higher human GLP-1R affinity than GLP-1(7-36) amide and dispalys in vivo therapeutic efficacy in murine and rat models of type 2 diabetes, as well as rat models of dox-induced renal fibrosis, global cerebral I/R injury, abdominal aortic aneurysm (AAA) and Aβ25-35 toxicity.
Artificial cells, nanomedicine, and biotechnology, 47(1), 2325-2332 (2019-06-09)
Increased free fatty acids (FFA) are one of the risk factors for type 2 diabetes. FFA also contribute to endothelial dysfunction in both the prediabetes and diabetes conditions. Therefore, FFA are an important link between diabetes and endothelial dysfunction. In
American journal of physiology. Gastrointestinal and liver physiology, 315(5), G671-G684 (2018-08-03)
Endogenous glucagon-like peptide-1 (GLP-1) regulates glucose-induced insulin secretion through both direct β-cell-dependent and indirect gut-brain axis-dependent pathways. However, little is known about the mode of action of the GLP-1 receptor agonist lixisenatide. We studied the effects of lixisenatide (intraperitoneal injection)
Recent clinical studies indicate that glucagon-like peptide-1 (GLP-1) analogues prevent acute cardiovascular events in type 2 diabetes mellitus but their mechanisms remain unknown. In the present study, the impact of GLP-1 analogues and their potential underlying molecular mechanisms in insulin
Diabetes, metabolic syndrome and obesity : targets and therapy, 8, 387-398 (2015-09-01)
Glucagon-like peptide-1 induces glucose-dependent insulin secretion and, in rodents, increases proliferation and survival of pancreatic beta cells. To investigate the effects on human beta cells, we used immunodeficient mice transplanted with human islets. The goal was to determine whether lixisenatide
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