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.
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
To demonstrate the protective effect of glucagon-like peptide 1 (GLP-1) signaling on the cardiovascular system, we conducted this study to show that the GLP-1 receptor analog (lixisenatide) could inhibit abdominal aortic aneurysm (AAA) development in rats. Lixisenatide was injected subcutaneously
The Journal of pharmacology and experimental therapeutics, 307(2), 490-496 (2003-09-17)
We characterized the novel, rationally designed peptide glucagon-like peptide 1 (GLP-1) receptor agonist H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSK KKKKK-NH2 (ZP10A). Receptor binding studies demonstrated that the affinity of ZP10A for the human GLP-1 receptor was 4-fold greater than the affinity of GLP-1 (7-36) amide.
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)
Biochemical and biophysical research communications, 508(4), 1120-1125 (2018-12-17)
Mitochondrial dysregulation has been associated with vascular endothelial dysfunction and pathophysiological development of cardiovascular diseases. Lixisenatide is a drug approved by the US Food and Drug Administration for the treatment of type 2 diabetes (T2D). Little information regarding the effects
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