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.
European review for medical and pharmacological sciences, 23(9), 4017-4026 (2019-05-23)
The aim of this study was to investigate whether Lixisenatide, NF-kB/TNF-α, and TGF-β/Smad pathways exert clear regulatory roles in doxorubicin-induced renal fibrosis in rats, and to explore the possible underlying mechanism. 30 rats were randomly assigned into the sham group
Preclinical pharmacology of the new GLP-1 receptor agonist AVE0010.
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
The metabolic benefits of lixisenatide as an anti-diabetic agent are recognized but potential extra-pancreatic effects of this glucagon-like peptide-1 (GLP-1) mimetic in the brain are less well known. This study examines actions within the hippocampus following chronic 40-day peripheral administration
Alzheimer's disease (AD) is a progressive and degenerative disorder accompanied by cognitive impairment, but effective strategies against AD are currently not available. Interestingly, glucagon-like peptide-1 (GLP-1) used in type 2 diabetes mellitus (T2DM) has shown neuroprotective effects in preclinical studies
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