Target Validation Information
TTD ID T09694
Target Name Glucagon-like peptide 1 (GLP-1:7-37)
Type of Target
Literature-reported
Drug Potency against Target Albiglutide Drug Info EC50 = 1.5 nM [1]
Action against Disease Model Lixisenatide Drug Info Lixisenatide protected Ins-1 cells (a rat-derived beta-cell line) from both lipid- and cytokine-induced apoptosis. More importantly, Lixisenatide also prevented lipotoxicity-induced insulin depletion in h uMan islets and preserved insulin production, storage and pancreatic beta-cell function in vitro. In animal models of diabetes, Lixisenatide improved basal blood glucose and HbA(1c) with a rapid onset and sustained duration of action, and prevented the deterioration of pancreatic responsiveness and glucose homeostasis. Lixisenatide also delayed gastric emptying and reduced food intake. [2]
References
REF 1 Medicinal Chemistry of Incretin Mimetics and DPP-4 Inhibitors. ChemMedChem. 2010 Feb 1;5(2):179-85.
REF 2 Protein kinase C inhibitor sotrastaurin selectively inhibits the growth of CD79 mutant diffuse large B-cell lymphomas. Cancer Res. 2011 Apr 1;71(7):2643-53.

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