Discovery of Insulin/GLP-1/Glucagon Triagonists for the Treatment of Diabetes and Obesity.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00218
Abstract: The combination of insulin and incretin-based therapies has emerged as a potential promising tactic for the treatment of diabetes. Here we report the first example of a unimolecular triagonist to simultaneously target insulin, GLP-1, and… read more here.
Keywords: glp; glp glucagon; chemistry; insulin glp ... See more keywords
Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors
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DOI: 10.1038/s41467-022-28683-0
Abstract: Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several multi-targeting agonists at GIPR, GLP-1R or GCGR, developed to maximize metabolic benefits with reduced side-effects,… read more here.
Keywords: glp; glp glucagon; glucagon; gipr glp ... See more keywords
A GLP‐1/glucagon (GCG)/CCK2 receptors tri‐agonist provides new therapy for obesity and diabetes
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DOI: 10.1111/bph.15860
Abstract: Glucagon‐like peptide‐1 (GLP‐1) and glucagon (GCG) receptor dual agonist have promising therapeutic effects in the treatment of obesity and diabetes. Moreover, GLP‐1 and cholecystokinin 2 (CCK2) dual agonists have been shown to restore pancreas function… read more here.
Keywords: glp glucagon; glucagon; obesity diabetes; glucagon gcg ... See more keywords
Preclinical evaluation of a protracted GLP-1/glucagon receptor co-agonist: Translational difficulties and pitfalls
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DOI: 10.1371/journal.pone.0264974
Abstract: During recent years combining GLP-1 and glucagon receptor agonism with the purpose of achieving superior weight loss and metabolic control compared to GLP-1 alone has received much attention. The superior efficacy has been shown by… read more here.
Keywords: evaluation; glp glucagon; glucose tolerance; glucagon ... See more keywords
MEDI0382, a GLP-1/Glucagon Receptor Dual Agonist, Dramatically Reduces Hepatic Collagen in a Mouse Model of NASH
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DOI: 10.2337/db18-1841-p
Abstract: Nonalcoholic steatohepatitis (NASH), characterized by hepatic steatosis, inflammation and fibrosis is an unmet medical need. MEDI0382, a balanced GLP-1/glucagon dual receptor agonist, is under development for the treatment of T2DM. Here we examined the effects… read more here.
Keywords: glp glucagon; self astrazeneca; self; medi0382 ... See more keywords