SHORT COMMENT FOR NATURE REVIEWS ENDOCRINOLOGY Targeting simultaneously GLP-1, GIP and glucagon receptors : a new paradigm for treating obesity and diabetes
نویسنده
چکیده
An innovative unimolecular, polypharmaceutical strategy using a well-balanced monomeric peptide triagonist targeting three metabolically-related hormone receptors (glucagon-like peptide-1, glucose-dependent insulinotropic poplypeptide and glucagon) appears the most effective pharmacological approach to reversing obesity and metabolic comorbidities in rodents and could open new perspective to tackle the dual obesity-diabetes burden in humans.
منابع مشابه
Molecular Pharmacology of the Incretin Receptors
The incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) are important regulators of insulin and glucagon secretion as well as lipid metabolism and appetite. These biological functions make their respective receptors (GIPR and GLP-1R) attractive targets in the treatment of both type 2 diabetes mellitus (T2DM) and obesity. The use of these nati...
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The incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are physiological gut peptides with insulin-releasing and extrapancreatic glucoregulatory actions. Incretin analogues/mimetics activate GLP-1 or GIP receptors whilst avoiding physiological inactivation by dipeptidyl peptidase 4 (DPP-4), and they represent one of the newest classes of ant...
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OBJECTIVE Glucose-dependent insulinotropic polypeptide (GIP), unlike glucagon-like peptide (GLP)-1, lacks glucose-lowering properties in patients with type 2 diabetes. We designed this study to elucidate the underlying pathophysiology. RESEARCH DESIGN AND METHODS Twenty-two insulin-naïve subjects with type 2 diabetes were given either synthetic human GIP (20 ng x kg(-1) x min(-1)) or placebo ...
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therapy and represent a new class of drug candidates for the treatment of metabolic diseases. selective GLP-1 therapies. These dual incretin co-agonists signify a new direction for unimolecular combination its inherent mixed agonism, lowered the drug dose and ameliorated the dose-limiting nausea that has plagued incretin was engineered with selective chemical modifications to enhance pharmacoki...
متن کاملThe separate and combined impact of the intestinal hormones, GIP, GLP-1, and GLP-2, on glucagon secretion in type 2 diabetes.
Type 2 diabetes mellitus (T2DM) is associated with reduced suppression of glucagon during oral glucose tolerance test (OGTT), whereas isoglycemic intravenous glucose infusion (IIGI) results in normal glucagon suppression in these patients. We examined the role of the intestinal hormones glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1), and glucagon-like peptid...
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