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Regulation of energy metabolism through central GIPR signaling.
Peptides 176:171198 (2024)
In recent years, significant progress has been made to pharmacologically combat the obesity pandemic, particularly with regard to biochemically tailored drugs that simultaneously target the receptors for glucagon-like peptide-1 (GLP-1) and the glucose-dependent insulinotropic polypeptide (GIP). But while the pharmacological benefits of GLP-1 receptor (GLP-1R) agonism are widely acknowledged, the role of the GIP system in regulating systems metabolism remains controversial. When given in adjunct to GLP-1R agonism, both agonism and antagonism of the GIP receptor (GIPR) improves metabolic outcome in preclinical and clinical studies, and despite persistent concerns about its potential obesogenic nature, there is accumulating evidence indicating that GIP has beneficial metabolic effects via central GIPR agonism. Nonetheless, despite growing recognition of the GIP system as a valuable pharmacological target, there remains great uncertainty as to where and how GIP acts in the brain to regulate metabolism, and how GIPR agonism may differ from GIPR antagonism in control of energy metabolism. In this review we highlight current knowledge on the central action of GIP, and discuss open questions related to its multifaceted biology in the brain and the periphery.
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Publication type
Article: Journal article
Document type
Review
Keywords
Gip ; Gipr ; Gipr:glp-1r Co-agonism ; Glp-1 ; Glp-1r ; Obesity; Dependent Insulinotropic Polypeptide; Gastric-inhibitory Polypeptide; Glucagon-like Peptide-1; Glp-1 Receptor Agonist; Adipose-tissue; Body-weight; Lipoprotein-lipase; Glucose-homeostasis; Induced Nausea; Dual Gip
ISSN (print) / ISBN
0196-9781
e-ISSN
1873-5169
Journal
Peptides
Quellenangaben
Volume: 176,
Article Number: 171198
Publisher
Elsevier
Publishing Place
New York, NY
Non-patent literature
Publications
Reviewing status
Peer reviewed
Institute(s)
Institute of Diabetes and Obesity (IDO)
Grants
German Center for Diabetes Research
German Research Foundation (DFG)
European Union within the scope or the European Research Council ERC-CoG
German Research Foundation (DFG)
European Union within the scope or the European Research Council ERC-CoG