Ontology highlight
ABSTRACT:
SUBMITTER: Borner T
PROVIDER: S-EPMC7376604 | biostudies-literature | 2020 Jun
REPOSITORIES: biostudies-literature
Cell reports 20200601 11
Glucagon-like peptide-1 receptor (GLP-1R) agonists used to treat type 2 diabetes mellitus often produce nausea, vomiting, and in some patients, undesired anorexia. Notably, these behavioral effects are caused by direct central GLP-1R activation. Herein, we describe the creation of a GLP-1R agonist conjugate with modified brain penetrance that enhances GLP-1R-mediated glycemic control without inducing vomiting. Covalent attachment of the GLP-1R agonist exendin-4 (Ex4) to dicyanocobinamide (Cbi), ...[more]