Matches in SemOpenAlex for { <https://semopenalex.org/work/W2800843957> ?p ?o ?g. }
- W2800843957 abstract "Abstract Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cells, causes weight loss, and is an important pharmacological target in type 2 diabetes (T2D). Like other G protein-coupled receptors, the GLP-1R undergoes agonist-mediated endocytosis, but the functional and therapeutic consequences of modulating GLP-1R endocytic trafficking have not been clearly defined. Here, we investigate a series of biased GLP-1R agonists with variable propensities for GLP-1R internalization and recycling. Compared to a panel of FDA-approved GLP-1 mimetics, compounds that retain GLP-1R at the plasma membrane produce greater long-term insulin release, which is dependent on a reduction in β-arrestin recruitment and faster agonist dissociation rates. Such molecules elicit glycemic benefits in mice without concomitant increases in signs of nausea, a common side effect of GLP-1 therapies. Our study identifies a set of agents with specific GLP-1R trafficking profiles and the potential for greater efficacy and tolerability as T2D treatments." @default.
- W2800843957 created "2018-05-17" @default.
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- W2800843957 date "2018-04-23" @default.
- W2800843957 modified "2023-10-14" @default.
- W2800843957 title "Targeting GLP-1 receptor trafficking to improve agonist efficacy" @default.
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- W2800843957 doi "https://doi.org/10.1038/s41467-018-03941-2" @default.
- W2800843957 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5913239" @default.
- W2800843957 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29686402" @default.
- W2800843957 hasPublicationYear "2018" @default.
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