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Disconnect between signalling potency and in vivo efficacy of pharmacokinetically optimised biased glucagon-like peptide-1 receptor agonists

OBJECTIVE: The objective of this study was to determine how pharmacokinetically advantageous acylation impacts on glucagon-like peptide-1 receptor (GLP-1R) signal bias, trafficking, anti-hyperglycaemic efficacy, and appetite suppression. METHODS: In vitro signalling responses were measured using bio...

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Publicado en:Mol Metab
Autores principales: Lucey, Maria, Pickford, Philip, Bitsi, Stavroula, Minnion, James, Ungewiss, Jan, Schoeneberg, Katja, Rutter, Guy A., Bloom, Stephen R., Tomas, Alejandra, Jones, Ben
Formato: Artigo
Lenguaje:Inglês
Publicado: Elsevier 2020
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Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC7262448/
https://ncbi.nlm.nih.gov/pubmed/32278079
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.molmet.2020.100991
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