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

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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Bibliographic Details
Main Authors: Maria Lucey, Philip Pickford, Stavroula Bitsi, James Minnion, Jan Ungewiss, Katja Schoeneberg, Guy A. Rutter, Stephen R. Bloom, Alejandra Tomas, Ben Jones
Format: Article
Language:English
Published: Elsevier 2020-07-01
Series:Molecular Metabolism
Subjects:
Type 2 diabetes
Biased signalling
Glucagon-like peptide-1 receptor
Exendin-4
Trafficking
Online Access:http://www.sciencedirect.com/science/article/pii/S221287782030065X

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http://www.sciencedirect.com/science/article/pii/S221287782030065X

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