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

• Main Authors: Maria Lucey (Author), Philip Pickford (Author), Stavroula Bitsi (Author), James Minnion (Author), Jan Ungewiss (Author), Katja Schoeneberg (Author), Guy A. Rutter (Author), Stephen R. Bloom (Author), Alejandra Tomas (Author), Ben Jones (Author)
• Format: Book
• Published: Elsevier, 2020-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...