Disconnect between signalling potency and in vivo efficacy of pharmacokinetically optimised biased glucagon-like peptide-1 receptor agonists
M. Lucey, P. Pickford, J. Minnion, J. Ungewiss, K. Schoeneberg, G. A. Rutter, S. R. Bloom, A. Tomas, B. Jones
This study evaluates how C-terminal acylation affects GLP-1R signal bias and in vivo efficacy, finding that acylated ligands show improved therapeutic potential despite reduced potency.
bioRxiv · Nov 26, 2019Pharmacology & Toxicology