Evaluation of efficacy- versus affinity-driven agonism with biased GLP-1R ligands P5 and exendin-F1
A. Marzook, S. Chen, P. Pickford, M. Lucey, Y. Wang, I. R. Correa, J. Broichhagen, D. Hodson, V. Salem, G. A. Rutter, T. M. Tan, S. R. Bloom, A. Tomas, B. Jones
This study compares the efficacy and affinity of two GLP-1R agonists, P5 and exendin-F1, showing that exendin-F1's lower acute efficacy correlates with sustained insulin secretion and anti-hyperglycaemic effects.
bioRxiv · Apr 1, 2021Pharmacology & Toxicology