Zhang et al. show that the non-peptide GLP-1R agonist PF 06882961, but not CHU-128, was able to closely mimic the in vitro pharmacological fingerprint of GLP-1. These pharmacological activities could be rationalized from high-resolution structures that provide a novel template for the design of new agonists targeting the GLP-1R.
- cryoelectron microscopy
- G-protein-coupled receptor
- glucagon-like peptide-1 receptor
- non-peptide agonists
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