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Here, the authors assess the molecular mechanisms of peptide agonists binding to GLP-1R and the responses elucidated by these ligands, including distinct kinetics of G protein activation.

Phase 2 clinical trials have demonstrated exceptional efficacy for weight reduction, with up to 24.2% weight loss at 48 weeks with the highest doseresults that exceed those typically observed with existing GLP-1 receptor agonists

GLP-1R agonist 2 (compound 2) is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R