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Article

Characterizing the role of extracellular domain in GLP-1R biased agonism.

The international journal of biochemistry & cell biology - 1 Dec 2025

Xie Linshan, Xu Rong, Liu Huining, Na Man, Qin Qikai, Xu Fei, Stevens Raymond C, Liu Yan

Abstract excerpt

The biased agonism of glucagon-like peptide-1 receptor (GLP-1R) plays a key role in the efficacy and side effects of drugs used to treat type II diabetes mellitus and obesity. Despite its therapeutic potential, the mechanisms underlying GLP-1R biased agonism remain poorly understood. In this study, we investigate the role of the extracellular domain (ECD) in GLP-1R signaling bias through saturation mutagenesis at...

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PMID: 40998235
DOI: 10.1016/j.biocel.2025.106867

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ECD

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