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Article

Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations.

Molecular metabolism - 1 Mar 2026

Tran Hanh Duyen, Zuo Yiming, Wong Carissa, Pollard Alice, Bloom Steve, Jones Ben

Abstract excerpt

BACKGROUND AND AIM: The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target for type 2 diabetes and obesity. Agonists showing bias in favour of G protein signalling over β-arrestin recruitment and GLP-1R internalisation, e.g. tirzepatide and orforglipron, have favourable clinical efficacy profiles. However, understanding of the effects of biased agonism has been hampered by differences in...

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Identifiers

PMID: 41570980
DOI: 10.1016/j.molmet.2026.102321
PMCID: PMC12925471

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