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Article

An extracellular allosteric gate modulates the ligand efficacy of GPR119.

Structure (London, England : 1993) - 6 Aug 2026

Zhang Yi, Wang Jiening, Han Zhen, Qian Yuxia, Ye Sheng, Wu Shan, Qiao Anna

Abstract excerpt

GPR119 is a promising therapeutic target for metabolic diseases, yet the structural basis for its ligand-dependent efficacy remains unclear. Here, we report the cryo-EM structure of GPR119 bound to the partial agonist AS1269574 and Gs protein, revealing a non-canonical ligand-binding mode. Unlike full agonists, AS1269574 occupies a restricted pocket within the activation cavity and stabilizes a closed...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to GTP-Binding Protein alpha Subunits, Gs

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Identifiers

PMID: 42269610
DOI: 10.1016/j.str.2026.05.007

Genes

GPR119

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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