β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1

Abstract : Background: FFAR1/GPR40 is a potential target to enhance insulin secretion in type 2 diabetes, yet knowledge of the pharmacobiology of GPR40 remains incomplete. Results: GPR40 functions via both G protein-mediated and β-arrestin-mediated mechanisms; endogenous and synthetic ligands differentially engage these pathways to promote insulin secretion. Conclusion: GPR40 is subject to functionally relevant biased agonism. Significance: Biased agonism at GPR40 could be exploited for therapeutic purposes.
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https://hal.umontpellier.fr/hal-02068657
Contributeur : Mélanie Karli <>
Soumis le : vendredi 15 mars 2019 - 10:37:19
Dernière modification le : vendredi 20 septembre 2019 - 14:00:03

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Arturo Mancini, Gyslaine Bertrand, Kevin Vivot, Éric Carpentier, Caroline Tremblay, et al.. β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1. Journal of Biological Chemistry, American Society for Biochemistry and Molecular Biology, 2015, 290 (34), pp.21131-21140. ⟨10.1074/jbc.M115.644450⟩. ⟨hal-02068657⟩

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