Article
Allosteric modulation of ghrelin receptor signaling by lipids.
Nature communications - 24 Jun 2021
Damian Marjorie, Louet Maxime, Gomes Antoniel Augusto Severo, M'Kadmi Céline, Denoyelle Séverine, Cantel Sonia, Mary Sophie, Bisch Paulo M, Fehrentz Jean-Alain, Catoire Laurent J, Floquet Nicolas, Banères Jean-Louis
Abstract excerpt
The membrane is an integral component of the G protein-coupled receptor signaling machinery. Here we demonstrate that lipids regulate the signaling efficacy and selectivity of the ghrelin receptor GHSR through specific interactions and bulk effects. We find that PIP2 shifts the conformational equilibrium of GHSR away from its inactive state, favoring basal and agonist-induced G protein activation. This occurs...
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