Abstract
Background: GHS-R1a activates multiple signaling pathways mediating feeding and addictive behaviors. Results: Some GHS-R1a ligands activate Gq but not Gi/o and fail to recruit β-arrestin2; others act as selective inverse agonists at Gq compared with G13. Conclusion: Synthetic ligands can selectively activate or reverse Gq-dependent signaling at GHS-R1a. Significance: Ligand-biased signaling can be exploited for the development of selective drugs to treat GHS-R1a-mediated Disorders.
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CITATION STYLE
M’Kadmi, C., Leyris, J. P., Onfroy, L., Galés, C., Sauliére, A., Gagne, D., … Marie, J. (2015). Agonism, antagonism, and inverse agonism bias at the ghrelin receptor signaling. Journal of Biological Chemistry, 290(45), 27021–27039. https://doi.org/10.1074/jbc.M115.659250
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