The dynamic character of GPCRs (G-protein-coupled receptors) is essential to their function. However, the details of how ligands and signalling proteins stabilize a receptor conformation to trigger the activation of a given signalling pathway remain largely unexplored. Multiple data, including recent results obtained with the purified ghrelin receptor, suggest a model where ligand efficacy and functional selectivity are directly related to different receptor conformations. Importantly, distinct effector proteins (G-proteins and arrestins) as well as ligands are likely to affect the conformational landscape of GPCRs in different manners, as we show with the isolated ghrelin receptor. Such modulation of the GPCR conformational landscape by pharmacologically distinct ligands and effector proteins has major implications for the design of new drugs that activate specific signalling pathways.
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February 2013
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Conference Article|
January 29 2013
How ligands and signalling proteins affect G-protein-coupled receptors' conformational landscape
Sophie Mary;
Sophie Mary
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Jean-Alain Fehrentz;
Jean-Alain Fehrentz
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Marjorie Damian;
Marjorie Damian
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Pascal Verdié;
Pascal Verdié
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Jean Martinez;
Jean Martinez
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Jacky Marie;
Jacky Marie
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
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Jean-Louis Banères
Jean-Louis Banères
1
1CNRS UMR 5247, and Université Montpellier 1 and 2, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, Montpellier 34093, cedex 05, France
1To whom correspondence should be addressed (email[email protected]).
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Publisher: Portland Press Ltd
Received:
October 15 2012
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2013 Biochemical Society
2013
Biochem Soc Trans (2013) 41 (1): 144–147.
Article history
Received:
October 15 2012
Citation
Sophie Mary, Jean-Alain Fehrentz, Marjorie Damian, Pascal Verdié, Jean Martinez, Jacky Marie, Jean-Louis Banères; How ligands and signalling proteins affect G-protein-coupled receptors' conformational landscape. Biochem Soc Trans 1 February 2013; 41 (1): 144–147. doi: https://doi.org/10.1042/BST20120267
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