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New advances in production and functional folding of G-protein-coupled receptors |
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| Authors: | Banères Jean-Louis Popot Jean-Luc Mouillac Bernard |
| Institution: | 1 CNRS, UMR-5247, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, F-34000 Montpellier, France 2 Universités de Montpellier 1 & 2, F-34000 Montpellier, France 3 CNRS, UMR-7099, Laboratoire de Physico-Chimie Moléculaire des Protéines Membranaires, Institut de Biologie Physico-Chimique, 13 rue Pierre et Marie Curie, F-75000 Paris, France 4 Université Paris-7, F-75000 Paris, France 5 CNRS, UMR-5203, Institut de Génomique Fonctionnelle, Département de Pharmacologie Moléculaire, 141 rue de la Cardonille, F-34000 Montpellier, France 6 INSERM, U661, F-34000 Montpellier, France |
| Abstract: | G-protein-coupled receptors (GPCRs), the largest family of integral membrane proteins, participate in the regulation of many physiological functions and are the targets of approximately 30% of currently marketed drugs. However, knowledge of the structural and molecular bases of GPCR functions remains limited owing to difficulties related to their overexpression, purification and stabilization. The development of new strategies aimed at obtaining large amounts of functional GPCRs is therefore crucial. Here, we review the most recent advances in the production and functional folding of GPCRs from Escherichia coli inclusion bodies. Major breakthroughs open exciting perspectives for structural and dynamic investigations of GPCRs. In particular, combining targeting to bacterial inclusion bodies with amphipol-assisted folding is emerging as a highly powerful strategy. |
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