How ligands and signalling proteins affect G-protein-coupled receptors' conformational landscape

Biochemical Society Transactions

Volumn 41, Issue 1, 2013, Pages 144-147

  Mary, Sophie ^a   Fehrentz, Jean Alain ^a   Damian, Marjorie ^a   Verdié, Pascal ^a   Martinez, Jean ^a   Marie, Jacky ^a   Banères, Jean Louis ^a  

^a CNRS   (France)

Author keywords

Arrestin; Conformation stabilization; G protein; G protein coupled receptor; Ghrelin receptor; Ligand; Signalling

Indexed keywords

CYSTEINE; G PROTEIN COUPLED RECEPTOR; GHRELIN RECEPTOR; LIGAND; SIGNAL PEPTIDE;

CONFERENCE PAPER; CROSS COUPLING REACTION; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN STABILITY; PROTEIN TRANSPORT;

LIGANDS; PROTEIN BINDING; PROTEIN CONFORMATION; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION;

EID: 84873177291     PISSN: 03005127     EISSN: 14708752     Source Type: Journal    
DOI: 10.1042/BST20120267     Document Type: Conference Paper

References (19)

1. Lagerstrom, M. C. and Schioth, H. B. (2008) Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat. Rev. Drug Discovery 7, 339-357
2. Audet, M. and Bouvier, M. (2012) Restructuring G-protein-coupled receptor activation. Cell 151, 14-23
3. Luttrell, LM. and Kenakin, T. P. (2011) Refining efficacy: allosterism and bias in G protein-coupled receptor signaling. Methods Mol. Biol. 756, 3-35
4. Popot, J.-L (2010) Amphipols, nanodiscs, and fluorinated surfactants: three nonconventional approaches to studying membrane proteins in aqueous solutions. Annu. Rev. Biochem. 79, 737-775
5. Vilardaga, J.-P., Steinmeyer, R., Harms, G. S. and Lohse, M. J. (2005) Molecular basis of inverse agonism in a G protein-coupled receptor. Nat. Chem. Biol. 1, 25-28
6. 2a-adrenergic receptor activation reveals distinct agonist-specific conformational changes. Mol. Pharmacol. 75, 534-541
7. Audet, N., Gales, C, Archer-Lahlou, E., Vallieres, M., Schiller, P. W., Bouvier, M. and Pineyro, G. (2008) Bioluminescence resonance energy transfer assays reveal ligand-specific conformational changes within preformed signaling complexes containing δ-opioid receptors and heterotrimeric G proteins. J. Biol. Chem. 283, 15078-15088
8. 2- adrenergic receptor. J. Biol. Chem. 285, 36188-36198
9. Saulière, A., Bellot, M., Paris, H., Denis, C., Finana, F., Hansen, J. T., Altié, M. F., Seguelas, M. H., Pathak, A., Hansen, J. L. et al. (2012) Deciphering biased-agonism complexity reveals a new active AT1 receptor entity. Nat. Chem. Biol. 8, 622-630
10. Ghanouni, P., Gryczynski, Z., Steenhuis, J. J., Lee, T. W., Farrens, D. L., Lakowicz, J. R. and Kobilka, B. K. (2001) Functionally different agonists induce distinct conformations in the G protein coupling domain of the β2 adrenergic receptor. J. Biol. Chem. 276, 24433-24436
11. Kahsai, A. W., Xiao, K., Rajagopal, S., Ahn, S., Shukla, A. K., Sun, J., Oas, T. G. and Lefkowitz, R. J. (2011) Multiple ligand-specific conformations of the β2-adrenergic receptor. Nat. Chem. Biol. 7, 692-700
12. Liu, J. J., Horst, R., Katritch, V., Stevens, R. C. and Wüthrich, K. (2012) Biased signaling pathways in β2-adrenergic receptor characterized by 19 F-NMR. Science 335, 1106-1110
13. 4 receptor: a structural basis for drug efficacy. J. Biol. Chem. 280, 20253-20260 (Pubitemid 40776722)
14. Rameh, R., Damian, M., Cottet, M., Orcel, H., Mendre, C., Durroux, T., Sharma, K. S., Durand, G., Pucci, B., Trinquet, E. et al. (2012) Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy. Proc. Natl. Acad. Sci. U. S. A. 109, 6733-6738
15. Mary, S., Damian, M., Louet, M., Floquet, N., Fehrentz, J.-A., Marie, J., Martinez, J. and Baneres, J.-L (2012) Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor. Proc. Natl. Acad. Sci. U. S. A. 109, 8304-8309
16. α-subunits differentially alter the conformation and agonist affinity of κ-opioid receptors. Biochemistry 47, 1567-1578 (Pubitemid 351231207)
17. Deupi, X. and Kobilka, B. K. (2010) Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology 25, 293-303
18. 2 adrenoceptor. Nature 469, 175-180
19. s protein complex. Nature 477, 549-555