Direct observation of G-protein binding to the human delta-opioid receptor using plasmon-waveguide resonance spectroscopy, J Biol Chem, vol.278, issue.49, pp.48890-48897, 2003. ,
Pharmacological comparison between [ 3 H]-GR113808 binding sites and functional 5-HT4 receptors in neurons, Eur J Pharmacol, vol.298, pp.165-174, 1996. ,
Integrated methods for the construction of three dimentional models and computational probing of structure-function relations in G protein coupled receptors, Methods in Neurosciences, vol.25, pp.366-428, 1995. ,
Serine and threonine residues bend alpha-helices in the chi(1) = g(-) conformation, Biophys J, vol.79, issue.5, pp.2754-2760, 2000. ,
Molecular characterization of a purified 5-HT4 receptor: a structural basis for drug efficacy, J Biol Chem, vol.280, issue.21, pp.20253-20260, 2005. ,
URL : https://hal.archives-ouvertes.fr/hal-00016896
Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements, J Biol Chem, vol.280, issue.30, pp.27924-27934, 2005. ,
URL : https://hal.archives-ouvertes.fr/hal-00016899
Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor, Nature, vol.374, issue.6519, pp.272-276, 1995. ,
, , vol.9, 2006.
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor, Science, vol.318, issue.5854, pp.1258-1265, 2007. ,
A Single Mutation in the 5-HT4 Receptor (5-HT4-R D100(3.32)A) Generates a Gs-coupled Receptor Activated Exclusively by Synthetic Ligands (RASSL), J Biol Chem, vol.278, issue.2, pp.699-702, 2003. ,
Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain, Mol Pharmacol, vol.55, issue.5, pp.910-920, 1999. ,
Pharmacological properties of 5-Hydroxytryptamine(4) receptor antagonists on constitutively active wild-type and mutated receptors, Mol Pharmacol, vol.58, issue.1, pp.136-144, 2000. ,
A point-charge force field for molecular mechanics simulations of proteins based on condensed-phase quantum mechanical calculations, J Comput Chem, vol.24, issue.16, pp.1999-2012, 2003. ,
Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor, J Biol Chem, vol.276, issue.27, pp.24433-24436, 2001. ,
Linking agonist binding to histamine H1 receptor activation, Nat Chem Biol, vol.1, issue.2, pp.98-103, 2005. ,
A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists, J Biol Chem, vol.277, issue.28, pp.25502-25511, 2002. ,
G protein coupled receptor structure and activation, Biochim Biophys Acta, vol.1768, issue.4, pp.794-807, 2007. ,
The two-state model of receptor activation, Trends Pharmacol Sci, vol.16, issue.3, pp.89-97, 1995. ,
Structure of bovine rhodopsin in a trigonal crystal form, J Mol Biol, vol.343, issue.5, pp.1409-1438, 2004. ,
Specific tryptophan UV-absorbance changes are probes of the transition of rhodopsin to its active state, Biochemistry, vol.35, issue.34, pp.11149-11159, 1996. ,
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligandreceptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors, J Med Chem, vol.48, issue.7, pp.2548-2558, 2005. ,
Structural mimicry in class A G protein-coupled receptor rotamer toggle switches: the importance of the F3.36(201)/W6.48(357) interaction in cannabinoid CB1 receptor activation, J Biol Chem, vol.279, pp.48024-48037, 2004. ,
Analysis of the relationship between side-chain conformation and secondary structure in globular proteins, J Mol Biol, vol.198, issue.2, pp.295-310, 1987. ,
Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling, Br J Pharmacol, vol.130, issue.3, pp.527-538, 2000. ,
Activation of rhodopsin: new insights from structural and biochemical studies, Trends Biochem Sci, vol.26, issue.5, pp.318-324, 2001. ,
Crystal structure of rhodopsin: A G protein-coupled receptor, Science, vol.289, issue.5480, pp.739-745, 2000. ,
The role of internal water molecules in the structure and function of the rhodopsin family of G protein-coupled receptors, Chembiochem, vol.8, issue.1, pp.19-24, 2007. ,
Crystal structure of the ligand-free G-protein-coupled receptor opsin, Nature, vol.454, issue.7201, pp.183-187, 2008. ,
GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function, Science, vol.318, issue.5854, pp.1266-1273, 2007. ,
Electron crystallography reveals the structure of metarhodopsin I, Embo J, vol.23, issue.18, pp.3609-3620, 2004. ,
A mutation-induced activated state of the b2-adrenergic receptor. Extending the ternary complex model, J Biol Chem, vol.268, pp.4625-4635, 1993. ,
Structure of rhodopsin and the metarhodopsin I photointermediate, Curr Opin Struct Biol, vol.15, issue.4, pp.408-415, 2005. ,
Molecular mechanism of 7TM receptor activation--a global toggle switch model, Annu Rev Pharmacol Toxicol, vol.46, pp.481-519, 2006. ,
The binding site of aminergic G protein-coupled receptors: the transmembrane segments and second extracellular loop, Annu Rev Pharmacol Toxicol, vol.42, pp.437-467, 2002. ,
Beta2 adrenergic receptor activation. Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch, J Biol Chem, vol.277, issue.43, pp.40989-40996, 2002. ,
Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity, Annu Rev Pharmacol Toxicol, vol.47, pp.53-87, 2007. ,
Sequential binding of agonists to the beta2 adrenoceptor. Kinetic evidence for intermediate conformational states, J Biol Chem, vol.279, issue.1, pp.686-691, 2004. ,
An activation switch in the rhodopsin family of G protein-coupled receptors: the thyrotropin receptor, J Biol Chem, vol.280, issue.17, pp.17135-17141, 2005. ,
Three-dimensional representations of G proteincoupled receptor structures and mechanisms, Methods Enzymol, vol.343, pp.329-371, 2002. ,
Development and testing of a general amber force field, J Comput Chem, vol.25, issue.9, pp.1157-1174, 2004. ,
, bond between the -NH amide and a carbonyl or methoxy group, respectively. BIMU8 elicits 5-HT4R activation by forming a hydrogen bond interaction with W6, p.while
, S-zacopride triggers activation via the interaction with T3.36 in the active g+ conformation (B). The atoms implicated in these interactions are pointed out: oxygen of the drugs is asterisked and T3, vol.36
, cAMP accumulation at different densities of 5-HT4-W6.48A mutant
, *Data are expressed as a percentage of maximal stimulation due to 5-HT in W6.48A mutant expressing the highest receptor density (6490 fmol/mg protein), cells, was measured over 10 min-stimulation induced by 5-HT (A) or BIMU8 (B), vol.500, 1000.
, In the absence of W6.48, the aromatic ring of BIMU8 occupies the position of the active t conformation of W6.48 in the WT receptor (see Fig. 5C); and the carbonylic oxygen hydrogen bonds the active g+ rotamer of T3.36. The atoms implicated in this interaction are pointed out: oxygen of the drug is asterisked and T3, Computational models of the complex between BIMU8 and W6.48A mutant receptor