Exploration of the ligand binding site of the human 5-HT4 receptor by site-directed mutagenesis and molecular modeling

British Journal of Pharmacology

Volumn 130, Issue 3, 2000, Pages 527-538

  Mialet, Jeanne ^a,b   Dahmoune, Yamina ^a   Lezoualc'h, Frank ^a,b   Berque Bestel, Isabelle ^a   Eftekhari, Pierre ^c   Hoebeke, Johan ^c   Sicsic, Sames ^a,d   Langlois, Michel ^a   Fischmeister, Rodolphe ^a,b  

^a UNIVERSITÉ PARIS SACLAY   (France)

^b INSERM   (France)

^c INSTITUT DE BIOLOGIE MOLÉCULAIRE ET CELLULAIRE   (France)

^d UNIVERSITÉ PARIS SUD   (France)

Author keywords

Binding site; Directed mutagenesis; Human; Molecular modeling; Receptor; Serotonin

Indexed keywords

1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 4 AMINO 5 CHLORO 2 METHOXYBENZOIC ACID 2 (1 PIPERIDINYL)ETHYL ESTER; 4 AMINO 5 CHLORO 2 METHOXYBENZOIC ACID 2 (3,5 DIMETHYLPIPERIDINO)ETHYL ESTER; MUTANT PROTEIN; SEROTONIN; SEROTONIN 4 AGONIST; SEROTONIN 4 ANTAGONIST; SEROTONIN 4 RECEPTOR; TRITIUM; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING COMPETITION; BINDING SITE; CONTROLLED STUDY; DNA TRANSFECTION; ENZYME ACTIVATION; HUMAN; ISOTOPE LABELING; LIGAND BINDING; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION;

EID: 0034067964     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703356     Document Type: Article

References (32)

1. 2C receptors: direct and indirect effects on ligand affinity mediated by the same locus. Mol. Pharmacol. 50, 34-42.
2. BALDWIN, J.M. (1994). Structure and function of receptors coupled to G proteins. Curr. Opin. Cell. Biol., 6, 180-190.
3. BALDWIN, J.M., SCHERTLER, G.F.X. & UNGER, V.M. (1997). An alpha-carbon template for the transmembrane helices in rhodopsin family of G-protein-coupled receptors. J. Mol. Biol., 272, 144-164.
4. BALLESTEROS, J.A. & WEINSTEIN, H. (1995). Integrated methods for modelling G-protein coupled receptors. Methods Neurosci., 25, 366-428.
5. 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J. Neurochem., 70, 2252-2261.
6. 4 receptor cloned from human atrium. FEES Lett., 412, 465-474.
7. 6 receptor. J. Neurochem., 5, 2169-2177.
8. BOUSSIF, O., LEZOUALC'H, F., ZANTA, M.A., MERGNY, M.D., SCHERMAN, D., DEMENEIX, B. & BEHR, J.P. (1995). A versatile vector for gene and oligonucleotide transfer into cells in culture and in vivo: polyethylenimine. Proc. Natl. Acad. Sci. U.S.A., 92, 7297-7301.
9. BRADFORD, M.M. (1976). A rapid and sensitive method for the quantitation of microgram quantities of protein utilising the principle of protein-dye binding. Anal. Biochem., 72, 248-254.
10. 1B-adrenergic receptor involved in agonist binding: differences in docking catecholamines to receptor subtypes. FEBS Lett.. 399, 9-13.
11. 4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Mol. Pharmacol., 55, 910-920.
12. 4 receptors. Trends Pharmacol. Sci., 16, 391-397.
13. 4 receptors. FASEB J., 10, 1398-1407.
14. HIBERT, M.F., TRUMPP-KALLMEYER, A., BRUINVELS, A. & HOFLACK, J. (1991). Three dimensional models of neurotransmitter G-binding protein coupled receptors. Mol. Pharmacol., 40, 8-15.
15. 1A receptor: a site-directed mutation study. FEBS Lett., 312, 259-262.
16. 4 receptors mediate arrhythmias? Trends Pharmacol. Sci., 15, 451-455.
17. LEBESGUE, D., WALLUKAT, G., MIJARES, A., GRANIER, C., ARGIBAY, J. & HOEBEKE, J. (1998). An agonist-like monoclonal antibody against the human β2-adrenoreceptor. Eur. J. Pharmacol., 348, 123-133.
18. NEIMARK, J. & BRIAND, J.P. (1993). Development of a fully automated multichannel peptide synthesizer with integrated TFA cleavage capability. Peptide Res., 6, 219-228.
19. NORDVALL, G. & HACKSELL, U. (1993). Binding-site modeling of the muscarinic ml receptor: a combination of homology-based and indirect approaches. J. Med. Chem., 36, 967-976.
20. PERSSON, A. & JERGIL, B. (1992). Purification of plasma membranes by aqueous two-phase affinity partitioning. Anal. Biochem., 204, 131-136.
21. 4 receptors in post mortem human brain tissue: distribution, pharmacology and affects of neurodegenerative diseases. Br. J. Pharmacol., 114, 993-998.
22. X 32 Gap junctions. Biophys. J., 76, 2887-2898.
23. 2A receptors. Mol. Pharmacol., 52, 259-266.
24. SANKARARAMAKRISHNAN, R. & VISHVESHWARA, S. (1990). Conformational studies on peptides with proline in the right-handed alpha-helical region. Biopolymers, 30, 287-298.
25. SAVARESE, T.M. & FRASER, C.M. (1992). In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors. Biochem, J., 283, 1-19.
26. SAXENA, P.R. (1995). Serotonin receptors: subtypes, functional responses and therapeutic relevance. Pharmacol. Ther., 66, 339-368.
27. 2A receptor. J. Biol. Chem., 270, 16683-16688.
28. TRUMPP-KALLMEYER, S., HOFLACK, J., BRUINVELS, A. & HIBERT, M. (1992). Modeling of G-protein-coupled receptors: application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors. J. Med. Chem., 35, 3448-3462.
29. VAN RHEE, A.H. & JACOBSON, K.A. (1996). Molecular architecture of G protein-coupled receptors. Drug. Dev. Des., 37, 1-38.
30. 2 receptor: identification of amino acids necessary for ligand binding and receptor activation. Mol. Pharmacol., 43, 931-940.
31. 4 receptors in brain tissues from patients with neurodegenerative disorders. Behav. Brain. Res., 73, 249-252.
32. 4 receptors. J. Med. Chem., 40, 608-621.