Affinity labeling of cysteine-mutants evidences contact residues in modeled receptor binding sites

Journal of Receptors and Signal Transduction

Volumn 22, Issue 1-4, 2002, Pages 345-356

  Perret, P ^a   Laube, B ^b   Schemm, R ^b   Betz, H ^b   Goeldner, M ^c   Foucaud, B ^c  

^a TEXAS A AND M UNIVERSITY   (United States)

^b MAX PLANCK INSTITUTE FOR BRAIN RESEARCH   (Germany)

^c CNRS   (France)

Author keywords

Binding site topology; Cysteine scanning; Engineered chemical coupling

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 7 CHLORO 4 HYDROXY 3 (3 PHENOXYPHENYL) 2 QUINOLONE; CYSTEINE; GLYCINE; IONOTROPIC RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; POLYPEPTIDE; VERAPAMIL;

AFFINITY LABELING; BINDING SITE; CONFERENCE PAPER; GENE EXPRESSION SYSTEM; METHODOLOGY; MUTANT; MUTATION; PHARMACOPHORE; RECEPTOR BINDING; SITE DIRECTED MUTAGENESIS; WILD TYPE;

AFFINITY LABELS; ANIMALS; ANTI-ANXIETY AGENTS; BINDING SITES; CYSTEINE; GLYCINE; LIGANDS; MUTATION; OOCYTES; QUINOLONES; RECEPTORS, GABA-A; RECEPTORS, N-METHYL-D-ASPARTATE; XENOPUS LAEVIS;

EID: 0036977909     PISSN: 10799893     EISSN: 15324281     Source Type: Journal    
DOI: 10.1081/RRS-120014606     Document Type: Conference Paper

References (31)

1. Ralston, E.; De Coen, J.-L. Folding of Polypeptide Chains Induced by the Amino Acid Side-Chains. J. Mol. Biol. 1974, 83, 393-420.
2. Kossiakoff, A.A. Protein Dynamics Investigated by the Neutron Diffraction-Hydrogen Exchange Technique. Nature 1982, 296, 713-721.
3. Paas, Y.; Devillers-Thiery, A.; Teichberg, V.I.; Changeux, J.-P.; Eisenstein, M. How Well Can Molecular Modelling Predict the Crystal Structure: The Case of the Ligand-Binding Domain of Glutamate Receptors. Trends Pharmacol. Sci. 2000, 21, 87-92.
4. Sutcliffe, M.J.; Smeeton, A.H.; Wo, Z.G.; Oswald, R.E. Molecular Modeling of Ligand-Gated Ion Channels. Methods Enzymol. 1998, 293, 589-620.
5. Ivanovic, A.; Reilander, H.; Laube, B.; Kuhse, J. Expression and Initial Characterization of a Soluble Glycine Binding Domain of the N-Methyl-D-Aspartate Receptor NR1 Subunit. J. Biol. Chem. 1998, 273, 19933-19937.
6. Madden, D.R.; Abele, R.; Andersson, A.; Keinanen, K. Large-Scale Expression and Thermodynamic Characterization of a Glutamate Receptor Agonist-Binding Domain. Eur. J. Biochem. 2000, 267, 4281-4289.
7. Armstrong, N.; Sun, Y.; Chen, G.Q.; Gouaux, E. Structure of a Glutamate-Receptor Ligand-Binding Core in Complex with Kainate. Nature 1998, 395, 913-917.
8. Foucaud, B.; Perret, P.; Grutter, T.; Goeldner, M. Cysteine Mutants as Chemical Sensors for Ligand Receptor Interactions. Trends Pharmacol. Sci. 2001, 22, 170-173.
9. A-Receptor Subtypes Really Occur in the Brain? Trends Neurosci. 1996, 19, 139-143.
10. A Channel that Abolish Block by Picrotoxin. Recept. Channels 1995, 3, 13-20.
11. A Alpha1 Beta1 Receptors. J. Membrane Biol. 1996, 154, 11-21.
12. Ffrench-Constant, R.H.; Mortlock, D.P.; Shaffer, C.D.; McIntyre, R.J.; Roush, R.T. Molecular Cloning and Transformation of Cyclodiene Resistance in Drosophila: An Invertebrate Gamma-Aminobutyric Acid Subtype A Receptor Locus. Proc. Natl. Acad. Sci. 1991, 88, 7209-7213.
13. A Receptor Channel-Lining Residues Probed in Cysteine Mutants. Biophys. J. 1995, 69, 1858-1867.
14. Perret, P.; Sarda, X.; Wolff, M.; Bushey, D.; Goeldner, M. Interaction of Non-Competitive Blockers Within the Gamma-Aminobutyric Acid Type A Chloride Channel Using Chemically-Reactive Probes as Chemical Sensors for Cysteine Mutants. J. Biol. Chem. 1999, 274, 25350-25354.
15. 3H] Quinacrine Azide in the Active State of the Nicotinic Acetylcholine Receptor. J. Biol. Chem. 1990, 265, 11017-11029.
16. Laube, B.; Kuhse, J.; Betz, H. Evidence for a Tetrameric Structure of Recombinant NMDA Receptors. J. Neurosci. 1998, 18, 2954-2961.
17. Laurie, D.J.; Seeburg, P.H. Ligand Affinities at Recombinant N-Methyl-D-Aspartate Receptors Depend on Subunit Composition. Eur. J. Pharmacol.-Molec. Pharm. 1994, 268, 335-345.
18. Buller, A.L.; Larson, H.C.; Schneider, B.E.; Beaton, J.A.; Morrisett, R.A.; Monaghan, D.T. The Molecular Basis of NMDA Receptor Subtypes: Native Receptor Diversity is Predicted by Subunit Composition. J. Neurosci. 1994, 14, 5471-5484.
19. Hirai, H.; Kirsch, J.; Laube, B.; Betz, H.; Kuhse, J. The Glycine Binding Site of the N-Methyl-D-Aspartate Receptor Subunit NR1: Identification of Novel Determinants of Co-Agonist Potentiation in the Extracellular M3-M4 Loop Region. Proc. Natl. Acad. Sci. USA 1996, 93, 6031-6036.
20. Kuryatov, A.; Laube, B.; Betz, H.; Kuhse, J. Mutational Analysis of the Glycine-Binding Site of the NMDA Receptor: Structural Similarity with Bacterial Amino Acid-Binding Proteins. Neuron 1994, 12, 1291-1300.
21. Wafford, K.A.; Kathoria, M.; Bain, C.J.; Marshall, G.; Le Bourdellés, B.; Kemp, J.A.; Whiting, P.J. Identification of Amino Acids in the N-Methyl-D-Aspartate Receptor NR1 Subunit That Contributes to the Glycine Binding Site. Mol. Pharmacol. 1995, 47, 374-380.
22. Williams, K.; Chao, J.; Kashiwagi, K.; Masuko, T.; Igarashi, K. Activation of N-Methyl-D-Aspartate Receptors by Glycine: Role of an Aspartate Residue in the M3-M4 Loop of the NR1 Subunit. Mol. Pharmacol. 1996, 50, 701-708.
23. Wood, M.W.; VanDongen, H.M.; VanDongen, A.M. An Alanine Residue in the M3-M4 Linker Lines the Glycine Binding Pocket of the N-Methyl-D-Aspartate Receptor. J. Biol. Chem. 1997, 272, 3532-3537.
24. Laube, B.; Hirai, H.; Sturgess, M.; Betz, H.; Kuhse, J. Molecular Determinants of Agonist Discrimination by NMDA Receptor Subunits: Analysis of the Glutamate Binding Site on the NR2B Subunit. Neuron 1997, 18, 493-503.
25. Armstrong, N.; Gouaux, E. Mechanisms for Activation and Antagonism of an AMPA-Sensitive Glutamate Receptor: Crystal Structures of the GluR2 Ligand Binding Core. Neuron 2000, 28, 165-181.
26. Wittekindt, B.; Malany, S.; Schemm, R.; Otvos, L.; Maccecchini, M.-L.; Laube, B.; Betz, H. Point Mutations Identify the Glutamate Binding Pocket of the N-Methyl-D-Aspartate Receptor as Major Site of Conantokin-G Inhibition. Neuropharmacology 2001, 41, 753-761.
27. Foucaud, B.; Laube, B.; Schemm, R.; Kreimeyer, A.; Goeldner, M.; Betz, H. Unpublished.
28. Kreimeyer, A.; Laube, B.; Sturgess, M.; Goeldner, M.; Foucaud, B. Evaluation and Biological Properties of Reactive Ligands for the Mapping of the Glycine Site on the N-Methyl-D-Aspartate (NMDA) Receptor. J. Med. Chem. 1999, 42, 4394-4404.
29. Loo, T.W.; Clarke, D.M. Defining the Drug-Binding Site in the Human Multidrug Resistance P-Glycoprotein Using a Methanethiosulfonate Analog of Verapamil, MTS-Verapamil. J. Biol. Chem. 2001, 276, 14972-14979.
30. Wood, M.W.; VanDongen, H.M.; VanDongen, A.M. A Mutation in the Glycine Binding Pocket of the N-Methyl-D-Aspartate Receptor NR1 Subunit Alters Agonist Efficacy. Mol. Brain Res. 1999, 73, 189-192.
31. Brejc, K.; van Dijk, W.J.; Klaassen, R.V.; Schuurmans, M.; van der Oost, J.; Smit, A.B.; Sixma, T.K. Crystal Structure of an ACh-Binding Protein Reveals the Ligand-Binding Domain of Nicotinic Receptors. Nature 2001, 411, 269-276.