Cyclothiazide binding to functionally active AMPA receptor reveals genuine allosteric interaction with agonist binding sites

Neurochemistry International

Volumn 44, Issue 4, 2004, Pages 271-280

  Kovács, Ilona ^a   Simon, Ágnes ^a   Szárics, Éva ^a   Barabás, Péter ^a   Héja, László ^a   Nyikos, Lajos ^a   Kardos, Julianna ^a  

^a CHEMICAL RESEARCH CENTER   (Hungary)

Author keywords

Agonist; AMPA; Cyclothiazide

Indexed keywords

6 NITRO 7 SULFAMOYLBENZO[F]QUINOXALINE 2,3 DIONE; AMPA RECEPTOR; CYCLOTHIAZIDE; WILLARDIINE;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; BINDING SITE; BIOAVAILABILITY; BRAIN CORTEX; CELL MEMBRANE; CONTROLLED STUDY; DRUG BINDING; MALE; MEMBRANE VESICLE; MOLECULAR INTERACTION; MOLECULAR RECOGNITION; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; RAT; SEQUENTIAL ANALYSIS;

EID: 0242268074     PISSN: 01970186     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0197-0186(03)00137-2     Document Type: Article

References (46)

1. Arai C.A., Kessler M., Rogers G., Lynch G. Effects of potent ampakine CX614 on hippocampal and recombinant AMPA receptors: interactions with cyclothiazide and GYKI 52466. Mol. Pharmacol. 58:2000;802-813.
2. Armstrong N., Gouaux E. Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structure of the GluR2 ligand-binding core. Neuron. 28:2000;165-181.
3. Armstrong N., Sun Y., Chen G.-Q., Gouaux E. Structure of a glutamate receptor ligand-binding core in complex with kainate. Nature. 395:1998;913-917.
4. Baker E.N., Hubbard R.E. Hydrogen-bonding in globular proteins. Prog. Biophys. Mol. Biol. 44:1984;97-197.
5. Clark M., Cramer R.D. III, Van Opdenbosch J. Validation of the general purpose Tripos 5.2 force field. J. Comput. Chem. 10:1989;982-1012.
6. Clements J.D., Feltz A., Sahara Y., Westbrook G.L. Activation kinetics of AMPA receptor channel reveals the number of functional agonist binding sites. J. Neurosci. 18:1998;119-127.
7. Colquhoun D. Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonist and of the effects of mutating receptors. Br. J. Pharmacol. 125:1998;924-947.
8. 3H ]nitro-7- sulphamoylbenzo[f]-quinoxaline-2,3-dione to rat brain J. Neurochem. 67:1996;2609-2612.
9. Gasteiger J., Marsili M. A new model for calculating atomic charges in molecules. Tetrahedron Lett. 34:1978;3181-3184.
10. 3H ]AMPA binding to rat brain membranes: evidence that AMPA receptor desensitisation increases agonist affinity Brain Res. 628:1993;345-348.
11. 3H ]-5-fluorowillardiine binding in rat brain Br. J. Pharmacol. 116:1995a;2033-2039.
12. 3H ]AMPA to rat brain synaptic membranes: effects of a series of structural analogues of the non-NMDA receptor agonist willardiine Neuropharmacology. 34:1995b;405-410.
13. Hawkinson J.E., Espitia S.A. Effects of thiocyanate and AMPA receptor ligands on (S)-5-fluorowillardiine, (S)-AMPA and (R,S)-AMPA binding. Eur. J. Pharmacol. 329:1997;213-221.
14. Jin R., Gouaux E. Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5′-substituted willardiines and GluR2 S1S2 in the crystal. Biochemistry. 42:2002;5201-5213.
15. Jin R., Horning M., Mayer M.L., Gouaux E. Mechanism of activation and selectivity in a ligand-gated ion channel: structural and functional studies of GluR2 and quisqualate. Biochemistry. 41:2002;15635-15643.
16. A receptor J. Neurochem. 55:1990;1095-1099.
17. Kardos J., Nyikos L. Universality of receptor channel responses. Trends Pharmacol. Sci. 22:2001;642-645.
18. Kardos J., Kovács I., Blandl T., Cash D.J. Modulation of GABA flux across rat brain membranes resolved by a rapid quenched incubation technique. Neurosci. Lett. 182:1994;73-76.
19. Keserü, G.M., Kolossváry, I., 1999. Molecular Mechanics and Conformational Analysis in Drug Design, Blackwell Scientific Publications, Oxford, pp. 14-15.
20. Kessler M., Arai A., Quan A., Lynch G. Effect of cyclothiazide on binding properties of AMPA-type glutamate receptors: lack of competition between cyclothiazide and GYKI 52466. Mol. Pharmacol. 49:1996;123-131.
21. Koike M., Tsukada S., Tsuzuki K., Kijima H., Ozawa S. Regulation of kinetic properties of GluR2 AMPA receptor channels by alternative splicing. J. Neurosci. 20:2000;2166-2177.
22. Krogsgaard-Larsen P., Hansen J.J., Lauridsen J., Peet M.J., Leah J.D., Curtis D.R. Glutamic acid agonists. Stereochemical and conformational studies of DL-amino-3-hydroxy-5-methyl-isoxazolepropionic acid (AMPA) and related compounds. Neurosci. Lett. 31:1982;313-317.
23. 3H ]LY395153) to native and recombinant AMPA receptors Neuropharmacology. 40:2001;1010-1018.
24. Lowry O.H., Rosebrough N.J., Farr A.L., Randall R.J. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193:1951;265-275.
25. Martin A., Récasens M., Guiramand J. DNQX-induced toxicity in cultured rat hippocampal neurons: an apparent AMPA receptor-independent effect? Neurochem. Int. 42:2003;251-260.
26. McDonald I.K., Thornton J. Satisfying hydrogen-bonding potential in proteins. J. Mol. Biol. 238:1994;777-793.
27. Mosbacher J., Schoepfer R., Monyer H., Burnashev N., Seeburg P.H., Rupersberg J.P. A molecular determinant for submillisecond desensitisation in glutamate receptors. Science. 266:1994;1059-1061.
28. Nyikos L., Simon Á., Barabás P., Kardos J. Ligand-specific conformations of an ionotropic glutamate receptor. Protein Eng. 15:2002;717-720.
29. Partin K.M., Patneau D.K., Winters C.A., Mayer M.L., Buonanno A. Selective modulation of desensitisation at AMPA versus kainate receptors by cyclothiazide and concanavalin A. Neuron. 11:1993;1069-1082.
30. Partin K.M., Fleck M.W., Mayer M.L. AMPA receptor flip/flop mutants affecting deactivation, desensitisation, and modulation by cyclothiazide, aniracetam, and thiocyanate. J. Neurosci. 16:1996;6634-6647.
31. Patel D.R., Croucher M.J. Evidence for a role of presynaptic AMPA receptors in the control of neuronal glutamate release in the rat forebrain. Eur. J. Pharmacol. 332:1997;143-151.
32. Robert A., Irizarry S.N., Hughes T.E., Howe J.R. Subunit interactions and AMPA receptor desensitisation. J. Neurosci. 21:2001;5574-5586.
33. Rosenmund C., Mansour M. How to be desensitised. Nature. 417:2002;238-239.
34. Rosenmund C., Stern-Bach Y., Stevens C. The tetrameric structure of a glutamate receptor channel. Science. 280:1998;1596-1599.
35. Safferling M., Tichelaar W., Kümmerle G., Jouppila A., Kuusinen A., Keinänen K., Madden D.R. First images of a glutamate receptor ion channel: oligomeric state and molecular dimensions of GluRB homomers. Biochemistry. 40:2001;13948-13953.
36. Simon Á., Simon I., Rajnavölgyi É. Modeling MHC class II molecules and their bound peptides as expressed at the cell surface. Mol. Immunol. 38:2001;681-687.
37. Sinclair C., Reavy H., Grieve A., Schousboe A., Morelli E., Novellino E., Campiani G., Griffiths R. Inherent desensitisation-preventing properties of a novel, subtype-selective AMPA receptor agonist, (S)-CPW 399, as a possible explanation for its excitotoxic action in cultured cerebellar granule cells. Neurochem. Int. 42:2003;499-510.
38. Smith T.C., Wang L.-Y., Howe J.R. Heterogeneous conductance levels of native AMPA receptors. J. Neurosci. 20:2000;2073-2085.
39. Sommer B., Keinänen K., Verdorn T.A., Wisden W., Burnashev N., Herb A., Köhler M., Takagi T., Sakmann B., Seeburg P.H. Flip and flop: a cell-specific functional switch in glutamate-operated channels of the CNS. Science. 249:1990;1580-1585.
40. Sun Y., Olson R., Horning M., Armstrong N., Mayer M., Gouaux E. Mechanism of glutamate receptor desensitisation. Nature. 417:2002;245-253.
41. + ion flux and receptor desensitisation with native membrane. Neurochem. Int. 36:2000;83-90.
42. 2+ ion flux to (+)[S]-α-amino-3-hydroxy-5-methylisoxazole-4- propionic acid. Mol. Pharmacol. 59:2001;920-928.
43. Vizi E.S., Mike A., Tarnawa I. 2,3-Benzodiazepines (GYKI 52466 and analogs): negative allosteric modulators of AMPA receptors. CNS Drug Rev. 2:1996;91-126.
44. Vizi E.S., Mike A., Tarnawa I. The functional study of kainite receptors - hopes and doubts. Trends Neurosci. 20:1997;396.
45. Weiner S.J., Kollmann P.A., Case D.A., Singh U.C., Ghio C., Alagona G., Profeta S., Weiner P. A new force field for molecular mechanical simulation of nucleic acids and proteins. J. Am. Chem. Soc. 106:1984;765-784.
46. Yamada K.A., Tang C.-M. Benzothiazides inhibit rapid glutamate receptor desensitisation and enhance glutamatergic synaptic currents. J. Neurosci. 13:1993;3904-3915.