Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain

Acta Crystallographica Section D: Biological Crystallography

Volumn 69, Issue 9, 2013, Pages 1645-1652

  Krintel, Christian ^a   Harpsøe, Kasper ^a,c   Zachariassen, Linda G ^a   Peters, Dan ^b,d,e   Frydenvang, Karla ^a   Pickering, Darryl S ^a   Gajhede, Michael ^a   Kastrup, Jette S ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b NEUROSEARCH A S   (Denmark)

^c University of Copenhagen   (Denmark)

^d DanPET AB   (Sweden)

^e Aniona   (Denmark)

Author keywords

CX516; GluA2; ionotropic glutamate receptors; ligand binding domains; positive allosteric modulators

Indexed keywords

1,3 DIOXOLANE DERIVATIVE; 1-(QUINOXALIN-6-YLCARBONYL)PIPERIDINE; 2H,3H,6AH PYRROLIDINO(2'',1'' 3',2')1,3 OXAZINO(6',5' 5,4)BENZO(E)1, 4 DIOXAN 10 ONE; 2H,3H,6AH-PYRROLIDINO(2'',1''-3',2')1,3-OXAZINO(6',5'-5,4)BENZO(E)1, 4-DIOXAN-10-ONE; 3 METHYLPIPERIDINE; 3-METHYLPIPERIDINE; 6 QUINOXALINECARBOXYLIC ACID PIPERIDIDE; AMPA RECEPTOR; GLUTAMATE RECEPTOR IONOTROPIC, AMPA 2; IONOTROPIC RECEPTOR; LIGAND; OXAZINE DERIVATIVE; PIPERIDINE DERIVATIVE;

ALLOSTERISM; ANIMAL; ARTICLE; CHEMISTRY; DRUG ANTAGONISM; GENETICS; GLUA2; LIGAND-BINDING DOMAINS; MACROMOLECULE; METABOLISM; MUTATION; POSITIVE ALLOSTERIC MODULATORS; PROTEIN ANALYSIS; PROTEIN BINDING; PROTEIN TERTIARY STRUCTURE; RAT; X RAY CRYSTALLOGRAPHY;

CX516; GLUA2; IONOTROPIC GLUTAMATE RECEPTORS; LIGAND-BINDING DOMAINS; POSITIVE ALLOSTERIC MODULATORS;

ALLOSTERIC REGULATION; ANIMALS; CRYSTALLOGRAPHY, X-RAY; DIOXOLES; LIGANDS; MACROMOLECULAR SUBSTANCES; MUTATION; OXAZINES; PIPERIDINES; PROTEIN BINDING; PROTEIN INTERACTION MAPPING; PROTEIN STRUCTURE, TERTIARY; RATS; RECEPTORS, AMPA;

EID: 84883572916     PISSN: 09074449     EISSN: 13990047     Source Type: Journal    
DOI: 10.1107/S0907444913011839     Document Type: Article

References (39)

1. Adams, P. D. et al. (2010). Acta Cryst. D66, 213-221.
2. Arai, A. C. & Kessler, M. (2007). Curr. Drug Targets, 8, 583-602.
3. Arai, A., Kessler, M., Rogers, G. & Lynch, G. (1996). J. Pharmacol. Exp. Ther. 278, 627-638.
4. Arai, A. C., Kessler, M., Rogers, G. & Lynch, G. (2000). Mol. Pharmacol. 58, 802-813.
5. Arai, A. & Lynch, G. (1998). Brain Res. 799, 230-234.
6. Armstrong, N. & Gouaux, E. (2000). Neuron, 28, 165-181.
7. Battye, T. G. G., Kontogiannis, L., Johnson, O., Powell, H. R. & Leslie, A. G. W. (2011). Acta Cryst. D67, 271-281.
8. Bowie, D. (2008). CNS Neurol. Disord. Drug Targets, 7, 129-143.
9. Broberg, B. V., Glenthøj, B. Y., Dias, R., Larsen, D. B. & Olsen, C. K. (2009). Psychopharmacology, 206, 631-640.
10. Chen, V. B., Arendall, W. B., Headd, J. J., Keedy, D. A., Immormino, R. M., Kapral, G. J., Murray, L. W., Richardson, J. S. & Richardson, D. C. (2010). Acta Cryst. D66, 12-21.
11. Damgaard, T., Larsen, D. B., Hansen, S. L., Grayson, B., Neill, J. C. & Plath, N. (2010). Behav. Brain Res. 207, 144-150.
12. Emsley, P. & Cowtan, K. (2004). Acta Cryst. D60, 2126-2132.
13. Engh, R. A. & Huber, R. (1991). Acta Cryst. A47, 392-400.
14. Goff, D. C., Leahy, L., Berman, I., Posever, T., Herz, L., Leon, A. C., Johnson, S. A. & Lynch, G. (2001). J. Clin. Psychopharmacol. 21, 484-487.
15. Greenwood, J. R., Mewett, K. N., Allan, R. D., Mart?́n, B. O. & Pickering, D. S. (2006). Neuropharmacology, 51, 52-59.
16. Hayward, S. & Berendsen, H. J. (1998). Proteins, 30, 144-154.
17. Ingvar, M., Ambros-Ingerson, J., Davis, M., Granger, R., Kessler, M., Rogers, G. A., Schehr, R. S. & Lynch, G. (1997). Exp. Neurol. 146, 553-559.
18. Ito, I., Tanabe, S., Kohda, A. & Sugiyama, H. (1990). J. Physiol. 424, 533-543.
19. Jin, R., Clark, S., Weeks, A. M., Dudman, J. T., Gouaux, E. & Partin, K. M. (2005). J. Neurosci. 25, 9027-9036.
20. Krintel, C., Frydenvang, K., Olsen, L., Kristensen, M. T., de Barrios, O., Naur, P., Francotte, P., Pirotte, B., Gajhede, M. & Kastrup, J. S. (2012). Biochem. J. 441, 173-178.
21. Langer, G., Cohen, S. X., Lamzin, V. S. & Perrakis, A. (2008). Nature Protoc. 3, 1171-1179.
22. Lynch, G., Granger, R., Ambros-Ingerson, J., Davis, C. M., Kessler, M. & Schehr, R. (1997). Exp. Neurol. 145, 89-92.
23. McCoy, A. J., Grosse-Kunstleve, R. W., Adams, P. D., Winn, M. D., Storoni, L. C. & Read, R. J. (2007). J. Appl. Cryst. 40, 658-674.
24. Mosbacher, J., Schoepfer, R., Monyer, H., Burnashev, N., Seeburg, P. H. & Ruppersberg, J. P. (1994). Science, 266, 1059-1062.
25. Partin, K. M., Fleck, M. W. & Mayer, M. L. (1996). J. Neurosci. 16, 6634-6647.
26. Peters, D., Christensen, J. K., Harpsøe, K. & Liljefors, T. (2007). International Patent WO 2007/060144 A2.
27. Pøhlsgaard, J., Frydenvang, K., Madsen, U. & Kastrup, J. S. (2011). Neuropharmacology, 60, 135-150.
28. Ptak, C. P., Ahmed, A. H. & Oswald, R. E. (2009). Biochemistry, 48, 8594-8602.
29. Sobolevsky, A. I., Rosconi, M. P. & Gouaux, E. (2009). Nature (London), 462, 745-756.
30. Sommer, B., Keinänen, K., Verdoorn, T. A., Wisden, W., Burnashev, N., Herb, A., Kö hler, M., Takagi, T., Sakmann, B. & Seeburg, P. H. (1990). Science, 249, 1580-1585.
31. Stern-Bach, Y., Russo, S., Neuman, M. & Rosenmund, C. (1998). Neuron, 21, 907-918.
32. Sun, Y., Olson, R., Horning, M., Armstrong, N.,Mayer,M. & Gouaux, E. (2002). Nature (London), 417, 245-253.
33. Suppiramaniam, V., Bahr, B. A., Sinnarajah, S., Owens, K., Rogers, G., Yilma, S. & Vodyanoy, V. (2001). Synapse, 40, 154-158.
34. Tang, C.-M., Shi, Q.-Y., Katchman, A. & Lynch, G. (1991). Science, 254, 288-290.
35. Tomita, S., Sekiguchi, M., Wada, K., Nicoll, R. A. & Bredt, D. S. (2006). Proc. Natl Acad. Sci. USA, 103, 10064-10067.
36. White, H. S., Sarup, A., Bolvig, T., Kristensen, A. S., Petersen, G., Nelson, N., Pickering, D. S., Larsson, O. M., Frølund, B., Krogsgaard-Larsen, P. & Schousboe, A. (2002). J. Pharmacol. Exp. Ther. 302, 636-644.
37. Winn, M. D. et al. (2011). Acta Cryst. D67, 235-242.
38. Yamada, K. A. & Rothman, S. M. (1992). J. Physiol. 458, 409-423.
39. Yamada, K. A. & Tang, C.-M. (1993). J. Neurosci. 13, 3904-3915.