Glutamine 57 at the complementary binding site face is a key determinant of morantel selectivity for α7 nicotinic receptors

Journal of Biological Chemistry

Volumn 284, Issue 32, 2009, Pages 21478-21487

  Bartos, Mariana ^a   Price, Kerry L ^b   Lummis, Sarah C R ^b   Bouzat, Cecilia ^a  

^a UNIVERSIDAD NACIONAL DEL SUR   (Argentina)

^b UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC GROUP; DRUG DESIGN; HIGH EFFICACY; HIGH SELECTIVITY; IN-SILICO; KEY DETERMINANTS; MAMMALIAN MUSCLES; MORANTEL; NICOTINIC RECEPTOR; REVERSE MUTATION; SYNAPTIC TRANSMISSION;

AMINO ACIDS; BINDING ENERGY; MAMMALS; MUSCLE;

BINDING SITES;

BUNGAROTOXIN RECEPTOR; GLUTAMINE; GLYCINE; MORANTEL; OXANTEL; SEROTONIN 3A RECEPTOR; TRYPTOPHAN;

ANIMAL CELL; ARTICLE; BINDING SITE; CHOLINERGIC STIMULATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SENSITIVITY; DRUG STRUCTURE; MOUSE; MUTATION; NONHUMAN; PRIORITY JOURNAL; REVERTANT; STRUCTURE ACTIVITY RELATION;

BINDING SITES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ELECTROPHYSIOLOGY; GLUTAMINE; HUMANS; MEMBRANE POTENTIALS; MODELS, BIOLOGICAL; MODELS, CHEMICAL; MORANTEL; MUSCLES; MUTAGENESIS, SITE-DIRECTED; MUTATION; PYRANTEL; RECEPTORS, NICOTINIC;

MAMMALIA;

EID: 69249109185     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M109.013797     Document Type: Article

References (36)

1. Lester, H. A., Dibas, M. I., Dahan, D. S., Leite, J. F., and Dougherty, D. A. (2004) Trends Neurosci. 27, 329-336
2. Sine, S. M., and Engel, A. G. (2006) Nature 440, 448-455
3. Sine, S. M. (2002) J. Neurobiol. 53, 431-446
4. Unwin, N. (2005) J. Mol. Biol. 346, 967-989
5. Brejc, K., van Dijk, W. J., Klaassen, R. V., Schuurmans, M., van Der Oost, J., Smit, A. B., and Sixma, T. K. (2001) Nature 411, 269-276
6. Changeux, J. P., and Taly, A. (2008) Trends Mol. Med. 14, 93-102
7. Bartos, M., Rayes, D., and Bouzat, C. (2006) Mol. Pharmacol. 70, 1307-1318
8. Martin, R. J. (1997) Vet. J. 154, 11-34
9. Rayes, D., De Rosa, M. J., Bartos, M., and Bouzat, C. (2004) J. Biol. Chem. 279, 36372-36381
10. Wu, T. Y., Smith, C. M., Sine, S. M., and Levandoski, M. M. (2008) Mol. Pharmacol. 74, 466-475
11. Levandoski, M. M., Piket, B., and Chang, J. (2003) Eur. J. Pharmacol. 471, 9-20
12. Kalamida, D., Poulas, K., Avramopoulou, V., Fostieri, E., Lagoumintzis, G., Lazaridis, K., Sideri, A., Zouridakis, M., and Tzartos, S. J. (2007) FEBS J. 274, 3799-3845
13. Eiselé, J. L., Bertrand, S., Galzi, J. L., Devillers-Thiéry, A., Changeux, J. P., and Bertrand, D. (1993) Nature 366, 479-483
14. Rayes, D., Spitzmaul, G., Sine, S. M., and Bouzat, C. (2005) Mol. Pharmacol. 68, 1475-1483
15. Kelley, S. P., Dunlop, J. I., Kirkness, E. F., Lambert, J. J., and Peters, J. A. (2003) Nature 424, 321-324
16. Williams, M. E., Burton, B., Urrutia, A., Shcherbatko, A., Chavez-Noriega, L. E., Cohen, C. J., and Aiyar, J. (2005) J. Biol. Chem. 280, 1257-1263
17. Bouzat, C., Bren, N., and Sine, S. M. (1994) Neuron 13, 1395-1402
18. Bouzat, C., Barrantes, F., and Sine, S. (2000) J. Gen. Physiol. 115, 663-672
19. Bouzat, C., Gumilar, F., del Carmen Esandi, M., and Sine, S. M. (2002) Biophys. J. 82, 1920-1929
20. Hamill, O. P., Marty, A., Neher, E., Sakmann, B., and Sigworth, F. J. (1981) Pflugers Arch. 391, 85-100
21. Bouzat, C., Gumilar, F., Spitzmaul, G., Wang, H. L., Rayes, D., Hansen, S. B., Taylor, P., and Sine, S. M. (2004) Nature 430, 896-900
22. Sigworth, F. J., and Sine, S. M. (1987) Biophys. J. 52, 1047-1054
23. Neher, E., and Steinbach, J. H. (1978) J. Physiol. 277, 153-176
24. Liu, Y., and Dilger, J. P. (1991) Biophys. J. 60, 424-432
25. Spitzmaul, G., Dilger, J. P., and Bouzat, C. (2001) Mol. Pharmacol. 60, 235-243
26. Shi, J., Blundell, T. L., and Mizuguchi, K. (2001) J. Mol. Biol. 310, 243-257
27. Sali, A., and Blundell, T. L. (1993) J. Mol. Biol. 234, 779-815
28. Lovell, S. C., Davis, I. W., Arendall, W. B., 3rd, de Bakker, P. I., Word, J. M., Prisant, M. G., Richardson, J. S., and Richardson, D. C. (2003) Proteins 50, 437-450
29. Bouzat, C., Bartos, M., Corradi, J., and Sine, S. M. (2008) J. Neurosci. 28, 7808-7819
30. Dougherty, D. A. (2008) Chem. Rev. 108, 1642-1653
31. Xiu, X., Puskar, N. L., Shanata, J. A., Lester, H. A., and Dougherty, D. A. (2009) Nature 458, 534-537
32. Rayes, D., De Rosa, M. J., Spitzmaul, G., and Bouzat, C. (2001) Neuropharmacology 41, 238-245
33. Rayes, D., Flamini, M., Hernando, G., and Bouzat, C. (2007) Mol. Pharmacol. 71, 1407-1415
34. Shimomura, M., Okuda, H., Matsuda, K., Komai, K., Akamatsu, M., and Sattelle, D. B. (2002) Br. J. Pharmacol. 137, 162-169
35. Zhong, W., Gallivan, J. P., Zhang, Y., Li, L., Lester, H. A., and Dougherty, D. A. (1998) Proc. Natl. Acad. Sci. U.S.A. 95, 12088-12093
36. Celie, P. H., van Rossum-Fikkert, S. E., van Dijk, W. J., Brejc, K., Smit, A. B., and Sixma, T. K. (2004) Neuron 41, 907-914