A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

Journal of Biological Chemistry

Volumn 287, Issue 1, 2012, Pages 650-659

  Canals, Meritxell ^a   Lane, J Robert ^a   Wen, Adriel ^a   Scammells, Peter J ^a   Sexton, Patrick M ^a   Christopoulos, Arthur ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ALLOSTERIC MODULATION; ALLOSTERIC MODULATORS; ALLOSTERIC PROPERTIES; CARBACHOL; CELLULAR PROPERTIES; CONSTITUTIVELY ACTIVES; COOPERATIVITY; COUPLING EFFICIENCY; DRUG TARGETS; G-PROTEIN COUPLED RECEPTORS; INACTIVE MUTANTS; INTRACELLULAR PATHWAYS; MUSCARINIC ACETYLCHOLINE RECEPTORS; QUINOLONES; STATE DEPENDENCE; TWO-STATE; YEAST STRAIN;

CARBOXYLIC ACIDS; GENETIC ENGINEERING; YEAST;

MODULATORS;

BENZYL QUINOLONE CARBOXYLIC ACID; CARBACHOL; CARBOXYLIC ACID; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; MITOGEN ACTIVATED PROTEIN KINASE 1; MUSCARINIC M1 RECEPTOR; MUSCARINIC RECEPTOR; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CALCIUM MOBILIZATION; CONTROLLED STUDY; COOPERATION; FUNGAL STRAIN; INVERSE AGONISM; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; RECEPTOR AFFINITY; SIGNAL TRANSDUCTION; STIMULUS RESPONSE;

ACETYLCHOLINE; ALLOSTERIC REGULATION; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG INVERSE AGONISM; HUMANS; LIGANDS; MODELS, BIOLOGICAL; MUTATION; QUINOLONES; RECEPTOR, MUSCARINIC M1; SIGNAL TRANSDUCTION;

EID: 84855290525     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M111.314278     Document Type: Article

References (41)

1. Monod, J., Wyman, J., and Changeux, J. P. (1965) J. Mol. Biol. 12, 88-118
2. Changeux, J. P., and Edelstein, S. J. (2005) Science 308, 1424-1428
3. Karlin, A. (1967) J. Theor. Biol. 16, 306-320
4. Leff, P. (1995) Trends Pharmacol. Sci. 16, 89-97
5. Canals, M., Sexton, P. M., and Christopoulos, A. (2011) Trends Biochem. Sci. 36, 663-672
6. Christopoulos, A. (2002) Nat. Rev. Drug Discov. 1, 198-210
7. Conn, P. J., Christopoulos, A., and Lindsley, C. W. (2009) Nat. Rev. Drug Discov. 8, 41-54
8. Hall, D. A. (2000) Mol. Pharmacol. 58, 1412-1423
9. Ma, L., Seager, M. A., Seager, M., Wittmann, M., Jacobson, M., Bickel, D., Burno, M., Jones, K., Graufelds, V. K., Xu, G., Pearson, M., McCampbell, A., Gaspar, R., Shughrue, P., Danziger, A., Regan, C., Flick, R., Pascarella, D., Garson, S., Doran, S., Kreatsoulas, C., Veng, L., Lindsley, C. W., Shipe, W., Kuduk, S., Sur, C., Kinney, G., Seabrook, G. R., and Ray, W. J. (2009) Proc. Natl. Acad. Sci. U. S. A. 106, 15950-15955
10. Shirey, J. K., Brady, A. E., Jones, P. J., Davis, A. A., Bridges, T. M., Kennedy, J. P., Jadhav, S. B., Menon, U. N., Xiang, Z., Watson, M. L., Christian, E. P., Doherty, J. J., Quirk, M. C., Snyder, D. H., Lah, J. J., Levey, A. I., Nicolle, M. M., Lindsley, C. W., and Conn, P. J. (2009) J. Neurosci. 29, 14271-14286
11. Avlani, V. A., Langmead, C. J., Guida, E., Wood, M. D., Tehan, B. G., Herdon, H. J., Watson, J. M., Sexton, P. M., and Christopoulos, A. (2010) Mol. Pharmacol. 78, 94-104
12. Scholten, D., Canals, M., Wijtmans, M., de Munnik, S., Nguyen, P., Verzijl, D., de Esch, I., Vischer, H., Smit, M., and Leurs, R. (2011) Br. J. Pharmacol., in press
13. Stewart, G. D., Sexton, P. M., and Christopoulos, A. (2010) ACS Chem. Biol. 5, 365-375
14. Ehlert, F. J. (1988) Mol. Pharmacol. 33, 187-194
15. Leach, K., Sexton, P. M., and Christopoulos, A. (2007) Trends Pharmacol. Sci. 28, 382-389
16. Giraldo, J. (2004) FEBS Lett. 556, 13-18
17. Christopoulos, A. (1998) Trends Pharmacol. Sci. 19, 351-357
18. Leach, K., Loiacono, R. E., Felder, C. C., McKinzie, D. L., Mogg, A., Shaw, D. B., Sexton, P. M., and Christopoulos, A. (2010) Neuropsychopharmacology 35, 855-869
19. Keov, P., Sexton, P. M., and Christopoulos, A. (2011) Neuropharmacology 60, 24-35
20. Thomas, R. L., Mistry, R., Langmead, C. J., Wood, M. D., and Challiss, R. A. J. (2008) J. Pharmacol. Exp. Ther. 327, 365-374
21. Ballesteros, J. A., and Weinstein, H. (1995) Methods Neurosci. 25, 366-428
22. Lu, Z. L., and Hulme, E. C. (1999) J. Biol. Chem. 274, 7309-7315
23. Armbruster, B. N., Li, X., Pausch, M. H., Herlitze, S., and Roth, B. L. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 5163-5168
24. Nawaratne, V., Leach, K., Suratman, N., Loiacono, R. E., Felder, C. C., Armbruster, B. N., Roth, B. L., Sexton, P. M., and Christopoulos, A. (2008) Mol. Pharmacol. 74, 1119-1131
25. Stallaert, W., Christopoulos, A., and Bouvier, M. (2011) Expert Opin. Drug Discov. 6, 811-825
26. Whalen, E. J., Rajagopal, S., and Lefkowitz, R. J. (2011) Trends Mol. Med. 17, 126-139
27. Yu, R. C., Pesce, C. G., Colman-Lerner, A., Lok, L., Pincus, D., Serra, E., Holl, M., Benjamin, K., Gordon, A., and Brent, R. (2008) Nature 456, 755-761
28. Gregory, K. J., Hall, N. E., Tobin, A. B., Sexton, P. M., and Christopoulos, A. (2010) J. Biol. Chem. 285, 7459-7474
29. Pertz, O., Hodgson, L., Klemke, R. L., and Hahn, K. M. (2006) Nature 440, 1069-1072
30. May, L. T., Leach, K., Sexton, P. M., and Christopoulos, A. (2007) Annu. Rev. Pharmacol. Toxicol. 47, 1-51
31. Shekhar, A., Potter, W. Z., Lightfoot, J., Lienemann, J., Dubé, S., Mallinckrodt, C., Bymaster, F. P., McKinzie, D. L., and Felder, C. C. (2008) Am. J. Psychiatry 165, 1033-1039
32. Klinkenberg, I., and Blokland, A. (2010) Neurosci. Biobehav. Rev. 34, 1307-1350
33. Valant, C., Aurelio, L., Urmaliya, V. B., White, P., Scammells, P. J., Sexton, P. M., and Christopoulos, A. (2010) Mol. Pharmacol. 78, 444-455
34. Wisler, J. W., DeWire, S. M., Whalen, E. J., Violin, J. D., Drake, M. T., Ahn, S., Shenoy, S. K., and Lefkowitz, R. J. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 16657-16662
35. Stockton, J. M., Birdsall, N. J., Burgen, A. S., and Hulme, E. C. (1983) Mol. Pharmacol. 23, 551-557
36. Tucek, S., Musílková, J., Nedoma, J., Proska, J., Shelkovnikov, S., and Vorlícek, J. (1990) Mol. Pharmacol. 38, 674-680
37. Lanzafame, A., Christopoulos, A., and Mitchelson, F. (1996) Eur. J. Pharmacol. 316, 27-32
38. Proska, J., and Tucek, S. (1994) Mol. Pharmacol. 45, 709-717
39. Avlani, V. A., Gregory, K. J., Morton, C. J., Parker, M. W., Sexton, P. M., and Christopoulos, A. (2007) J. Biol. Chem. 282, 25677-25686
40. Avlani, V., May, L. T., Sexton, P. M., and Christopoulos, A. (2004) J. Pharmacol. Exp. Ther. 308, 1062-1072
41. Murray, C. W., and Rees, D. C. (2009) Nat. Chem. 1, 187-192