Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands

Journal of Biological Chemistry

Volumn 282, Issue 35, 2007, Pages 25677-25686

  Avlani, Vimesh A ^a   Gregory, Karen J ^a   Morton, Craig J ^b   Parker, Michael W ^b,c   Sexton, Patrick M ^a,d   Christopoulos, Arthur ^a,c,d  

^a MONASH UNIVERSITY   (Australia)

^b ST VINCENT'S INSTITUTE OF MEDICAL RESEARCH   (Australia)

^c National Health and Medical Research Council   (United States)

^d Australian Research Council

Author keywords

[No Author keywords available]

Indexed keywords

BINDING SITES; BIOASSAY; CELLS; DISSOCIATION; PROTEINS;

ALLOSTERIC MODULATORS; BINDING DYNAMICS; EXTRACELLULAR LOOPS; ORTHOSTERIC LIGANDS;

LIGANDS;

G PROTEIN COUPLED RECEPTOR; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; MUSCARINIC RECEPTOR; RHODOPSIN;

ALLOSTERISM; AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CRYSTAL STRUCTURE; DISSOCIATION; DISULFIDE BOND; LIGAND BINDING; MUTAGENESIS; NONHUMAN; PRIORITY JOURNAL; PROTEIN INTERACTION; RADIOASSAY;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; AMINO ACID SUBSTITUTION; ANIMALS; CATTLE; CYSTEINE; HUMANS; LIGANDS; MODELS, MOLECULAR; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, MUSCARINIC M2; RHODOPSIN; STRUCTURAL HOMOLOGY, PROTEIN;

BOVINAE; PYRONIA TITHONUS;

EID: 34548476934     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M702311200     Document Type: Article

References (27)

1. Kristiansen, K. (2004) Pharmacol. Ther. 103, 21-80
2. Palczewski, K., Kumasaka, T., Hori, T., Behnke, C. A., Motoshima, H., Fox, B. A., Le Trong, I., Teller, D. C., Okada, T., Stenkamp, R. E., Yamamoto, M., and Miyano, M. (2000) Science 289, 739-745
3. Lu, Z. L., Saldanha, J. W., and Hulme, E. C. (2002) Trends Pharmacol. Sci. 23, 140-146
4. Gether, U. (2000) Endocr. Rev. 21, 90-113
5. Neubig, R. R., Spedding, M., Kenakin, T., and Christopoulos, A. (2003) Pharmacol. Rev. 55, 597-606
6. Shi, L., and Javitch, J. A. (2004) Proc. Natl. Acad. Sci. U. S. A. 101, 440-445
7. Klco, J. M., Wiegand, C. B., Narzinski, K., and Baranski, T. J. (2005) Nat. Struct. Mol. Biol. 12, 320-326
8. Scarselli, M., Li, B., Kim, S. K., and Wess, J. (2007) J. Biol. Chem. 282, 7385-7396
9. Shi, L., and Javitch, J. A. (2002) Annu. Rev. Pharmacol. Toxicol. 42, 437-467
10. Christopoulos, A. (2002) Nat. Rev. Drug Discov. 1, 198-210
11. Christopoulos, A., and Kenakin, T. (2002) Pharmacol. Rev. 54, 323-374
12. May, L. T., Leach, K., Sexton, P. M., and Christopoulos, A. (2007) Annu. Rev. Pharmacol. Toxicol. 47, 1-51
13. Gnagey, A. L., Seidenberg, M., and Ellis, J. (1999) Mol. Pharmacol. 56, 1245-1253
14. Leppik, R. A., Miller, R. C., Eck, M., and Paquet, J. L. (1994) Mol. Pharmacol. 45, 983-990
15. Voigtlander, U., Johren, K., Mohr, M., Raasch, A., Trankle, C., Buller, S., Ellis, J., Holtje, H. D., and Mohr, K. (2003) Mol. Pharmacol. 64, 21-31
16. Guex, N., and Peitsch, M. C. (1997) Electrophoresis 18, 2714-2723
17. Johren, K., and Holtje, H. D. (2002) J. Comput. Aided Mol. Des. 16, 795-801
18. Morris, G. M., Goodsell, D. S., Halliday, R. S., Huey, R., Hart, W. W., Belew, R. K., and Olson, A. J. (1998) J. Comput. Chem. 19, 1639-1662
19. Avlani, V. A., May, L. T., Sexton, P. M., and Christopoulos, A. (2004) J. Pharmacol. Exp. Ther. 308, 1062-1072
20. Lazareno, S., and Birdsall, N. J. M. (1995) Mol. Pharmacol. 48, 362-378
21. Yan, F., Mosier, P. D., Westkaemper, R. B., Stewart, J., Zjawiony, J. K., Vortherms, T. A., Sheffler, D. J., and Roth, B. L. (2005) Biochemistry 44, 8643-8651
22. Christopoulos, A., and El-Fakahany, E. E. (1999) Biochem. Pharmacol. 58, 735-748
23. Lanzafame, A., Christopoulos, A., and Mitchelson, F. (1997) J. Pharmacol. Exp. Ther. 282, 278-285
24. Christopoulos, A., Lanzafame, A., and Mitchelson, F. (1998) Clin. Exp. Pharmacol. Physiol. 25, 184-194
25. Matsui, H., Lazareno, S., and Birdsall, N. J. (1995) Mol. Pharmacol. 47, 88-98
26. Ray, K., and Northup, J. (2002) J. Biol. Chem. 277, 18908-18913
27. Lee, B., Sharron, M., Blanpain, C., Doranz, B. J., Vakili, J., Setoh, P., Berg, E., Liu, G., Guy, H. R., Durell, S. R., Parmentier, M., Chang, C. N., Price, K., Tsang, M., and Doms, R. W. (1999) J. Biol. Chem. 274, 9617-9626