Site-directed mutagenesis of the human β3-adrenoceptor - Transmembrane residues involved in ligan binding and signal transduction

European Journal of Biochemistry

Volumn 251, Issue 3, 1998, Pages 590-596

  Gros, Jérôme ^a   Manning, Brian S ^a   Pietri Rouxel, France ^a   Guillaume, Jean Luc ^a   Drumare, Marie Françoise ^a   Strosberg, A Donny ^a  

^a CNRS   (France)

Author keywords

Adrenoceptor; Mutagenesis; Transduction signal; 3

Indexed keywords

ADENYLATE CYCLASE; BETA 3 ADRENERGIC RECEPTOR;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CHO CELL; ENZYME ACTIVATION; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS;

EID: 0032006031     PISSN: 00142956     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1432-1327.1998.2510590.x     Document Type: Article

References (45)

1. 3-adrenergic receptor, Annu. Rev. Pharmacol. Toxicol. 37, 421-450.
2. Atgié, C., Tavernier, G., D'Allaire, F., Bengtsson, T., Marti, L., Carpene, C., Lafontan, M., Bukowiecki, L. J. & Langin, D. (1996) Low expression and absence of biological effect of beta3-adrenoceptor in guinea pig brown and white adipocytes, Am. J. Physiol. 271, R1729-R1738.
3. Strosberg, A. D. & Pietri-Rouxel, F. (1996) Function and regulation of the beta 3-adrenoceptor, Trends. Pharmacol. Sci. 17, 373-381.
4. 3 and atypical β-adrenoceptors. Med. Res. Rev. 13, 663-729.
5. Enocksson, S., Shimizu, M., Lonnqvist, F., Nordenstrom, J. & Arner, P. (1995) Demonstration of an in vivo functional beta 3-adrenoceptor in man, J. Clin. Invest. 95, 2239-2245.
6. Arch, J. R. & Wilson, S. (1996) Prospects for beta 3-adrenoceptor agonists in the treatment of obesity and diabetes, Int. J. Obes. Relat. Metab. Disord. 20, 191-199.
7. Sennitt, M. V., Young, P. W., Kirkham, D., Smith, S. A. & Cawthorne, M. A. (1994) Multiple lipolytic beta-adrenoceptor subtypes in human adipose tissue: demonstration of functional beta3-adrenoceptor using CGP 12177, Int. J. Obes. 18, 69P.
8. 3-adrenoceptors with low lipolytic action in human subcutaneous white adipocytes, J. Lip. Res. 37, 1-11.
9. Kadowaki, H., Yasuda, K., Iwamoto, K., Otabe, S., Shimokawa, K., Silver, K., Walston, J., Yoshinaga, H., Kosaka, K., Yamada, N., Saito, Y., Hagura, R., Akanuma, Y. Shuldiner, A., Yazaki, Y. & Kadowaki, T. (1945) A mutation in the beta 3-adrenergic receptor gene is associated with obesity and hyperinsulinemia in Japanese subjects, Biochem. Biophys. Res. Commun. 215, 555-560.
10. Clement, K., Vaisse, C., Manning, B. S., Basdevant, A., Guy, G. B., Ruiz, J., Silver, K. D., Shuldiner, A. R., Froguel, P. & Strosberg, A. D. (1995) Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity, N. Engl. J. Med. 33, 352-354.
11. De Ponti, F., Gibelli, G., Croci, T., Arcidiaco, M., Crema, F. & Manara, L. (1996) Functional evidence of atypical beta(3)-adrenoceptors in the human colon using the beta(3)-selective adrenoceptor antagonist, SR 59230A, Br. J. Pharmacol. 117, 1374-1376.
12. Berkowitz, D. E., Nardone, N. A., Smiley, R. M., Price, D. T., Kreutter, D. K., Fremeau, R. T. & Schwinn, D. A. (1995) Distribution of beta 3-adrenoceptor mRNA in human tissues, Eur. J. Pharmacol. 289, 223-228.
13. Krief, S., Lonnqvist, F., Raimbault, S., Baude, B., Van Spronsen, A., Arner, P., Strosberg, A. D., Ricquimer, D. & Emorine, L. J. (1993) Tissue distribution of beta 3-adrenergic receptor mRNA in man, J. Clin. Invest. 91, 344-349.
14. Gauthier, C., Tavernier, G., Charpentier, F., Langin, D. & Lemarec, H. (1996) Functional beta(3)-adrenoceptor in the human heart, J. Clin. Invest. 98, 556-562.
15. Kaumann, A. J. (1996) (-)-CGP 12177-induced increase of human atrial contraction through a putative third beta-adrenoceptor, Br. J. Pharmacol. 117, 93-98.
16. Guan, X. M., Amend, A. & Strader, C. D. (1995) Determination of structural domains for G protein coupling and ligand binding in beta 3-adrenergic receptor, Mol. Pharmacol. 48, 492-498.
17. 3-adrenergic receptor is resistant to short-term agonist-promoted desensitization, Mol. Pharmacol. 43, 548-555.
18. Jockers, R., Da Silva, A., Strosberg, A. D., Bouvier, M. & Marullo, S. (1996) New molecular and structural determinants involved in beta 2-adrenergic receptor desensitization and sequestration. Delineation using chimeric beta 3/beta 2-adrenergic receptors, J. Biol. Chem. 271, 9355-9362.
19. 3-Adrenoceptor Activity, Eur. J. Biochem. 247, 1174-1179.
20. Kunkel, T. A. (1985) Rapid and efficient site-specific mutagenesis without phenotypic selection, Proc. Natl Acad. Sci. USA 82, 488-492.
21. Zilberfarb, V., Pietri-Rouxel, F., Jockers, R., Krief, S., Delouis, C., Issad, T. & Strosberg, A. D. (1997) Human immortalized brown adipocytes express functional beta3-adrenoceptor coupled to lipolysis, J. Cell. Sci. 110, 801-807.
22. 3-adrenergic receptor, Eur. J. Biochem. 224, 761-770.
23. Cheng, Y. C. & Prusoff, W. H. (1973) Relationship between the inhibition constant (Ki) and the concentration of inhibitor (150) which causes an enzymatic reaction, Biochem. Pharmacol. 22, 3099-3108.
24. Blin, N., Camoin, L., Maigret, B. & Strosberg, A. D. (1993) Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor, Mol. Pharmacol. 44, 1094-1104.
25. Strosberg, A. D., Camoin, L., Blin, N. & Maigret, B. (1993) In receptors coupled to GTP-binding proteins, ligand binding and G-protein activation is a multistep dynamic process, Drug Des. Discov. 9, 199-211.
26. 3-adrenergic receptor: relationship with the atypical receptor of adipocytes, EMBO J. 10, 3721-3727.
27. Pietri-Rouxel, F. & Strosberg, A. D. (1995) Pharmacological characteristics and species-related variations of beta 3-adrenergic receptors, Fundam. Clin. Pharmacol. 9, 211-218.
28. Ho, B. Y., Karschin, A., Branchek, T., Davidson, N. & Lester, H. A. (1992) The role of conserved aspartate and serine residues in ligand binding and in function of the 5-HT(1A) receptor - a site-directed mutation study, FEBS Lett. 312, 259-262.
29. Zhang, D. & Weinstein, H. (1994) Polarity conserved positions in transmembrane domains of G-protein coupled receptors and bacteriorhodopsin, FEBS Lett. 337, 207-212.
30. Strader, C. D., Sigal, I. S., Candelore, M. R., Rands, E., Hill, W. S. & Dixon, R. A. F. (1987) Conserved aspartic acid residues 79 and 113 of the β-adrenergic receptor have different roles in receptor function, J. Biol. Chem. 263, 10267-10271.
31. Whaley, B. S., Yuan, N., Birnbaumer, L., Clark, R. B. & Barber, R. (1994) Differential expression of the beta-adrenergic receptor modifies agonist stimulation of adenylyl cyclase: a quantitative evaluation, Mol. Pharmacol. 45, 481-489.
32. Mizobe, T., Maze, M., Lam, V., Suryanarayana, S. & Kobilka, B. K. (1996) Arrangement of transmembrane domains in adrenergic receptors. Similarity to bacteriorhodopsin, J. Biol. Chem. 271, 2387-2389.
33. Zhou, W., Flanagan, C., Ballesteros, J. A., Konvicka, K., Davidson, J. S., Weinstein, H., Millar, R. P. & Sealfon, S. C. (1994) A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor, Mol. Pharmacol. 45, 165-170.
34. Strader, C. D., Sigal, I. S., Register, R. B., Candelore, M. R., Rands, K. & Dixon, R. A. F. (1987) Identification of residues required for ligand binding to the β-adrenergic receptor, Proc. Natl Acad. Sci. USA 84, 4384-4388.
35. Dixon, R. A. F., Sigal, I., Rands, E., Register, R. B., Candelore, M. R., Blake, A. D. & Strader, C. D. (1987) Ligand binding to the β-adrenergic receptor involves its rhodopsine-like core, Nature 326, 73-77.
36. Wang, C. D., Buck, M. A. & Fraser, C. M. (1991) Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists, Mol. Pharmacol. 40, 168-179.
37. Bluml, K., Mutschler, E. & Wess, J. (1994) Functional role in ligand binding and receptor activation of an asparagine residue present in the sixth transmembrane domain of all muscarinic acetylcholine receptors, J. Biol. Chem. 269, 18870-18876.
38. Hwa, J., Graham, R. M. & Perez, D. M. (1996) Chimeras of alpha1-adrenergic receptor subtypes identify critical residues that modulate active state isomerization, J. Biol. Chem. 271, 7956-7964.
39. Kim, J., Wess, J., Van Rhee, A. M., Schoneberg, T. & Jacobson, K. A. (1995) Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor, J. Biol. Chem. 270, 13987-13997.
40. Breu, V., Hashido, K., Broger, C., Miyamoto, C., Furuichi, Y., Hayes, A., Kalina, B., Loffler, B. M., Ramuz, H. & Clozel, M. (1995) Separable binding sites for the natural agonist endothelin-1 and the non-peptide antagonist bosentan on human endothelin-A receptors, Eur. J. Biochem. 231, 266-270.
41. Barak, L. S., Menard, L., Ferguson, S. S., Colapietro, A. M. & Caron, M. G. (1995) The conserved seven-transmembrane sequence NP(X)2,3Y of the G-protein-coupled receptor superfamily regulates multiple properties of the beta 2-adrenergic receptor. Biochemistry 34, 15407-15414.
42. Suryanarayana, S. & Kobilka, B. K. (1993) Amino acid substitutions at position 312 in the seventh hydrophohic segment of the beta 2-adrenergic receptor modify ligand-binding specificity, Mol. Pharmacol. 44, 111-114.
43. Wieland, K., Zuurmond, H., Krasel, C., Ijzerman, A. & Lohse, M. (1996) Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor, Proc. Natl Acad. Sci. USA 93, 9276-9281.
44. Chaudhry, A., MacKenzie, R. G., Georgie, L. M. & Granneman, J. G. (1994) Differential interaction of beta 1- and beta 3-adrenergic receptors with Gi in rat adipocytes, Cell Signal 6, 457-465.
45. Marullo, S., Emorine, L., Strosberg, A. D. & Delavier-Klutchko, C. (1990) Selective binding of ligands to β1, β2 or chimeric β1/β2-adrenergic receptors involves multiple subsites, EMBO J. 9, 1471-1476.