Agonist-induced modulation of inverse agonist efficacy at the β2- adrenergic receptor

Molecular Pharmacology

Volumn 50, Issue 3, 1996, Pages 662-669

  Chidiac, Peter ^a,b   Nouet, Sandrine ^a   Bouvier, Michel ^a  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; BETA 2 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR STIMULATING AGENT; GUANINE NUCLEOTIDE BINDING PROTEIN;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DESENSITIZATION; DRUG EFFICACY; DRUG RECEPTOR BINDING; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

ADENYLATE CYCLASE; ADRENERGIC BETA-AGONISTS; ADRENERGIC BETA-ANTAGONISTS; ANIMALS; CELL LINE; CELL MEMBRANE; GENES, MYC; GTP-BINDING PROTEINS; HUMANS; KINETICS; LIGANDS; RECEPTORS, ADRENERGIC, BETA-2; RECOMBINANT PROTEINS; SPODOPTERA; STRUCTURE-ACTIVITY RELATIONSHIP; TIMOLOL; TRANSFECTION;

EID: 0029787046     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (27)

1. Costa, T., and A. Herz. Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86:7321-7325 (1989).
2. Chidiac, P., T. E. Hebert, M. Valiquette, M. Dennis, and M. Bouvier. Inverse agonist activity of β-adrenergic antagonists. Mol. Pharmacol. 45: 490-499 (1994).
3. Leeb-Lundberg, L. M. F., S. A. Mathis, and M. C. S. Herzig. Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells. J. Biol. Chem. 269:25970-25973 (1994).
4. Westphal, R., and E. Sanders-Bush. Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol. Pharmacol. 46:937-942 (1994).
5. 2c receptor in Sf9 cells. Mol. Pharmacol. 48:150-159 (1995).
6. 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state. Mol. Pharmacol. 45:524-531 (1994).
7. Kenakin, T. Pharmacologic Analysis of Drug-Receptor Interaction. Raven Press, New York (1993).
8. Ehlert, F. J., W. R. Roeske, K. W. Gee, and H. I. Yamamura. An allosteric model for benzodiazepine receptor function. Biochem. Pharmacol. 32: 2375-2383 (1983).
9. Leff, P. The two-state model of receptor activation. Trends Pharmacol. Sci. 16:89-97 (1995).
10. Benovic, J. L., M. Bouvier, M. G. Caron, and R. J. Lefkowitz. Regulation of adenylyl cyclase-coupled β-adrenergic receptors. Annu. Rev. Cell. Biol. 4:405-427 (1988).
11. Hausdorff, W. P., M. G. Caron, and R. J. Lefkowitz. Turning off the signal: desensitization of β-adrenergic receptor function. FASEB J. 4:2881-2889 (1990).
12. 2-adrenergic receptor in Sf9 cells. J. Biol. Chem. 267:21733-21737 (1992).
13. Bradford, M. M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72:248-254 (1976).
14. Salomon, Y., C. Londos, and M. Rodbell. A highly sensitive adenylate cyclase assay. Anal. Biochem. 58:541-548 (1974).
15. 2-adrenergic receptor. J. Biol. Chem. 268: 4625-4636 (1993).
16. Perlman, S., H. T. Schambye, R. A. Rivero, W. J. Greenlee, S. A. Hjorth, and T. W. Schwartz Non-peptide angiotensin agonist. J. Biol. Chem. 270:1493-1496 (1995).
17. Waller, D. G. β-Adrenoceptor partial agonists: a renaissance in cardiovascular therapy? Br. J. Clin. Pharmacol. 30:157-171 (1990).
18. McDevitt, D. G. Pharmacological characteristics of β blockers and their role in clinical practice. J. Cardiovasc. Pharm. 8 (Suppl. 6):S5-S11 (1986).
19. Cerione, R. A., J. Codina, J. L. Benovic, R. J. Lefkowitz, L. Birnbaumer, and M. G. Caron. The mammalian β2-adrenergic receptor: reconstitution of functional interactions between pure receptor and pure stimulatory nucleotide binding protein of the adenylate cyclase system. Biochemistry 23:4519-4525 (1984).
20. Gotze, K., and K. H. Jakobs. Unoccupied β-adrenoceptor-induced adenylyl cyclase stimulation in turkey erythrocyte membranes. Eur. J. Pharmacol. 268:151-158 (1994).
21. 2-adrenergic receptor lacking the palmitoylated Cys341. EMBO J. 12:349-356 (1993).
22. Katz, B., and S. Thesleff. A study of the "desensitization" produced by acetylcholine at the motor end-plate. J. Physiol. 138:63-80 (1957).
23. Gero, A. Desensitization, two-state receptors, and pharmacological parameters. J. Theor. Biol. 103:137-161 (1983).
24. Sibley, D. R., R. H. Strasser, J. L. Benovic, K. Daniel, and R. J. Lefkowitz. Phosphorylation/dephosphorylation of the β-adrenergic receptor regulates its functional coupling to adenylate cyclase and subcellular distribution. Proc. Natl. Acad. Sci. USA 83:9408-9412 (1986).
25. Yu, S. S., R. J. Lefkowitz, and W. P. Hausdorff. β-Adrenergic receptor sequestration: a potential mechanism for receptor resensitization. J. Biol. Chem. 268:337-341 (1993).
26. Bond, R. A., P. Leff, T. D. Johnson, C. A. Milano, H. A. Rockman, T. R. McMinn, S. Apparsundaram, M. F. Hyek, T. P. Kenakin, L. F. Allen, and R. J. Lefkowitz. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor. Nature (Lond.) 374:272-276 (1995).
27. Pei, G., P. Samama, M. Lohse, M. Wang, J. Codina, and R. J. Lefkowitz. A constitutively active mutant beta 2-adrenergic receptor is constitutively desensitized and phosphorylated. Proc. Natl. Acad. Sci. USA 91:2699-2702 (1994).