Changes in the carboxyl-terminal domain of metabotropic glutamate receptor 1 by alternative splicing generate receptors with differing agonist-independent activity

Molecular Pharmacology

Volumn 49, Issue 3, 1996, Pages 422-429

  Prézeau, Laurent ^a   Gomeza, Jesús ^a   Ahern, Shawn ^a,b   Mary, Sophie ^a   Galvez, Thierry ^a   Bockaert, Joel ^a   Pin, Jean Philippe ^a  

^a CCIPE   (France)

^b UNIVERSITY OF WISCONSIN MADISON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GLUTAMATE RECEPTOR; GLUTAMATE RECEPTOR AGONIST; GLUTAMATE RECEPTOR ANTAGONIST; GLUTAMIC ACID; GUANINE NUCLEOTIDE BINDING PROTEIN; INOSITOL PHOSPHATE; METABOTROPIC RECEPTOR; PHOSPHOLIPASE C;

ANIMAL CELL; ARTICLE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFECT; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN DETERMINATION; PROTEIN EXPRESSION; RECEPTOR BLOCKING;

ALTERNATIVE SPLICING; ANIMALS; GTP-BINDING PROTEINS; ISOMERISM; LLC-PK1 CELLS; PHOSPHOLIPASE C; RECEPTORS, METABOTROPIC GLUTAMATE; SWINE;

EID: 0029963929     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (55)

1. Bettler, B., and C. Mulle. AMPA and kainate receptors. Neuropharmacology 34:123-139 (1995).
2. Pin, J.-P., and J. Bockaert. Get receptive to metabotropic glutamate receptors. Curr. Opin. Neurol. 5:342-349 (1995).
3. Pin, J.-P., and R. Duvoisin. The metabotropic glutamate receptors: structure and functions. Neuropharmacology 34:1-26 (1995).
4. Savarese, T. M., and C. M. Fraser: In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors. Biochem. J. 283:1-19 (1992).
5. 2-adrenoceptor that blocks coupling to potassium but not calcium currents. Science (Washington D. C.) 257:977-980 (1992).
6. Zhou, W , C. Flanagan, J. A. Ballesteros, K. Konvicka, J. S. Davidson, H. Weinstein, R P Millar, and S. C. Sealfon. A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-reieasing hormone receptor. Mol. Pharmacol. 45:165-170 (1994).
7. Trumpp-Kallmeyer, S., J. Hoflack, A. Bruinvels, and M. Hibert. Modeling of G protein-coupled receptors' application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors. J. Med Chem. 35: 3448-3462 (1992).
8. Pin, J.-P., C. Joly, S. F. Heinemann, and J. Bockaert. Domains involved in the specificity of G protein activation in phospholipase C coupled metabotropic glutamate receptor. EMBO J 13:342-348 (1994).
9. Pin, J.-P., J. Gomeza, C. Joly, and J. Bockaert. The metabotropic glutamate receptors: their second intracellular loop plays a critical role in the G protein coupling specificity. Biochem. Soc. Trans. 23:91-96 (1995).
10. Takahashi, K., K. Tsuchida, Y. Tanabe, M. Masu, and S. Nakanishi. Role of the large extracellular domain of metabotropic glutamate receptors in agonist selectivity determination. J. Biol. Chem. 268:19341-19345 (1993).
11. O'Hara, P. J., P. O. Sheppard, H. Thøgersen, D Venezia, B. A. Haldeman, V. McGrane, K. M. Houamed, C. Thomsen, T. L. Gilbert, and E R. Mulvihill. The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins. Neuron 11:41-52 (1993).
12. Kjelsberg, M. A., S Cotecchia, J. Ostrowski, M. G. Caron, and R. J. Lefkowitz. Constitutive activation of the α1B-adrenergic receptor by all amino acid substitutions at a single site: evidence for a region which constrains receptor activation. J. Biol. Chem. 267:1430-1433 (1992).
13. Robinson, P. R., G. B. Cohen, E. A. Zhukovsky, and D. D. Oprian. Constitutively active mutants of rhodopsin. Neuron 9:719-725 (1992).
14. Ren, Q., H. Kurose, R. J. Lefkowitz, and S. Cotecchia. Constitutively active mutants of the α2-adrenergic receptor. J. Biol. Chem. 268:16483-16487 (1993).
15. Samama, P., S. Cotecchia, T. Costa, and R. J. Lefkowitz. A mutation-induced activated state of the β2-adrenergic receptor. J. Biol. Chem. 268: 4625-4636 (1993).
16. Shenker, A., L. Laue, S. Kosugl, J. Merendlno, Jr., T. Mineglshi, and G. Cutler, Jr. A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty. Nature (Lond.) 365:652-654 (1993).
17. Parma, J., L. Duprez, J. Van Sande, P. Cochaux, C. Gervy, J. Mockel, J. Dumont, and G. Vassart. Somatic mutations in the thyrotropin gene cause hyperfunctioning thyroid adenomas. Nature (Lond.) 365:649-651 (1993).
18. Robbins, L. S., J. H. Nadeau, K. R. Johnson, M. A. Kelly, L. Roselli-Rehfuss, E. Baack, K. G. Mountjoy, and R. D. Cone. Pigmentation phenotypes of a variant extension locus alleles result from point mutations that alter MSH receptor function. Cell 72:827-834 (1993).
19. 2+-sensing receptor gene mutation. Nat. Genet. 8:303-307 (1994).
20. Tiberi, M., and M. G. Caron. High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype. J. Biol. Chem. 269:27925-27931 (1994).
21. Costa, T., and A. Hertz. Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86:7321-7325 (1989).
22. Barker, E. L., R. S. Westphal, D. Schmidt, and E. Sanders-Bush. Constitutive active 5-hydroxytryptamine 2c receptors reveal novel inverse agonist activity of receptor ligands. J. Biol. Chem. 269:11687-11690 (1994).
23. 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state. Mol. Pharmacol. 45:524-531 (1994).
24. 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).
25. 2-adrenergic receptor. Mol. Pharmacol. 45:390-394 (1994).
26. Costa, T., Y. Ogino, P. J. Munson, H. O. Onaran, and D. Rodbard. Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand. Mol. Pharmacol. 41:549-560 (1991)
27. 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 β2-adrenoceptor. Nature (Lond.) 374:272-276 (1995).
28. Hilf, G., and K. H. Jakobs. Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes. Eur. J. Pharmacol. 225:245-252 (1992).
29. + currents in frog and rat cardiac cells J. Physiol. (Lond.) 461:743-765 (1993).
30. Murray, R., and A. K. Keenan. The β-adrenoceptor is precoupled to Gs in chicken erythrocyte membranes. Cell Signalling 1:173-179 (1989)
31. Mewes, T., S. Dutz, U. Ravens, and K. H. Jakobs. Activation of calcium currents in cardiac myocytes by empty β-adrenoceptors. Circulation 88: 2916-2922 (1993).
32. Gotze, K., and K. H. Jakobs. Unoccupied β-adrenoceptor-induced adenylyl cyclase stimulation in turkey erythrocyte membranes. Eur. J. Pharmacol. 268:151-158 (1994).
33. 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. 269:25970-25978 (1994)
34. Lefkowitz, R. J., S. Cotecchia, P. Samama, and T. Costa. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol. Sci. 14:303-307 (1993).
35. Leff, P The two-state model of receptor activation. Trends Pharmacol. Sci. 16:89-97 (1995).
36. Pin, J -P., C. Waeber, L. Prézeau, J. Bockaert, and S. F. Heinemann. Alternative splicing generates metabotropic glutamate receptors inducing different patterns of calcium release in Xenopus oocytes. Proc. Natl. Acad. Sci. USA 89:10331-10335 (1992).
37. Joly, C., J. Gomeza, I. Brabet, K. Curry, J. Bockaert, and J.-P. Pin. Molecular, functional and pharmacological characterization of the metabotropic glutamate receptor type 5 splice variants: comparison with mGluR1. J. Neurosci. 15:3970-3981 (1995).
38. Eaton, D. L , W. I. Wood, D. Eaton, P. E. Hass, P. Hollingshead, K. Wion, J. Mather, R. M. Lawn, G. A. Vehar, and C. Gorman. Construction and characterization of an active factor VIII variant lacking the central one-third of the molecule. Biochemistry 25:8343-8347 (1986).
39. 2+ mobilizing hormones. Biochem. J. 212:733-743 (1983).
40. Pin, J.-P., S. Weiss, M. Sebben, D. Kemp, and J Bockaert. Release of endogenous amino acids from striatal neurones in primary culture. J. Neurochem. 47:594-603 (1986).
41. Conquet, F., Z. I. Bashir, C. H. Davies, H. Daniel, F. Ferraguti, F. Bordi, K. Franz-Bacon, A. Reggiani, V. Matarese, F. Condé. G. L. Colingridge, and F. Crépel. Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1. Nature (Lond.) 372:237-243 (1994).
42. Thomsen, C., A. Bau, P. Faarup, C. Foged, A. Kanstrup, and P. D. Suzdak, Effects of bromohomoibotenate on metabotropic glutamate receptors. NeuroReport 5:2417-2420 (1994).
43. Tellier, F., F. Acher, I. Brabet, J.-P Pin, J. Bockaert, and R. Azerad. Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptors. Bioorg. Med. Chem. Lett. 5:2627-2632 (1995).
44. Pickering, D. S., C. Thomsen, P. D. Suzdak, E. J. Fletcher, R. Robitaille, M. W. Salter, J. F. MacDonald, X. Huang, and D. R. Hampson. A comparison of two alternatively spliced forms of a metabotropic glutamate receptor coupled to phosphoinositides turnover. J. Neurochem. 61:85-92 (1993).
45. Aramori, I., and S. Nakanishi. Signal transduction and pharmacological characteristics of a metabotropic glutamate receptor, mGluR1, in transfected CHO cells. Neuron 8:757-765 (1992).
46. Kunkel, M. T., and E. G. Peralta. Charged amino acids required for signal transduction by the m3 muscarinic acetylcholine receptor. EMBO J. 12: 3809-3815 (1993).
47. Okamoto, T., Y. Murayama, Y. Hayashi, M. Inagaki, E. Ogata, and I. Nishimoto. Identification of a Gs activator region of the β2-adrenergic receptor that is autoregulated via protein kinase A-dependent phosphorylation. Cell 67:723-730 (1991).
48. Palm, D., G. Munch, C. Dees, and M. Hekman. Mapping of β-adrenoceptor coupling domains to Gs-protein by site-specific synthetic peptides. FEBS Lett. 254:89-93 (1989).
49. Okamoto, T., and I. Nishimoto. Detection of G protein-activator regions in M4 subtype muscarinic, cholinergic, and α2-adrenergic receptors based upon characteristics in primary structure. J Biol. Chem. 267:8342-8346 (1992).
50. Cheung, A. H., R.-R. C. Huang, M. P. Graziano, and C. D. Strader. Specific activation of Gs by synthetic peptides corresponding to an intracellular loop of the β-adrenergic receptor. FEBS Lett. 279:277-280 (1991).
51. Varrault, A., D. Le Nguyen, S. McClue, B. Harris, P. Jouin, and J. Bockaert. 5-Hydroxytryptamine1A receptor synthetic peptides: mechanisms of adenylyl cyclase inhibition. J. Biol. Chem. 269:16720-16725 (1994).
52. Martin, L. J., C. D. Blackstone, R. L. Huganir, and D. L. Price. Cellular localization of a metabotropic glutamate receptor in rat brain. Neuron 9:259-270 (1992).
53. Fotuhi, M., A. H. Sharp, C. E. Glatt, P. M. Hwang, M. Von Krosigk, S. H. Snyder, and T. M. Dawson. Differential localization of phosphoinositide-linked metabotropic glutamate receptor (mGluR1) and the inositol 1,4,5-triphosphate receptor in rat brain J. Neurosci. 13:2001-2012 (1993).
54. Baude, A., Z. Nusser, J. D. B. Roberts, E. Mulvihill, R. A. J. McIlhinney, and P. Somogyi. The metabotropic glutamate receptor (mGluR1α) is concentrated at perisynaptic membrane of neuronal subpopulations as detected by immunogold reaction. Neuron 11:771-787 (1993).
55. Romano, C., M. A. Sesma, C. MacDonald, K. O'Malley, A. N. van den Pol, and J. W. Olney. Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain. J. Comp. Neurol. 355:455-469 (1995).