Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: A molecular basis for agonist-directed trafficking of receptor stimulus

Molecular Pharmacology

Volumn 64, Issue 2, 2003, Pages 421-429

  Skrzydelski, Delphine ^a   Lhiaubet, Anne Marie ^a   Lebeau, Antony ^a   Forgez, Patricia ^a   Yamada, Misa ^a,c   Hermans, Emmanuel ^b   Rostene, William ^a   Pelaprat, Didier ^a  

^a HÔPITAL SAINT ANTOINE   (France)

^b UNIVERSITÉ CATHOLIQUE DE LOUVAIN   (Belgium)

^c SHOWA UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ARACHIDONIC ACID; ARGINYLLYSYLPROLYLTRYPTOPHANYL TERT LEUCYLLEUCYLETHOXYMETHYL ESTER; CARBOXYL GROUP; CYCLIC AMP; EISAI 1; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); INOSITOL 1,4,5 TRISPHOSPHATE; NEUROMEDIN N; NEUROTENSIN RECEPTOR; NEUROTENSIN RECEPTOR 1; NEUROTENSIN RECEPTOR STIMULATING AGENT; STIMULATORY GUANINE NUCLEOTIDE BINDING PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BRAIN CELL; CARBOXY TERMINAL SEQUENCE; CHO CELL; CONTROLLED STUDY; DRUG POTENCY; GENE DELETION; GENETIC TRANSFECTION; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN EXPRESSION; RAT;

ANIMALS; ARACHIDONIC ACID; CHO CELLS; CRICETINAE; CYCLIC AMP; GTP-BINDING PROTEINS; OLIGOPEPTIDES; PHOSPHOTRANSFERASES (ALCOHOL GROUP ACCEPTOR); PROTEIN STRUCTURE, TERTIARY; RATS; RECEPTORS, NEUROTENSIN; TRITIUM;

EID: 0041341923     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.64.2.421     Document Type: Article

References (38)

1. Barroso S, Richard F, Nicolas-Ethève D, Reversat JL, Bernassau JM, Kitabgi P, and Labbé-Jullié C (2000) Identification of residues involved in neurotensin binding and modeling of the agonist binding site in neurotensin receptor 1. J Biol Chem 275:328-336.
2. Berg KA, Maayani S, Goldfarb J, Scaramellini C, Leff P, and Clarke WP (1998) Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus. Mol Pharmacol 54:94-104.
3. Berod A and Rostene W (2002) Neurotensin: an endogenous psychostimulant? Curr Opin Pharmacol 2:93-98.
4. Boudin H, Gruaz-Guyon A, Faure MP, Forgez P, Lhiaubet AM, Dennis M, Beaudet A, Rostene W, and Pelaprat D (1995) Immunological recognition of different forms of the neurotensin receptor in transfected cells and rat brain. Biochem J 305:277-283.
5. s. J Pharmacol Exp Ther 294:539-547.
6. 2c receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking. Mol Pharmacol 62:578-589.
7. Doulut S, Rodriguez M, Lugrin D, Vecchini F, Kitabgi P, Aumelas A, and Martinez J (1992) Reduced peptide bond pseudopeptide analogues of neurotensin. Peptide Res 5:30-38.
8. Gailly P, Najimi M, and Hermans E (2000) Evidence for the dual coupling of the rat neurotensin receptor with pertussis toxin sensitive and insensitive G-proteins. FEBS Lett 483:109-113.
9. 1α receptors on the pharmacological properties of agonists and antagonists. Br J Pharmacol 126:873-882.
10. Hermans E and Maloteaux JM (1998) Mechanisms of regulation of neurotensin receptor. Pharmacol Ther 79:89-104.
11. Hermans E, Octave JN, and Maloteaux JM (1996) Interaction of the COOH-terminal domain of the neurotensin receptor with a G protein does not control the phospholipase C activation but is involved in the agonist-induced internalization. Mol Pharmacol 49:365-372.
12. Hillairet de Boisferon M, Raguin O, Thiercelin C, Dussaillant M, Rostene W, Barbet J, Pelegrin A, and Gruaz-Guyon A (2002) Improved tumor selectivity of radiolabeled peptides by receptor and antigen dual targeting in the neurotensin receptor model. Bioconjug Chem 13:654-662.
13. Ishizuka J, Townsend CM, and Thompson JC (1993) Neurotensin regulates growth of human pancreatic cancer. Ann Surg 217:439-446.
14. Kaskow J and Nemeroff CB (1991) The neurobiology of neurotensin: focus on neurotensin-dopamine interactions. Regul Pept 36:153-164.
15. Kenakin T (1995) Agonist-receptor efficacy II: agonist trafficking of receptor signals. Trends Pharmacol Sci 16:232-238.
16. Kenakin T (1996) The classification of seven transmembrane receptors in recombinant expression systems. Pharmacol Rev 48:413-463.
17. Kenakin T (2001) Inverse, protean and ligand-selective agonism: matters of receptor conformation. FASEB J 15:598-611.
18. Kenakin T and Onaran O (2002) The ligand paradox between affinity and efficacy: can you be there and not make a difference? Trends Pharmacol Sci 23:275-280.
19. Kinkead B and Nemeroff CB (2002) Neurotensin: an endogenous antipsychotic? Curr Opin Pharmacol 2:99-103.
20. Kitabgi P (2002) Targeting neurotensin receptors with agonists and antagonists for therapeutic purposes. Curr Opin Drug Discov Dev 5:764-776.
21. Lépée-Lorgeoux I, Betancur C, Souazé F, Rostène W, Bérod A, and Pélaprat D (2000) Regulation of the neurotensin NT1 receptor in the developing rat brain following chronic treatment with the antagonist SR 48692. J Neurosci Res 60:362-369.
22. Machida R, Tokumura T, Tsuchiya Y, Sasaki A, and Abe K (1993) Pharmacokinetics of novel hexapeptides with neurotensin activity in rats. Biol Pharm Bull 16:43-47.
23. Manning DR (2002) Measures of efficacy using G proteins as endpoints: differential engagement of G proteins through single receptors. Mol Pharmacol 62:451-452.
24. Martin S, Vincent JP, and Mazella J (2003) Involvement of the neurotensin receptor-3 in the neurotensin-induced migration of human microglia. J Neurosci 23:1198-1205.
25. Mazella J (2001) Sortilin/neurotensin receptor-3: a new tool to investigate neurotensin signaling and cellular trafficking? Cell Signalling 13:1-6.
26. Munson PJ and Rodbard D (1980) Ligand: a versatile computerized approach for characterization of ligand binding systems. Anal Biochem 107:220-226.
27. Najimi M, Gailly P, Maloteaux JM, and Hermans E (2002) Distinct regions of the high affinity neurotensin receptor mediate the functional coupling with pertussis toxin sensitive and insensitive G-proteins. FEBS Lett 512:329-333.
28. Perez DM, Hwa J, Gaivin R, Mathur M, Brown F, and Graham RM (1996) Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor. Mol Pharmacol 49:112-122.
29. Reubi JC, Waser B, Schaer JC, and Laissue JA (1999) Neurotensin receptors in human neoplasms: high incidence in Ewing's sarcomas. Int J Cancer 82:213-218.
30. Robb S, Cheek T, Harman FL, Hall L, Midgley JM, and Eveans PD (1994) Agonist-specific coupling of a cloned Drosophila octopamine/tyramine receptor to multiple second messenger systems. EMBO (Eur Mol Biol Organ) J 13:1325-1330.
31. Rostene W and Alexander MJ (1997) Neurotensin and neuroendocrine regulation. Front Neuroendocrinol 18:115-173.
32. Sadoul JL, Mazella J, Amar S, Kitabgi P, and Vincent JP (1984) Preparation of neurotensin selectively iodinated on the tyrosine 3 residue. Biological activity and binding properties on mammalian neurotensin receptors. Biochem Biophys Res Commun 120:812-819.
33. 11] SP analogues. J Biol Chem 274:23770-23776.
34. Spengler D, Waeber C, Pantoloni C, Holsboer F, Bockaert J, Seeburg PH, and Journot L (1993) Differential signal transduction by five splice variants of the PACAP receptor. Nature (Lond) 365:170-175.
35. Vincent JP, Mazella J, and Kitabgi P (1999) Neurotensin and the neurotensin receptors. Trends Pharmacol Sci 20:302-309.
36. q-proteins. Mol Pharmacol 58:954-966.
37. Yamada M, Yamada M, Watson MA, and Richelson E (1994) Deletion mutation in the putative third intracellular loop of the rat neurotensin receptor abolishes polyphosphoinositide hydrolysis but not cyclic AMP formation in CHO-K1 cells. Mol Pharmacol 46:470-476.
38. Yamada M, Yamada M, Watson MA, and Richelson E (1993) Neurotensin stimulates cyclic AMP formation in CHO-rNTR-10 cells expressing the cloned rat neurotensin receptor. Eur J Pharmacol 244:99-101.