Binding sites and transduction process of the cholecystokinin(B) receptor: Involvement of highly conserved aromatic residues of the transmembrane domains evidenced by site-directed mutagenesis

Molecular Pharmacology

Volumn 53, Issue 5, 1998, Pages 878-885

  Jagerschmidt, Alexandre ^a,b   Guillaume, Nathalie ^a   Roques, Bernard P ^a   Noble, Florence ^a  

^a INSERM   (France)

^b Laboratoire de Pharmacochimie   (France)

Author keywords

[No Author keywords available]

Indexed keywords

1 (2,3 DIHYDRO 1 METHYL 2 OXO 5 PHENYL 1H 1,4 BENZODIAZEPIN 3 YL) 3 (3 METHYLPHENYL)UREA; 4 [[2 [2 [[(2 ADAMANTYLOXY)CARBONYL]AMINO] 3 (1H INDOL 3 YL) 2 METHYLPROPIONAMIDO] 1 PHENYLETHYL]AMINO] 4 OXOBUTYRIC ACID MEGLUMINE; CHOLECYSTOKININ; CHOLECYSTOKININ B RECEPTOR; DEVAZEPIDE; INOSITOL PHOSPHATE; PHOSPHATIDYLINOSITIDE;

AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; GENETIC TRANSFECTION; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; COS CELLS; HUMANS; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PHOSPHATIDYLINOSITOLS; RADIOLIGAND ASSAY; RATS; RECEPTOR, CHOLECYSTOKININ B; RECEPTORS, CHOLECYSTOKININ; SEQUENCE HOMOLOGY, AMINO ACID; SIGNAL TRANSDUCTION;

EID: 0031780615     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Befort K, Tabbara L, Kling D, Maigret B, and Kieffer BL (1996) Role of aromatic transmembrane residues of the δ-opioid receptor in ligand recognition. J Biol Chem 271:10161-10168.
2. Beinborn M, Lee YM, McBride EW, Quinn SM, and Kopin AS (1993) A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non peptides antagonists. Nature (Lond) 362:348-350.
3. Bradwejn J, Koszicki D, Dutertre AC, Megen HV, Boer JD, Westenberg H, Karkanias C, and Haigh J (1992) L-365,260, a CCK-B antagonist, blocks CCK-4-panic disorder. Clin Pharmacol 15, Suppl. 1:5.
4. Charpentier B, Durieux C, Pélaprat D, Dor A, Reibaud M, Blanchard JC, and Roques BP (1988) Enzyme-resistant CCK analogs with high affinities for central receptors. Peptides 9:835-841.
5. Chini B, Mouillac B, Ala Y, Balestre M, Kallmeyer S, Hoflack J, Elands J, Hibert M, Manning M, Jard S, and Barberis C (1995) Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J 14:2176-2182.
6. Chini B, Mouillac B, Balestre MN, Trumpp-Kallmeyer S, Hoflack J, Hibert M, Andriolo M, Pupier S, Jard S, and Barberis C (1996) Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin. FEBS Lett 397:201-206.
7. 2 receptors. Mol Pharmacol 43:755-761.
8. Daugé V and Roques BP (1995) Opioid and CCK systems in anxiety and reward, in Cholecystokinin and Anxiety: From Neuron to Behavior (Bradwejn J and Vasar E, eds.) pp 151-171, R. G. Landes Company, Austin.
9. Derrien M, Durieux C, and Roques BP (1994) Antidepressant-like effects of CCK-B antagonists in mice: antagonism by naltrindole. Br J Pharmacol 111:956-960.
10. Du K, Nicole P, Couveneau A, and Laburthe M (1997) Aspartate 196 in the first extracellular loop of the human VIP1 receptor is essential for VIP binding and VIP-stimulated cAMP production. Biochem Biophys Res Commun 230:289-292.
11. 3H]SNF 8702. Mol Pharmacol 41:1089-1095.
12. Evans BE, Bock MG, Rittle KE, de Pardo RM, Whitter WL, Veber DF, Anderson PS, and Freidinger RM (1986) Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin. Proc Natl Acad Sci USA 83:4948-4922.
13. Fong TM, Huang RRC, and Strader CD (1992) Localization of agonist and antagonist binding domains of the human NK-1 receptor. J Biol Chem 267:25664-25667.
14. Fong TM, Yu H, Cascieri MA, Underwood D, Swain CJ, and Strader CD (1994) The role of histidine 265 in antagonist binding to the neurokinin-1 receptor. J Biol Chem 269:2728-2732.
15. Graham FL and van der Erb AJ (1973) A new technique for the assay of infectivity of human adenovirus 5 DNA. Virology 52:456-467.
16. Hibert MF, Trumpp-Kallmeyer S, Bruinvels A, and Hoflack J (1991) Three-dimensional models of neurotransmitter G-binding protein-coupled receptors. Mol Pharmacol 40:8-15.
17. Hjorth SA, Schambye HT, Greenlee WJ, and Schwartz TW (1994) Identification of peptide binding residues in the extracellular domains of the AT(1) receptor. J Biol Chem 269:30953-30959.
18. Huang RRC, Yu H, Strader CD, and Fong TM (1994) Interaction of substance P with the second and seventh transmembrane domains of the neurokinin-1 receptor. Biochemistry 33:3007-3013.
19. Hughes J, Boden P, Costall B, Domeney A, Kelly E, Horwell DC, Hunter JC, Pinnock RD, and Woodruff GN (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci USA 87:6728-6732.
20. 100 in the second transmembrane domain of the cholecystokinin B receptor increases antagonist binding and reduces signal transduction. Mol Pharmacol 48:783-789.
21. A receptor antagonist selectivity. Eur J Pharmacol 296:97-106.
22. Kaupman K, Bruns C, Raulf H, Weber HP, Mattes H, and Lubbert H (1995) Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS 201-995 for the SSTR2 somatostatin receptor. EMBO J 14:727-735.
23. Kennedy K, Gigoux V, Escreut C, Maigret B, Martinez J, Moroder L, Fréhel D, Gully D, Vaysse N, and Fourmy D (1997) Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin. J Biol Chem 272:2920-2926.
24. Kong H, Raynor K, Yano H, Takeda J, Bell GI, and Reisine T (1994) Agonists and antagonists bind to different domains of the cloned Κ opioid receptor. Proc Natl Acad Sci USA 91:8042-8046.
25. Kopin AS, McBride EW, Quinn SM, Kolakowski LF, and Beinborn M (1995) The role of the cholecystokinin-B/gastrin receptor transmembrane domains in determining affinity for subtype-selective ligands. J Biol Chem 270:5019-5023.
26. Lotti VJ and Chang RSL (1989) A new potent and selective non peptide gastrin antagonist and brain CCK-B ligand: L-365,260. Eur J Pharmacol 162:273-280.
27. Maldonado R, Derrien M, Noble F, and Roques BP (1993) Association of the peptidase inhibitor RB 101 and a CCK-B antagonist strongly enhances antinociceptive responses. Neuroreport 4:947-950.
28. Mantamadiotis T and Baldwin GS (1994) The seventh transmembrane domain of gastrin/CCK receptors contributes to non-peptide antagonist binding. Biochem Biophys Res Commun. 201:1382-1389.
29. 1A angiotensin II receptor is essential for its coupling to phospholipase C. J Biol Chem 269:20815-20818.
30. Miyake A (1995) A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon. Biochem Biophys Res Commun 208:230-237.
31. Pepin MC, Yue SY, Roberts E, Wahlestedt C, and Walker P (1997) Novel 'restoration of function' mutagenesis strategy to identify amino acids of the δ-opioid receptor involved in ligand binding. J Biol Chem 272:9260-9267.
32. Probst WC, Snyder LA, Schuster DI, Brosius J, and Sealfon SC (1992) Sequence alignment of the G protein-coupled receptor superfamily. Cell Biol 11:1-20.
33. Schwartz TW and Rosenkilde MM ( 1996) Is there a 'lock' for all agonist 'keys'" in 7TM receptors? Trends Pharmacol Sci 17:213-216.
34. Silvente-Poirot S and Wank SA (1996) A segment of five amino acids in the second extracellular loop of the cholecystokinin-B receptor is essential for selectivity of the peptide agonist gastrin. J Biol Chem 271:14698-14706.
35. Surratt CK, Johnson PS, Moriwaki A, Seidleck BK, Blaschak CJ, Wang JB, and Uhl GR (1994) μ Opiate receptor: charged transmembrane domain amino acids are critical for agonist recognition and intrinsic activity. J Biol Chem 269:20548-20553.
36. 1A subtype, G protein-coupled receptor. Chem Biol 1:211-221.
37. B and neurotensin receptors. Br J Pharmacol 121:310-316.
38. Wank SA (1995) Cholecystokinin receptors. Am J Physiol 269:G628-G646.
39. Wess J, Maggio R, Palmer JR, and Vogel Z (1992) Role of conserved threonine and tyrosine residues in acetylcholine binding and muscarinic receptor activation: a study with m3 muscarinic receptor point mutants. J Biol Chem 267:19313-19319.
40. 3 muscarinic receptor. EMBO J 12:331-338.