Functional inactivation of the nociceptin receptor by alanine substitution of glutamine 286 at the C terminus of transmembrane segment VI: Evidence from a site-directed mutagenesis study of the ORL1 receptor transmembrane-binding domain

Molecular Pharmacology

Volumn 57, Issue 3, 2000, Pages 495-502

  Mouledous, Lionel ^a   Topham, Christopher M ^a   Moisand, Christiane ^a   Mollereau, Catherine ^a   Meunier, Jean Claude ^a  

^a INSTITUT DE PHARMACOLOGIE ET DE BIOLOGIE STRUCTURALE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; CYCLIC AMP; ETORPHINE; FORSKOLIN; GLUTAMINE; GUANINE NUCLEOTIDE BINDING PROTEIN; KAPPA OPIATE RECEPTOR; LOFENTANIL; NOCICEPTIN; NOCICEPTIN RECEPTOR; NORBINALTORPHIMINE; OPIATE AGONIST; TRITIUM;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHO CELL; DRUG RECEPTOR BINDING; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS;

EID: 0034090704     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.57.3.495     Document Type: Article

References (40)

1. Alvarez R and Daniels DV (1992) A separation method for the assay of adenylylcyclase, intracellular cyclic AMP, and cyclic AMP phosphodiesterase using tritium-labeled substrates. Anal Biochem 203:76-82.
2. Befort K, Tabbara L, Bausch S, Chavkin C, Evans C and Kieffer B (1996a) The conserved aspartate residue in the third putative transmembrane domain of the δ-opioid receptor is not the anionic counterpart for cationic opiate binding but is a constituent of the receptor binding site. Mol Pharmacol 49:216-223.
3. Befort K, Tabbara L, Kling D, Maigret B and Kieffer B (1996b) Role of aromatic transmembrane residues of the δ-opioid receptor in ligand recognition. J Biol Chem 271:10161-10168.
4. Bikker JA, Trumpp-Kallmeyer S and Humblet C (1998) G-protein-coupled receptors: Models, mutagenesis, and drug design. J Med Chem 41:2911-2927.
5. Butour J-L, Moisand C, Mazarguil H, Mollereau C and Meunier J-C (1997) Recognition and activation of the opioid receptor-like ORL1 receptor by nociceptin, nociceptin analogs and opioids. Eur J Pharmacol 321:97-103.
6. 2 N-terminal tetrapeptide and discovery of a nociceptin receptor antagonist. J Med Chem 41:3360-3366.
7. Chavkin C and Goldstein A (1981) Specific receptor for the opioid peptide dynorphin: Structure-activity relationships. Proc Natl Acad Sci USA 78:6543-6547.
8. Chen C and Okayama H (1987) High efficiency transformation of mammalian cells by plasmid DNA. Mol Cell Biol 7:2745-2752.
9. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
10. Darland T, Heinricher MM and Grandy DK (1998) Orphanin FQ/nociceptin: A role in pain and analgesia, but so much more. Trends Neurosci 21: 215-221.
11. Dooley CT and Houghten RA (1996) Orphanin FQ: Receptor binding and analog structure activity relationships in rat brain. Life Sci 59:PL23-29.
12. Dooley CT, Spaeth CG, Bertzetei-Gurske IP, Craymer K, Adapa ID, Brandt SR, Houghten RA and Toll L (1997) Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther 283:735-741.
13. Dunham TD and Farrens DL (1999) Conformational changes in rhodopsin: Movement of helix F detected by site-specific chemical labeling and fluorescence spectroscopy. J Biol Chem 274:1683-1690.
14. Guerrini R, Calo' G, Rizzi A, Bianchi C, Lazarus LH, Salvadori S, Temussi PA and Regoli D (1997) Address and message sequences for the nociceptin receptor: A structure-activity study of nociceptin-(1-13)-peptide amide. J Med Chem 40:1789-1793.
15. Henderson G and McKnight AT (1997) The orphan opioid receptor and its endogenous ligand - nociceptin/orphanin FQ. Trends Pharmacol Sci 18:293-300.
16. Hjorth SA, Thirstrup K, Grandy DK and Schwartz TW (1995) Analysis of selective binding epitopes for the κ-opioid receptor antagonist nor-binaltorphimine. Mol Pharmacol 47:1089-1094.
17. Jones RM, Hjorth SA, Schwartz TW and Portoghese PS (1998) Mutational evidence for a common κ antagonist binding pocket in the wild-type κ and mutant μ[K303E] opioid receptors. J Med Chem 41:4911-4914.
18. Kawai S and Nishizawa M (1984) New procedure for DNA transfection with polycation and dimethyl sulfoxide. Mol Cell Biol 4:1172-1174.
19. Lapalu S, Moisand C, Butour J-L, Mollereau C and Meunier J-C (1998) Different domains of the ORL1 and κ-opioid receptors are involved in recognition of nociceptin and dynorphin A. FEBS Lett 427:296-300.
20. Lapalu S, Moisand C, Mazarguil H, Cambois G, Mollereau C and Meunier J-C (1997) Comparison of the structure-activity relationships of nociceptin and dynorphin A using chimeric peptides. FEBS Lett 417:333-336.
21. Mansour A, Hoversten MT, Taylor LP, Watson SJ and Akil H (1995) The cloned μ, δ and κ receptors and their endogenous ligands: Evidence for two opioid peptide recognition cores. Brain Res 700:89-98.
22. Meng F, Taylor LP, Hoversten MT, Ueda Y, Ardati A, Reinscheid RK, Monsma FJ, Watson SJ, Civelli O and Akil H (1996) Moving from the orphanin FQ receptor to an opioid receptor using four point mutations. J Biol Chem 271:32016-32020.
23. Meng F, Ueda Y, Hoversten MT, Taylor LP, Reinscheid RK, Monsma FJ, Watson SJ, Civelli O and Akil H (1998) Creating a functional opioid alkaloid binding site in the orphanin FQ receptor through site-directed mutagenesis. Mol Pharmacol 53:772-777.
24. Meunier J-C (1997) Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor. Eur J Pharmacol 340:1-15.
25. Meunier J-C, Mollereau C, Toll L, Suaudeau C, Moisand C, Alvinerie P, Butour J-L, Guillemot J-C, Ferrara P, Monsarrat B, Mazarguil H, Vassart G, Parmentier M and Costentin J (1995) Isolation and structure of the endogenous agonist of opioid receptor- like ORL1 receptor. Nature 377:532-535.
26. 280 by His in TM 6 of the human ORL1 receptor increases affinity but reduces intrinsic activity of opioids. FEBS Lett 396:17-21.
27. Mollereau C, Moulèdous L, Lapalu S, Moisand C, Butour J-L and Meunier J-C (1999) Distinct mechanisms for activation of the ORL1 and κ-opioid receptors by nociceptin and dynorphin A. Mol Pharmacol. 55:324-331.
28. Mollereau C, Parmentier M, Mailleux P, Buteur J-L, Moisand C, Chalon P, Caput D, Vassart G and Meunier J-C (1994) ORL1, a novel member of the opioid receptor family: Cloning, functional expression and localization. FEBS Lett 341:33-38.
29. Monod J, Wyman J and Changeux JP (1965) On the nature of the allosteric transition: a plausible model. J Mol Biol 12:88-118.
30. Paterlini G, Portoghese PS and Ferguson DM (1997) Molecular simulation of dynorphin A-(1-10) binding to extracellular loop 2 of the κ-opioid receptor: A model for receptor activation. J Med Chem 40:3254-3262.
31. Pogozheva ID, Lomize AL and Mosberg HI (1998) Opioid receptor three-dimensional structures from distance geometry calculations with hydrogen bonding constraints. Biophys J 75:612-634.
32. Reinscheid RK, Ardati A, Monsma FJ Jr and Civelli O (1996) Structure-activity relationship studies on the novel neuropeptide orphanin FQ. J Biol Chem 271: 14163-14168.
33. Reinscheid RK, Higelin J, Henningsen RA, Monsma FJ Jr and Civelli O (1998) Structures that delineate orphanin FQ and dynorphin A pharmacological selectivities. J Biol Chem 273:1490-1495.
34. Reinscheid RK, Nothacker HP, Bourson A, Ardati A, Henningsen RA, Bunzow JR, Grandy DK, Langen H, Monsma FJ and Civelli O (1995) Orphanin FQ: A neuropeptide that activates an opioidlike G protein-coupled receptor. Science 270:792-794.
35. Schwyzer R (1977) ACTH: A short introductory review. Ann NYAcad Sci 297:3-26.
36. Shimohigashi Y, Hatano R, Fujita T, Nakashima R, Nose T, Sujaku T, Saigo A, Shinjo K and Nagahisa A (1996) Sensitivity of opioid receptor-like receptor ORL1 for chemical modification on nociceptin, a naturally occuring nociceptive peptide. J Biol Chem 271:23642-23645.
37. 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.
38. Topham CM, Moulédous L, Poda G, Maigret B and Meunier J-C (1998) Molecular modelling of the ORL1 receptor and its complex with nociceptin. Protein Eng 11:1163-1179.
39. Trumpp-Kallmeyer S, Hoflack J, Bruinvels A and Hibert M (1992) Modeling of G protein-coupled receptors: Application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors. J Med Chem 36:3448-3462.
40. Valiquette M, Vu HK, Yue SY, Wahlestedt C and Walker P (1996) Involvement of Trp-284, Val-296, and Val-297 of the human δ-opioid receptor in binding of δ-selective ligands. J Biol Chem 271:18789-18796.