Constitutive activation of the opioid receptor-like (ORL1) receptor by mutation of Asn133 to tryptophan in the third transmembrane region

Journal of Neurochemistry

Volumn 83, Issue 6, 2002, Pages 1461-1470

  Kam, Kenneth W L ^a   New, David C ^a   Wong, Yung H ^a,b  

^a HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (Hong Kong)

^b UNIVERSITY OF HONG KONG   (Hong Kong)

Author keywords

CAM; G protein coupling; ORL1; Receptor

Indexed keywords

ASPARAGINE; G PROTEIN COUPLED RECEPTOR; MUTANT PROTEIN; OPIATE RECEPTOR; OPIOID RECEPTOR LIKE RECEPTOR; TRYPTOPHAN; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; HUMAN; HUMAN CELL; LIGAND BINDING; MUTAGENESIS; POINT MUTATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN FUNCTION; RECEPTOR BINDING; SIGNAL TRANSDUCTION;

EID: 0036905714     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.2002.01231.x     Document Type: Article

References (43)

1. Baldwin J. M. (1993) The probable arrangement of the helices in G protein-coupled receptors. EMBO J. 12, 1693-1703.
2. 1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII. J. Biol. Chem. 272, 4245-4251.
3. 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.
4. 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.
5. Befort K., Zilliox C., Filliol D., Yue S. and Kieffer B. L. (1999) Constitutive activation of the δ-opioid receptor by mutations in transmembrane domains III and VIl. J. Biol. Chem. 274, 18574-18581.
6. Bunzow J. R., Saez C., Mortrud M., Bouvier C., Williams J. T., Low M. and Grandy D. K. (1994) Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a μ-, δ- or κ-opioid receptor type. FEBS Lett. 347, 284-288.
7. 1). Peptides 21, 1147-1154.
8. Calo' G., Guerrini R., Rizzi A., Salvadori S. and Regoli D. (2000) Pharmacology of nociceptin and its receptor: A novel therapeutic target. Br. J. Pharm. 129, 1261-1283.
9. 1 receptor through multiple G proteins. J. Pharmacol. Exp. Ther. 295, 1094-1100.
10. 16 proteins. J. Neurochem. 71, 2203-2210.
11. Chen G., Way J., Armour S., Watson C., Queen K., Jayawickreme C. K., Chen W. J. and Kenakin T. (2000) Use of constitutive G protein-coupled receptor activity for drug discovery. Mol. Pharmacol. 57, 125-134.
12. Chiu T. T., Yung L. Y. and Wong Y. H. (1996) Inverse agonistic effect of ICI-174,864 on the cloned δ-opioid receptor: Role of G protein and adenylyl cyclase activation. Mol. Pharmacol. 50, 1651-1657.
13. 1 dopamine receptor binding and signal transduction. Mol. Pharmacol. 50, 1338-1345.
14. Cohen G. B., Yang T., Robinson P. R. and Oprian D. D. (1993) Constitutive activation of opsin: Influence of charge at position 134 and size at position 296. Biochemistry 32, 6111-6115.
15. 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function. Proc. Natl Acad. Sci. USA 87, 2896-2900.
16. 1A angiotensin II receptor induces its constitutive activation. J. Biol. Chem. 272, 1822-1826.
17. von Heijne G. (1991) Proline kinks in transmembrane α-helices. J. Mol. Biol. 218, 499-503.
18. Jin J., Mao G. F. and Ashby B. (1997) Constitutive activity of human prostaglandin E receptor EP3 isoforms. Br. J. Pharmacol. 121, 317-323.
19. Joseph M. P., Maigret B., Bonnafus J.-C., Marie J. and Scherega H. A. (1995) A Computer modeling postulated mechanism for angiotensin II receptor activation. J. Prot. Chem. 14, 381-398.
20. 1B-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.
21. 16-mediated stimulation of phospholipase C. J. Neurochem. 70, 2203-2211.
22. Li J., Chen C., Huang P. and Liu-Chen L. Y. (2001a) Inverse agonist upregulates the constitutively active D3.49 (164) Q mutant of the rat μ-opioid receptor by stabilizing the structure and blocking constitutive internalization and down-regulation. Mol. Pharmacol. 60, 1064-1075.
23. Li J., Huang P., Chen C., de Riel J. K., Weinstein H. and Liu-Chen L. Y. (2001b) Constitutive activation of the μ-opioid receptor by mutation of D3.49 (164), but not D3.32 (147): D3.49 (164) is critical for stabilization of the inactive form of the receptor and for its expression. Biochemistry 40, 12039-12050.
24. 2-adrenoceptor by sustained treatment with inverse agonists but not antagonists. FEBS Lett. 399, 108-112.
25. Mansour A., Taylor L. P., Fine J. L., Thompson R. C., Hoversten M. T., Mosberg H. I., Watson S. J. and Akil H. (1997) Key residues defining the μ-opioid receptor binding pocket: A site-directed mutagenesis study. J. Neurochem. 68, 344-353.
26. 2 receptor induced by mutations in transmembrane helices III and VI. Mol. Pharmacol. 55, 92-101.
27. 1 receptor. Nature 377, 532-535.
28. Mogil J. S. and Pastemak G. W. (2001) The molecular and behavioural pharmacology of the orphanin FQ/Nociceptin peptide and receptor family. Pharamacol. Rev. 53, 381-415.
29. 1 receptor transmembrane-binding domain. Mol. Pharm. 57, 495-502.
30. Pauwels P. J. and Wurch T. (1998) Amino acid domains involved in constitutive activation of G protein-coupled receptors. Mol. Neurobiol. 17, 109-135.
31. Perez D. M., Hwa J., Gaivin R., Mathur M., Brown F. and Graham R. M. (1996) Constitutive activation of a single effector pathway: Evidence for multiple activation states of a G protein-coupled receptor. Mol. Pharmacol. 49, 112-122.
32. 1B-adrenergic receptor is initiated by disruption of an interhelical salt bridge constraint. J. Biol. Chem. 271, 28318-28323.
33. Reinscheid R. K., Nothacker H. P., Bourson A., Ardati A., Henningsen R. A., Bunzow J. R., Grandy D. K., Langen H., Monsma F. J. and Civelli O. (1995) Orphanin FQ: A neuropeptide that activates an opioid-like G protein-coupled receptor. Science 270, 792-794.
34. 2-adrenergic receptor. J. Biol. Chem. 268, 16483-16487.
35. 1B-adrenergic receptor: Role of highly conserved polar amino acids in receptor activation. EMBO J. 15, 3566-3578.
36. 1B-adrenergic receptor: Potential role of protonation and hydrophobicity of a highly conserved aspartate. Proc. Natl Acad. Sci. USA 94, 808-813.
37. Sibley D. R. and Neve K. A. (1997) The Dopamine Receptors, in Molecular Biology of Dopamine Receptors (Neve K. A. and Neve R. L., eds), pp. 383-424. Humana Press, Totowa, NJ.
38. Strange P. G. (2001) Antipsychotic drugs: Importance of dopamine receptors for mechanisms of therapeutic actions and side effects. Pharmacol. Rev. 53, 119-133.
39. 1 receptor and its complex with nociceptin. Prot. Eng. 11, 1163-1179.
40. Tsai S. C., Adamik R., Kanaho Y., Hewlett E. L. and Moss J. (1984) Effects of guanyl nucleotides and rhodopsin on ADP-ribosylation of the inhibitory GTP-binding component of adenylate cyclase by pertussis toxin. J. Biol. Chem. 259, 15320- 15323.
41. Wonerow P., Schoneberg T., Schultz G., Gudermann T. and Paschke R. (1998) Deletions in the third intracellular loop of the thyrotropin receptor. A new mechanism for constitutive activation. J. Biol. Chem. 273, 7900-7905.
42. 14) couples the opioid receptor-like1 receptor to stimulation of phospholipase C. J. Pharmacol. Exp. Ther. 288, 232-238.
43. 2-adrenergic receptor. J. Biol. Chem. 273, 3401-3407.