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

Molecular Pharmacology

Volumn 49, Issue 2, 1996, Pages 216-223

  Befort, Katia ^a   Tabbara, Lina ^a   Bausch, Suzanne ^b   Chavkin, Charles ^b   Evans, Christopher ^c   Kieffer, Brigitte ^a,d  

^a UNIVERSITÉ DE STRASBOURG   (France)

^b UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d NONE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ASPARTIC ACID; OPIATE; SIGMA OPIATE RECEPTOR;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; DRUG RECEPTOR BINDING; NONHUMAN; PRIORITY JOURNAL; RECEPTOR BINDING; STRUCTURE ACTIVITY RELATION;

EID: 0030040907     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Mansour, A., C. A. Fox, H. Akil, and S J Watson. Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications. Trends Neurosci. 18:22-29 (1995).
2. Goldstein, A., and A. Naidu. Multiple opioid receptors, ligand selectivity profiles and binding site signatures. Mol. Pharmacol. 36:265-272 (1989).
3. Akil, H., S. J Watson, E. Young, M. E. Lewis, H. Khachaturian, and J. J. Walker. Endogenous opioids: biology and function. Annu. Rev. Neurosci. 7:223-255 (1984).
4. Dickenson, A. H. Mechanisms of the analgesic actions of opiates and opioids. Br. Med. Bull. 47:690-702 (1991).
5. Di Chiara, G., and A. North. Neurobiology of opiate abuse. Trends Pharmacol. Sci. 13:185-193 (1992).
6. Olson, G. A., R. D. Olson, and A J. Kastin. Endogenous opiates: 1993. Peptides 15:1513-1556 (1994).
7. Rees, D. C., and J. C. Hunter. Opioid receptors, in Comprehensive Medicinal Chemistry (J. C. Emmet, ed.). Pergamon Press, New York, 805-846 (1990).
8. Schiller, P. W. Development of receptor-selective opioid peptide analogs as pharmacologic tools and as potential drugs, in Opioids I (A. Herz, ed.). Vol. 104. Springer-Verlag, Berlin, 681-704 (1993).
9. Barnard, E. A. Pipe dreams realized. Curr. Biol 3011-214 (1993).
10. Evans, C. J., D. E. Keith, H. Morrison, K. Magendzo, and R. H. Edwards. Cloning of a delta opioid receptor by functional expression. Science (Washington D. C.) 258:1952-1955 (1992).
11. Kieffer, B. L., K. Befort, C. Gaveriaux-Ruff, and C. G. Hirth. The delta opioid receptor: isolation of a cDNA by expression cloning and pharmacological characterization. Proc. Natl. Acad. Sci. USA 89:12048-12052 (1992).
12. Strader, C. D., I. S. Sigal, R. B. Register, M. R. Candelore, E. Rands, and R. A. F. Dixon. Identification of residues required for ligand binding to the fteia-adrenergic receptor. Proc. Natl. Acad. Sci. USA 84:4384-1388 (1987).
13. Strader, C. D., I. S. Sigal, M. R. Candelore, E. Rands, W. S. Hill, and R. A. F. Dixon. Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor fonction. J. Biol. Chem. 263:10267-10271 (1988).
14. Strader, C. D., M. R. Candelore, W. S. Hill, R. A. F. Dixon, and I. S. Sigal. A single ami no acid substitution in the beta-adrenergic receptor promotes partial agonist activity for antagonists. J. Biol Chem. 264:16470-16477 (1989).
15. 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonist. Mol. Pharmacol. 40:168-179 (1991).
16. Fraser, C. D., C. D. Wang, D. A. Robinson, J. D. Gocayne, and J. C. Venter. Site-directed mutagenesis of m1 muscarinic acetylcholine receptors: conserved aspartic acids play important roles in receptor fonction. Mol. Pharmacol. 36:840-847 (1989).
17. Gantz, I., J. Delvalle, L. D. Wang, T. Tashiro, G. Munzert, Y. J. Guo, Y. Konda, and T. Yamada. Molecular basis for the interactions of histamine with the histamine H2 receptor. J. Biol. Chem. 267:20840-20843 (1992).
18. Ohta, K., H. Hayashi, H. Mizuguchi, H. Kagamiyama, K. Fujimoto, and H. Fukui. Site-directed mutagenesis of the histamine H1 receptor: roles of aspartic acid 107, asparagine 198 and threonine 194. Biochem. Biophys. Res Commun. 203:1096-1101 (1994).
19. Schwartz, R. D., C. J. Spencer, T. Mirzadegan, D. Moreland, H. Tecle, and A. J. Thomas. Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists. Life Sci. 56:923-929 (1995).
20. Surratt, C. K., P. S. Johnson, A. Moriwaki, B. K. Seidleck, C. J. Blaschak, J. B. Wang, and G. R. Uhl. Mu opiate receptor: charged transmembrane domain aminoacids are critical for agonist recognition and intrinsic activity. J. Biol. Chem. 269:20548-20553 (1994).
21. Strader, C. D., Y. Gaffney, E. E. Sugg, M. R. Candelore, R. Keys, A. A. Patchett, and R A. F. Dixon. Allele-specific activation of genetically engineered receptors. J. Biol. Chem. 266:5-8 (1991).
22. Kaufinan, D. L., D. E. Keith, B. Anton, J. Tian, K. Magendzo, D. Newman, T. H. Tran, D. S. Lee, C. Wen, Y.-R. Xia, A. J. Lusis, and C. J. Evans. Characterization of the murine mu opioid receptor gene. J. Biol Chem. 270:15877-15883 (1995).
23. Bausch, S. B., T. A. Patterson, S. M. Appleyard, and C. Chavkin. Immunocytochemical localization of delta opioid receptors in mouse brain. J. Chem. Neuroanat. 8:175-189 (1995).
24. Law, P.-Y., D. S. Hom, and H. H. Loh. Multiple affinity states of opiate receptor in neuroblastoma X glioma NG108-15 hybrid cells. J. Biol. Chem. 260:3561-3569 (1985)
25. Paterson, S. J., L. E. Robson, and H. W. Kosterlitz. Control by cations of opioid binding in guinea pig brain membranes. Proc. Natl. Acad. Sci. USA 83:6216-6220 (1986).
26. Law, P. Y., T. M. McGinn, M. J. Wick, L. J. Erickson, C. J. Evans, and H. H. Loh. Analysis of delta-opioid receptor activities stably expressed in CHO cells: function of receptor density? J. Pharmacol. Exp. Ther. 271: 1686-1694 (1994)
27. Childers, S. R., L. M. Fleming, D. E. Selley, R. W. McNutt, and K. J. Chang. BW373U86: A nonpeptidic δ-opioid agonist with novel receptor-G protein-mediated actions in rat brain membranes and neuroblastoma cells. Mol. Pharmacol 44:827-834 (1993).
28. Hibert, M. F., S. Trump-Kallmeyer, A. Bruinvels, and J. Hoflack. Three-dimensional models of neurotransmitter G-binding protein-coupled receptors. Mol. Pharmacol. 40:8-15 (1991).
29. Knapp, R J., E. Malatynska, N. Collins, L. Fang, J. Y. Wang, V. J. Hruby, W. R. Roeske, and H. I. Yamamura. Molecular biology and pharmacology of cloned opioid receptors. FASEB J. 9:516-525 (1995).
30. Xue, J C., C. G. Chen, J. M. Zhu, S. Kunapuli, J. K. Deriel, L. Yu, and L. Y. Liuchen. Differential binding domains of peptide and non-peptide ligands in the cloned rat kappa opioid receptor J. Biol. Chem. 269:30195-30199 (1994).
31. Fukuda, K., S. Kato, and K. Mori. Location of regions of the opioid receptor involved in selective agonist binding. J. Biol. Chem. 270:6702-6709 (1995).
32. Werling, L. L., P. S. Puttfarcken, and B. M. Cox. Multiple agonist affinity states of opioid receptors: regulation of binding by guanyl nucleotides in guinea pig cortical, NG108-15, and 7315C cell membranes. Mol. Pharmacol. 33:423-431 (1988).
33. Ott, S., and T. Costa. Guanine nucleotide-mediated inhibition of opioid agonist binding. Biochem Pharmacol. 38:1931-1939 (1989).
34. Kong, H., K. Raynor, K. Yasuda, S. T. Moe, P. S. Porthoghese, G. I. Bell, and T Reisine. A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding. J. Biol. Chem. 31:23055-23058 (1993).
35. Harel, M., I. Schalk, L. Ehret-Sabatier, F. Bouet, M. Goeldner, C. Hirth, P. Axelsen, I. Silman, and J. L. Sussman. Quaternary ligand binding to aromatic residues in the active-site of acetylcholinesterase. Proc. Natl. Acad. Sci. USA 90:9031-9035 (1993).
36. Waksman, G., D. Kommos, S. C. Robertson, N. Pant, D. Baltimore, R. B. Birge, D. Cowburn, H. Hanafusa, B. J. Mayer, M. Overduin, M. D. Resh, C. B. Rios, L. Silverman, and J. Kuriyan. Crystal structure of the phosphotyrosine recognition domain SH2 of v-src complexed with tyrosine-phosphorylated peptides. Nature (Lond.) 358:646-653 (1992).
37. Fong, T. M , M A. Cascieri, H- Yu, A. Bansal, C. Swain, and C. D. Strader. Amino-aromatic interaction between, histidine 197 of the neurokinin 1 receptor and CP 96345, Nature (Lond.) 362:350-353 (1993).