Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition

Molecular Pharmacology

Volumn 49, Issue 4, 1996, Pages 683-691

  Kim, Jeongho ^a   Jiang, Qiaoling ^a   Glashofer, Marc ^a   Yehle, Susan ^a   Wess, Jürgen ^a   Jacobson, Kenneth A ^a,b  

^a NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

^b NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE A2 RECEPTOR; ADENOSINE A3 RECEPTOR; ADENOSINE RECEPTOR STIMULATING AGENT; GLUTAMIC ACID;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; CENTRAL NERVOUS SYSTEM DISEASE; DOPAMINERGIC SYSTEM; DRUG MECHANISM; DRUG RECEPTOR BINDING; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL;

ADENOSINE; AMINO ACID SEQUENCE; BASE SEQUENCE; BINDING SITES; CALCIUM; ENZYME-LINKED IMMUNOSORBENT ASSAY; GLUTAMIC ACID; HUMANS; LIGANDS; MAGNESIUM; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; PHENETHYLAMINES; RECEPTORS, PURINERGIC P1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0029960789     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Jacobson, K. A., P. J. M. van Galen, and M. Williams. Adenosine receptors: pharmacology, structure activity relationships, and therapeutic potential. J. Med. Chem. 35:407-422 (1992).
2. Barraco, R. A., K. Martens, M. Parizon, and H. J. Normile. Role of adenosine A(2a) receptors in the nucleus-accumbens. Prog. Neuropsychopharmocol. Biol. Psychiatry 18:545-553 (1994).
3. Olsson, R. A., and J. D. Pearson. Cardiovascular purinoceptors. Pharmacol. Rev. 3:761-845 (1990).
4. 2 receptors in rat brain. J. Pharmacol. Exp. Ther. 251:888-893 (1989).
5. 2 receptor regulation of striatal gene expression, in Adenosine and Adenine Nucleotides: From Molecular Biology to Integrative Physiology (L. Belardinelli and A. Pelleg, eds.). Kluver, Norwell, MA, 5-14 (1995).
6. Nikodijević, O., K. A. Jacobson, and J. W. Daly. Acute treatment of mice with high-doses of caffeine: an animal-model for choreiform movement. Drug Dev. Res. 30:121-128 (1993).
7. Martin, G. E., D. J. Rossi, and M. F. Jarvis. Adenosine agonists reduce conditioned avoidance responding in the rat. Pharm. Biochem. Behav. 45:951-958 (1993).
8. Jacobson, M. Molecular biology of adenosine receptors, in Adenosine and Adenine Nucleotides: from Molecular Biology to Integrative Physiology (L. Belardinelli and A. Pelleg, eds. J. Kluver, Norwell, MA, 5-14 (1995).
9. 2a Adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol. Pharmacol. 41:352-359 (1992).
10. Strader, C. D., M. R. Candelore, W. S. Hill, I. S. Sigal, and R. A. F. Dixon. Identification of two serine residues involved in agonist activation of the β-adrenergic receptor. J. Biol. Chem. 264:13572-13578 (1989).
11. Wess, J., N. Blin, E. Mutschler, and K. Blüml. Muscarinic acetylcholine receptors: structural basis of ligand binding and G protein coupling. Life Sci. 56:915-912 (1995).
12. 2a adenosine receptor. J. Biol. Chem. 270:13987-13997 (1995).
13. Olah, M. E., K. A. Jacobson, and G. L. Stiles. Identification of an adenosine receptor domain specifically involved in binding of 5′-subsatuted adenosine agonists. J. Biol. Chem. 269:18016-18020 (1994).
14. 1-adenosine receptor mediates specific agonist binding. J. Biol. Chem. 269:2373-2376 (1994).
15. 1 adenosine receptors: 2 amino-acids are responsible for species differences in ligand recognition. J. Biol. Chem. 269: 27900-27906 (1994).
16. Walker, P., M. Munoz, R. Martinez, and M. C. Peitsch. Acidic residues in extracellular loops of the human Y1 neuropeptide Y receptor are essential for ligand binding. J. Biol. Chem. 269:2863-2869 (1994).
17. Flanagan, C. A., I. I. Becker, J. S. Davidson, I. K. Wakefield, W. Zhou, S. C. Sealfon, and R. P. Millar. Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone. J. Biol. Chem. 268:22636-22641 (1994).
18. Chini, B., B. Mouillac, Y. Ala, M. Balestre, S. Trumpp-Kallmeyer, J. Hoflack, J. Elands, M. Hibert, M. Manning, S. Jard, and C. Barberis. Tyr 115 is the key residue for determining agonist selectivity in the V1A vasopressin receptor. EMBO J. 14:2176-2182 (1995).
19. 3-adenosine receptors. J. Biol. Chem. 269:24692-24698 (1994)
20. 3-selective adenosine agonists. J. Med. Chem. 37:636-646 (1994).
21. Okayama, H., and P. A. Berg. A cDNA cloning vector that permits expression of cDNA inserts in mammalian cells. Mol. Cell. Biol. 3:280-289 (1983).
22. Higuchi, R. Using PCR to engineer DNA, in PCR Technology (Ehrlich H. A., ed.). Stockton Press, New York, 61-70 (1989).
23. Sanger, R., S. Nicklen, and A. R. Coulson. DNA sequencing with chain-terminating inhibitors. Proc. Natl. Acad. Sci. USA 74:5463-5467 (1977).
24. Cullen, B. R. Use of eukaryotic expression technology in the functional analysis of cloned genes. Methods Enzymol. 152:684-704 (1987).
25. 2 dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary. Mol. Pharmacol. 23:576-584 (1983).
26. 2-Dopamine receptor-mediated inhibition of cyclic AMP formation in striatal neurons in primary culture. Mol Pharmacol. 27:595-599 (1985).
27. 3-adenosine receptors. Drug Dev. Res. 33:51-59 (1994).
28. 2 receptors: structure-function relationships. Med. Res. Rev. 12:423-471 (1992).
29. Finn, B. E., and S. Forsen. The evolving model of calmodulin structure, function and activation. Structure 3:7-11 (1995).
30. 2 receptors in rat striatum. Biochem. Pharmacol. 44:2365-2370 (1992).
31. Deleted in proof.
32. 1 adenosine receptor studies on the ligand binding site by site-directed mutagenesis. J. Biol. Chem. 267:10764-10770 (1992).
33. 2a receptor. Eur. J. Pharmacol. 268:95-104 (1994).
34. Fitzpatrick, D. V., and R. L. Vandlen. Agonist selectivity determinants in somatostatin receptor subtypes I and II. J. Biol. Chem. 269:24621-24526 (1994).
35. Anukanth, A., and H. G. Khorana. Structure and function in rhodopsin: requirements of a specific structure for the intradiscal domain. J. Biol. Chem. 269:19738-19744 (1994).
36. Matsui, H., S. Lazareno, and N. J. M. Birdsall. Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis. Mol. Pharmocol. 47:88-98 (1995).
37. Gohda, K., K. Oka, K. Tomita, and T. Hakoshima. Crystal structure of RNase T1 complexed with the product nucleotide 3′-GMP. J. Biol. Chem. 269:17531-17536 (1994).
38. Mowbray, S. L., and L. B. Cole. 1.7 A X-ray structure of the periplasmic ribose receptor from Escherichia coli. J. Mol. Biol. 225:155-175 (1992).
39. Schoneberg, T., J. Liu, and J. Wess. Plasma membrane Localization and functional rescue of truncated forms of a G protein-coupled receptor. J. Biol. Chem. 270:18000-18006 (1995).
40. MacKinnon, R. Pore loops: an emerging theme in ion channel structure. Neuron 14:889-892 (1995).