Site-directed mutagenesis studies of human A(2A) adenosine receptorsInvolvement of glu13 and his278 in ligand binding and sodium modulation

Biochemical Pharmacology

Volumn 60, Issue 5, 2000, Pages 661-668

  Gao, Zhan Guo ^a   Jiang, Qiaoling ^b   Jacobson, Kenneth A ^b   Ijzerman, Adriaan P ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

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

Author keywords

A(2A) Adenosine receptor; Glutamic acid; Histidine; Mutation; Sodium ions

Indexed keywords

2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 4 [2 [7 AMINO 2 (2 FURYL) 1,2,4 TRIAZOLO[2,3 A][1,3,5]TRIAZIN 5 YLAMINO]ETHYL]PHENOL; 5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; 6 N [2 (3,5 DIMETHOXYPHENYL) 2 (2 METHYLPHENYL)ETHYL]ADENOSINE; 6 N CYCLOPENTYLADENOSINE; 8 [4 (2 AMINOETHYLCARBAMOYL)METHOXYPHENYL] 1,3 DIPROPYLXANTHINE; 9 CHLORO 2 (2 FURYL) 5,6 DIHYDRO 5 IMINO 1,2,4 TRIAZOLO[2,3 C]QUINAZOLINE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE A2A RECEPTOR; THEOPHYLLINE;

AMINO ACID COMPOSITION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL CULTURE; CONTROLLED STUDY; HUMAN; IN VITRO STUDY; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING, COMPETITIVE; DRUG INTERACTIONS; GLUTAMIC ACID; GUANOSINE TRIPHOSPHATE; HISTIDINE; HUMANS; KINETICS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; RADIOLIGAND ASSAY; RECEPTOR, ADENOSINE A2A; RECEPTORS, PURINERGIC P1; SODIUM; TRIAZINES; TRIAZOLES; TRITIUM;

EID: 0034284625     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(00)00357-9     Document Type: Article

References (33)

1. Jacobson M, Molecular biology of adenosine receptors. In: Adenosine and Nucleotides: From Molecular Biology to Integrative Physiology (Eds. Belardinelli L and Pelleg A), pp. 5-14. Kluver, Norwell, MA, 1995.
2. 2A receptors in the nucleus accumbens. Prog Neuropsychopharmacol Biol Psychiatry. 18:1994;545-553.
3. Olsson R.A., Pearson J.D. Cardiovascular purinoceptors. Physiol Rev. 70:1990;761-845.
4. 2 receptors in rat brain. J Pharmacol Exp Ther. 251:1989;888-893.
5. 2 receptors in the ventral striopallidal system. Implications for the treatment of schizophrenia. Neuroscience. 63:1994;765-773.
6. Nikodijevic O., Jacobson K.A., Daly J.W. Acute treatment of mice with high-doses of caffeine An animal model for choreiform movement . Drug Dev Res. 30:1993;121-128.
7. Martin G.E., Rossi D.J., Jarvis M.F. Adenosine agonists reduce conditioned avoidance responding in the rat. Pharmacol Biochem Behav. 45:1993;951-958.
8. 2 receptor regulation of striatal gene expression. In: Adenosine and Nucleotides: From Molecular Biology to Integrative Physiology (Eds. Belardinelli L and Pelleg A), pp. 71-76. Kluver, Norwell, MA, 1995.
9. 2A receptor antagonist with anticataleptic activity . Eur J Pharmacol. 256:1994;263-268.
10. Fredholm B.B., Abbracchio M.P., Burnstock G., Daly J.W., Harden T.K., Jacobson K.A., Leff P., Williams M. Nomenclature and classification of purinoceptors. Pharmacol Rev. 46:1994;143-146.
11. 2A adenosine receptor. J Biol Chem. 270:1995;13987-13997.
12. 2A adenosine receptor are required for ligand recognition. Mol Pharmacol. 49:1996;683-691.
13. 2A receptor. Critical involvement of Glu13 in agonist recognition. Eur J Pharmacol. 310:1996;269-272.
14. 2A adenosine receptors are required for ligand recognition. Mol Pharmacol. 50:1996;512-521.
15. 2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem. 40:1997;2588-2595.
16. 3H]-SCH58261. Br J Pharmacol. 121:1997;353-360.
17. 2A receptor. Eur J Pharmacol. 268:1994;95-104.
18. Baldwin J.M., Schertler G.F., Unger V.M. An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors. J Mol Biol. 272:1997;144-164.
19. 2A adenosine receptors. Mol Pharmacol. 42:1992;123-133.
20. 1 adenosine receptor. Studies on the ligand binding site by site-directed mutagenesis. J Biol Chem. 267:1992;10764-10770.
21. 50) of an enzymatic reaction. Biochem Pharmacol. 22:1973;3099-3108.
22. 1 adenosine receptor Influences of acidic and hydroxy residues in the first four transmembrane domains on ligand binding . Mol Pharmacol. 50:1996;1635-1642.
23. 2 receptor antagonist, to rat brain membranes. Mol Pharmacol. 46:1994;817-822.
24. 125I]iodophenyl)ethylamino]adenosine. Mol Pharmacol. 47:1995;307-313.
25. 1 receptors . J Med Chem. 31:1988;745-751.
26. 2-adrenergic receptors by sodium. J Biol Chem. 265:1990;21590-21595.
27. +, 5′-guanylylimidodiphosphate, amiloride and ethylisopropylamiloride Evidence for receptor G-protein precoupling . J Pharmacol Exp Ther. 252:1990;1184-1196.
28. 2 receptors by sodium and pH. Mol Pharmacol. 39:1991;570-578.
29. 2 dopamine receptors by amiloride and amiloride analogs. Mol Pharmacol. 50:1996;1295-1308.
30. Hou X., Wehrle J., Menge W., Ciccarelli E., Wess J., Mutschler E., Lambrecht G., Timmerman H., Waelbroeck M. Influence of monovalent cations on the binding of a charged and an uncharged (′carbo′-)muscarinic antagonist to muscarinic receptors. Br J Pharmacol. 117:1996;955-961.
31. + exchange independent of cAMP. J Biol Chem. 265:1990;8989-8992.
32. Jacobson K.A., van Galen P.J., Williams M. Adenosine receptors Pharmacology, structure-activity relationships, and therapeutic potential . J Med Chem. 35:1992;407-422.
33. 1 adenosine receptors. Two amino acids are responsible for species differences in ligand recognition. J Biol Chem. 269:1994;27900-27906.