Identification of essential residues involved in the allosteric modulation of the human A3 adenosine receptor

Molecular Pharmacology

Volumn 63, Issue 5, 2003, Pages 1021-1031

  Gao, Zhan Guo ^a   Kim, Soo Kyung ^a   Gross, Ariel S ^a   Chen, Aishe ^a   Blaustein, Joshua B ^a   Jacobson, Kenneth A ^a  

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

Author keywords

[No Author keywords available]

Indexed keywords

2 CYCLOPENTYL 4 PHENYLAMINO 1H IMIDAZO[4,5 C]QUINOLINE; 4 ANILINO 2 CYCLOPENTYLIMIDAZO[4,5 C]QUINOLINE; 4 METHOXY N [7 METHYL 3 (2 PYRIDINYL) 1 ISOQUINOLINYL]BENZAMIDE; 5 (N,N HEXAMETHYLENE)AMILORIDE; 8 ETHYL 4 METHYL 2 PHENYL 4,5,7,8 TETRAHYDRO 1H IMIDAZO[2,1 I]PURIN 5 ONE; ADENOSINE A3 RECEPTOR; ADENOSINE A3 RECEPTOR AGONIST; ADENOSINE A3 RECEPTOR ANTAGONIST; AMINO ACID DERIVATIVE; IMIDAZOQUINOLINE DERIVATIVE; ISOQUINOLINE DERIVATIVE; N 6 (4 AMINO 3 IODOBENZYL) 5' N METHYLCARBOXAMIDOADENOSINE; PSB 11; RHODOPSIN; SODIUM CHLORIDE; SODIUM ION; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING SITE; CONTROLLED STUDY; DISSOCIATION; DRUG RECEPTOR BINDING; GENE MUTATION; LIGAND BINDING; MOLECULAR MODEL; MUTANT; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ANALYSIS;

ADENOSINE; ALLOSTERIC REGULATION; AMINO ACID MOTIFS; ANIMALS; COS CELLS; HUMANS; IMIDAZOLES; IODINE RADIOISOTOPES; MODELS, MOLECULAR; MUTATION; PROTEIN STRUCTURE, TERTIARY; PURINES; RADIOLIGAND ASSAY; RECEPTOR, ADENOSINE A3; RECEPTORS, PURINERGIC P1; SODIUM; TRITIUM;

EID: 0038407477     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.63.5.1021     Document Type: Article

References (40)

1. Angeli P, Marucci G, Buccioni M, Piergentili A, Giannella M, Quaglia W, Pigini M, Cantalamessa F, Nasuti C, Novi F, et al. (2002) Deoxamuscaroneoxime derivatives as useful muscarinic agonists to explore the muscarinic subsite: Demox, a modulator of orthosteric and allosteric sites at cardiac muscarinic M2 receptors. Life Sci 70:1427-1446.
2. 1 adenosine receptors: influences of acidic and hydroxy residues in the first four transmembrane domains on ligand binding. Mol Pharmacol 50:1635-1642.
3. Beukers MW, Kristiansen K, IJzerman AP and Edvardsen Ø. (1999) TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data. Trends Pharmacol Sci 20:475-477.
4. Birdsall NJ, Lazareno S, Popham A, and Saldanha J (2001) Multiple allosteric sites on muscarinic receptors. Life Sci 68:2517-2524.
5. Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
6. 1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol Pharmacol 38:939-949.
7. Buller S, Zlotos DP, Mohr K, and Ellis J (2002) Allosteric site on muscarinic acetylcholine receptors: a single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium ligands. Mol Pharmacol 61:160-168.
8. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
9. Christopoulos A (2002) Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat Rev Drug Disc 1:198-210.
10. Christopoulos A and Kenakin T (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
11. Christopoulos A, Lanzafame A, and Mitchelson F (1998) Allosteric interactions at muscarinic cholinoceptors. Clin Exp Pharmacol Physiol 25:185-194.
12. 2+ sensing receptor. Trends Pharmacol Sci 21:401-407.
13. Cullen BR (1987) Use of eukaryotic expression technology in the functional analysis of cloned genes. Methods Enzymo 152:684-704.
14. 2A adenosine receptors by amiloride analogues and sodium ions. Biochem Pharmacol 60:669-676.
15. 3 adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives. Mol Pharmacol 60:1057-1063.
16. Gao ZG, Chen A, Barak D, Kim S-K, Müller CE, and Jacobson KA (2002a) Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human As adenosine receptor. J Biol Chem 277:19056-19063.
17. 3 adenosine receptors by a series of imidazoquinoline derivatives. Mol Pharmacol 62:81-89.
18. 3 adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. J Med Chem 45:4471-4484.
19. 3 adenosine receptors. Biochem Pharmacol, 65:525-534.
20. Gnagey AL, Seidenberg M, and Ellis J (1999) Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors. Mol Pharmacol 56:1245-1253.
21. 2-adrenergic receptors by sodium. J Biol Chem 265:21590-21595.
22. 3 receptor with selectively enhanced affinity for amine-modified nucleosides. J Med Chem 44:4125-4136.
23. Judson R (1997) Genetic algorithms and their use in chemistry. Rev Comput Chem 10:1-73.
24. 1 receptor. Biochem Pharmacol 61:137-144.
25. Leppik RA, Miller RC, Eck M, and Paquet JL (1994) Role of acidic amino acids in the allosteric modulation by gallamine of antagonist binding at the m2 muscarinic acetylcholine receptor. Mol Pharmacol 45:983-990.
26. 2A-adrenoceptor: allosteric modulation by amilorides. Mol Pharmacol 58:10911099.
27. Linden J (1997) Allosteric enhancement of adenosine receptors, in Purinergic Approaches in Experimental Therapeutics (Jacobson KA and Jarvis MF eds), pp 85-97, Wiley-Liss Inc., New York.
28. A receptor channels. Annu Rev Neurosci 17:569-602.
29. Martin S, Botto JM, Vincent JP, and Mazella J (1999) Pivotal role of an aspartate residue in sodium sensitivity and coupling to G proteins of neurotensin receptors. Mol Pharmacol 55:210-215.
30. Martin Y, Burses M, Dahaner E, DeLazzer J, Lico I, and Pavlik P (1993) A fast approach to pharmacophore mapping and its application to dopaminergic and benzodiazepine agonists. J Comput-Aided Mol Des 7:83-102.
31. Matsui H, Lazareno S, and Birdsall NJ (1995) Probing of the location of the allosteric site on ml muscarinic receptors by site-directed mutagenesis. Mol Pharmacol 47:88-98.
32. 2 receptor. Mol Pharmacol 60:373-381.
33. 3 adenosine receptors. Bioorg Med Chem Lett 12:501-503.
34. Olin J and Schneider L (2002) Galantamine for Alzheimer's disease. Cochrane Database Syst Rev 3:CD001747.
35. Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp TE, et al. (2000) Crystal structure of rhodopsin: a G protein-coupled receptor. Science (Wash DC) 289:739-745.
36. Ryckaert JP, Ciccotti G, and Berendsen HJC (1977) Numerical integration of the cartesian equations of motion for a system with constraints: molecular dynamics of n-alkanes. J Comput Phys 23:327-333.
37. Schetz JA and Sibley DR (2001) The binding-site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation. J Pharmacol Exp Ther 296:359-363.
38. 2 receptor and its testing by docking of agonists and tricyclic antagonists. J Med Chem 37:2874-2888.
39. van Rhee AM and Jacobson KA (1996) Molecular architecture of G protein-coupled receptors. Drug Dev Res 37:1-38.
40. Wess J (1993) Mutational analysis of muscarinic acetylcholine receptors: structural basis of ligand/receptor/G protein interactions. Life Sci 53:1447-1463.