Multiplex GPCR assay in reverse transfection cell microarrays

Journal of Biomolecular Screening

Volumn 9, Issue 3, 2004, Pages 196-207

  Mishina, Yuji M ^a   Wilson, Christopher J ^a   Bruett, Linda ^a   Smith, Jesse J ^a   Stoop Myer, Chatanika ^a   Jong, Sena ^a   Amaral, Lizabeth P ^a   Pedersen, Robin ^a   Lyman, Susan K ^a   Myer, Vic E ^a   Kreider, Brent L ^a   Thompson, Craig M ^a  

^a Akceli Inc   (United States)

Author keywords

Cell microarray; GPCR de orphaning; GPCR drug discovery; Multiplexed assay; Reverse transfection

Indexed keywords

8 CHLORO 2,3,4,5 TETRAHYDRO 3 METHYL 5 PHENYL 1H 3 BENZAZEPIN 7 OL HYDROGEN MALEATE; ALPHA CHEMOKINE; CARBACHOL; CORTICOTROPIN; FENOLDOPAM; FLUPHENAZINE; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR AGONIST; G PROTEIN COUPLED RECEPTOR ANTAGONIST; HISTAMINE; KALLIDIN DERIVATIVE; LIGAND; MACROPHAGE INFLAMMATORY PROTEIN 3ALPHA; N [5 (4,5 DIHYDRO 1H IMIDAZOL 2 YL) 5,6,7,8 TETRAHYDRO 2 HYDROXY 1 NAPHTHYL]METHANESULFONAMIDE; NANOPARTICLE; OREXIN B; PIRENZEPINE; PROPIONIC ACID; RANTES; SALBUTAMOL; STROMAL CELL DERIVED FACTOR 1; UNCLASSIFIED DRUG; URIDINE DIPHOSPHATE; GUANINE NUCLEOTIDE BINDING PROTEIN;

ARTICLE; CALCIUM CELL LEVEL; CALCIUM MOBILIZATION; CALCIUM TRANSPORT; CONTROLLED STUDY; DNA MICROARRAY; DOSE RESPONSE; DRUG POTENCY; DRUG SELECTIVITY; DRUG TARGETING; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LIGAND BINDING; MICROPLATE; MULTIPLEXED ASSAY; PRIORITY JOURNAL; PROTEIN DETERMINATION; PROTEIN FAMILY; PROTEIN INTERACTION; QUANTITATIVE ANALYSIS; REVERSE TRANSFECTION; TITRIMETRY; VALIDATION PROCESS; DRUG ANTAGONISM; DRUG POTENTIATION; DRUG SCREENING; GENETICS; INSTRUMENTATION; METHODOLOGY; PROTEIN MICROARRAY;

DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; GTP-BINDING PROTEINS; HUMANS; LIGANDS; PROTEIN ARRAY ANALYSIS; RECEPTORS, G-PROTEIN-COUPLED; TRANSFECTION;

EID: 7044247678     PISSN: 10870571     EISSN: None     Source Type: Journal    
DOI: 10.1177/1087057103261880     Document Type: Article

References (31)

1. Vassilatis DK, Hohmann JG, Zeng H, et al: The G protein-coupled receptor repertoires of human and mouse. Proc Natl Acad Sci U S A 2003;100:4903-4908.
2. Wise A, Gearing K, Rees S: Target validation of G-protein coupled receptors. Drug Discov Today 2002;7:235-246.
3. 16 couple a wide variety of receptors to phospholipase C. J Biol Chem 1995;270:15175-15180.
4. Neves SR, Ram PT, Iyengar R: G protein pathways. Science 2002;296:1636-1639.
5. i-coupled receptors. Anal Biochem 1999;270:242-248.
6. Milligan G, Rees S: Chimeric Gα proteins: their potential use in drug discovery. Trends Pharmacol Sci 1999;20:118-124.
7. i-coupled receptors. Mol Pharmacol 2000;57:13-23.
8. 16/z chimeras efficiently link a wide range of G protein-coupled receptors to calcium mobilization. J Biomol Screen 2003;8:39-49.
9. Chambers JK, Macdonald LE, Sarau HM, et al: A G protein-coupled receptor for UDP-glucose. J Biol Chem 2000;275:10767-10771.
10. Elshourbagy NA, Ames RS, Fitzgerald LR, et al: Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor. J Biol Chem 2000;275:25965-25971.
11. Ziauddin J, Sabatini DM: Microarrays of cells expressing defined cDNAs. Nature 2001;411:107-110.
12. Watling KJ (ed): The Sigma-RBI Handbook of Receptor Classification and Signal Transduction 4th ed. Natick, MA: Sigma-RBI, 2001.
13. He R, Tan L, Browning DD, Wang JM, Ye RD: The synthetic peptide Trp-Lys-Tyr-Met-Val-D-Met is a potent chemotactic agonist for mouse formyl peptide receptor. J Immunol 2000;165:4598-4605.
14. Matloubian M, David A, Engel S, Ryan JE, Cyster JG: A transmembrane CXC chemokine is a ligand for HIV-coreceptor Bonzo. Nat Immunol 2000;1:298-304.
15. Sandmann J, Peralta EG, Wurtman RJ: Coupling of transfected muscarinic acetylcholine receptor subtypes to phospholipase D. J Biol Chem 1991;266:6031-6034.
16. Brauner-Osborne H, Brann MR: Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): high throughput assays in mammalian cells. Eur J Pharmacol 1996;295:93-102.
17. Ellis KE, Mistry R, Boyle JP, Challiss RA: Correlation of cyclic AMP accumulation and relaxation actions of salmeterol and salbutamol in bovine tracheal smooth muscle. Br J Pharmacol 1995;116:2510-2516.
18. 1 cells. J Pharmacol Exp Ther 1991;258:193-198.
19. Knepper SM, Buckner SA, Brune ME, DeBemardis JF, Meyer MD, Hancock AA: A-61603, a potent alpha1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype. J Pharmacol Exp Ther 1995;274:97-103.
20. Burnstein ES, Spalding TA, Brann MR: Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol Pharmacol 1997;51:312-319.
21. + exchanger activity in rat ventricular myocytes. Circ Res 1998;82:1078-1085.
22. Bymaster FP, Calligaro DO, Falcone JF: Arachidonic acid release in cell lines transfected with muscarinic receptors: a simple functional assay to determine response of agonists. Cell Signal 1999;11:405-413.
23. 2 adrenoceptor agonists on changes in intracellular cyclic AMP and on cyclic AMP driven gene expression in cultured human airway smooth muscle cells. Br J Pharmacol 1999;128:721-729.
24. Hensler JG, Cotterell DJ, Dubocovich ML: Pharmacological and biochemical characterization of the D-1 dopamine receptor mediating acetylcholine release in rabbit retina. J Pharmacol Exp Ther 1987;243:857-867.
25. Dorje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Bran MR: Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther 1991;256:727-733.
26. + (GIRK) channel expressed in Xenopus oocytes. Br J Pharmacol 1998;123:421-426.
27. Felder CC, Porter AC, Skillman TL, et al: Elucidating the role of muscarinic receptors in psychosis. Life Sci 2001;68:2605-2613.
28. Mirza NR, Peters D, Sparks RG: Xanomeline and the antipsychotic potential of muscarinic receptor subtype: selective agonists. CNS Drug Rev 2003;9:159-186.
29. George SR, O'Dowd BF, Lee PL: G-protein-coupled receptor oligomerization and its potential for drug discovery. Nature Rev Drug Discov 2002;1:808-820.
30. Zlokarnik G, Negulescu PA, Knapp TE, et al: Quantitation of transcription and clonal selection of single living cells with β-lactamase as reporter. Science 1998;279:84-88.
31. Cacace A, Banks M, Spicer T, et al: An ultra-HTS process for the identification of small molecule modulators of orphan G-protein-coupled receptors. Drug Discov Today 2003;8:785-792.