A bioluminescent-based, HTS-compatible assay to monitor G-protein-coupled receptor modulation of cellular cyclic AMP

Assay and Drug Development Technologies

Volumn 5, Issue 2, 2007, Pages 237-245

  Kumar, Meera ^a   Hsiao, Kevin ^a   Vidugiriene, Jolanta ^a   Goueli, Said A ^a,b  

^a UNIVERSITY OF WISCONSIN SCHOOL OF MEDICINE AND PUBLIC HEALTH   (United States)

^b PROMEGA CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 CHLOROMERCURIBENZOIC ACID; ADENOSINE TRIPHOSPHATE; CYCLIC AMP; CYCLIC AMP DEPENDENT PROTEIN KINASE; EBSELEN; EPHEDRINE; G PROTEIN COUPLED RECEPTOR; HYDROQUINONE; N (2 AMINOETHYL) 5 ISOQUINOLINESULFONAMIDE; N [2 (4 BROMOCINNAMYLAMINO)ETHYL] 5 ISOQUINOLINESULFONAMIDE; RECEPTOR BLOCKING AGENT;

ACCURACY; ARTICLE; BIOASSAY; BIOLUMINESCENT BASED HIGH THROUGHPUT SCREENING COMPATIBLE ASSAY; CONTROLLED STUDY; EMBRYO; ENZYME ACTIVITY; ENZYME MECHANISM; HUMAN; HUMAN CELL; MONITORING; NUCLEOTIDE SEQUENCE; PLATE COUNT; PROTEIN ANALYSIS; RECEPTOR INTRINSIC ACTIVITY; REGULATORY MECHANISM; REPRODUCIBILITY;

CELL LINE; CYCLIC AMP; DRUG EVALUATION, PRECLINICAL; FORSKOLIN; GTP-BINDING PROTEIN ALPHA SUBUNITS, GI-GO; GTP-BINDING PROTEIN ALPHA SUBUNITS, GS; HUMANS; LUMINESCENCE; RECEPTORS, DOPAMINE D1; RECEPTORS, DOPAMINE D2; RECEPTORS, G-PROTEIN-COUPLED; ROBOTICS;

EID: 34247586570     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2006.055     Document Type: Article

References (24)

1. Ellis C: The state of GPCR research in 2004. Nat Rev Drug Discov 2004;3:577-626.
2. Raiteri M: Functional pharmacology in human brain. Pharmacol Rev 2006;58:162-193
3. Milligan G, Kostenis E: Heterotrimeric G-proteins: a short history. Br J Pharmacol 2006;147(Suppl):S46-S55.
4. Eglen RM: An overview of high throughput screening at G protein coupled receptors. Front Drug Des Discov 2005; 1:97-111.
5. Leifert WR, Aloia ML, Bucco O, Glatz, RV, McMurchie EJ: G-protein-coupled receptors in drug discovery: nanosizing using cell-free technologies and molecular biology approaches. J Biomol Screen 2005;10:765-779.
6. Thomsen W, Frazer J, Unett D: Functional assays for screening GPCR targets. Curr Opin Biotechnol 2005;16: 655-665.
7. Niedernberg A, Tunaru S, Blaukat A, Harris B, Kostenis E: Comparative analysis of functional assays for characterization of agonist ligands at G protein-coupled receptors. J Biomol Screen 2003;8:500-510.
8. Dinger MC, Beck-Sickinger AG: The first reporter gene assay on living cells. Green fluorescent protein as reporter gene for the investigation of Gi-protein coupled receptors. Mol Biotechnol 2002;21:9-18.
9. Roeder T, Görich D, Heyden D, Gewecke M: A green-fluorescent- protein-based assay for the characterization of G-protein-coupled receptors. Anal Biochem 2004;332:38-45.
10. Wise A, Jupe SC, Rees S: The identification of ligands at orphan G-protein coupled receptors. Annu Rev Pharmacol Toxicol 2004;44:43-66.
11. Gabriel D, Vernier M, Pfeifer MJ, Dasen B, Tanaillon L, Bouhelal R: High throughput screening technologies for direct cyclic AMP measurement. Assay Drug Dev Technol 2003;1:291-303.
12. Williams C: cAMP detection methods in HTS: selecting the best from the rest. Nat Rev Drug Discov 2004;3:125-135.
13. Kupcho K, Somberg R, Bulleit B, Goueli SA: A homogeneous, nonradioactive high-throughput fluorogenic protein kinase assay. Anal Biochem 2003;317:210-217.
14. Goueli BS, Hsiao K, Tereba A, Goueli SA: A novel and simple method to assay the activity of individual protein kinases in a crude tissue extract. Anal Biochem 1995;225: 10-17.
15. Goueli SA, Hsiao K, Bulleit B: A homogeneous, luminescent, high-throughput, versatile assay for a wide range of kinases. In: Handbook of Assay Development in Drug Discovery (Minor LK, ed.), pp. 97-111. CRC Taylor & Francis, Boca Raton, FL, 2006.
16. Taylor SS, Kim C, Vigil D, Haste NM, Yang J, Wu J, et al.: Dynamics of signaling by PKA. Biochim Biophys Acta 2005;1754:25-37.
17. Zhang J-H, Chung TDY, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4: 67-73.
18. Gola R, Seethala R: A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonists. J Biomol Screen 2002;7:515-525.
19. Ryman-Rasmussen JP, Nichols DE, Mailman RB: Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists. Mol Pharmacol 2005;68:1039-1048.
20. Iorio LC, Barnett A, Leitz FH, Houser VP, Korduba CA: SCH 23390, a potential benzazepine antipsychotic with unique interactions on dopaminergic systems. J Pharmacol Exp Ther 1983;226:462-468.
21. 3H]quinpirole binding to D2-like dopamine receptors in rat brain. J Pharmacol Exp Ther 1992;262:929-935.
22. Weber M, Ferrer M, Zheng W, Inglese J, Strulovici B, Kunapuli P: A 1,536-well cAMP assay for Gs- and Gi-coupled receptors using enzyme fragmentation complementation Assay Drug Dev Technol 2004;2:39-49.
23. 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain. Biochem Pharmacol 1985;34:2251-2259.
24. Hall H, Kohler C, Gawell L, Farde L, Sedvall G: Raclopride, a new selective ligand for the dopamine-D2 receptors. Prog Neuropsychopharmacol Biol Psychiatry 1988; 12:559-568.