A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP production

Journal of Biomolecular Screening

Volumn 12, Issue 8, 2007, Pages 1074-1083

  Kool, Jeroen ^a   Van Marle, André ^a   Hulscher, Saskia ^a   Selman, Maurice ^a   Van Iperen, Dick J ^a   Van Altena, Klaas ^a   Gillard, Michel ^b   Bakker, Remko A ^a   Irth, Hubertus ^a   Leurs, Rob ^a   Vermeulen, Nico P E ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

^b UCB PHARMA   (Belgium)

Author keywords

cAMP; Flow through; Fluorescence polarization; GPCR; Histamine H3 receptor

Indexed keywords

CYCLIC AMP; CYCLIC AMP DEPENDENT PROTEIN KINASE; G PROTEIN COUPLED RECEPTOR; HISTAMINE H3 RECEPTOR AGONIST; RADIOLIGAND;

ACCURACY; ANALYTIC METHOD; ANIMAL CELL; ARTICLE; BIOASSAY; CELL ASSAY; CONTROLLED STUDY; COST EFFECTIVENESS ANALYSIS; FLUORESCENCE POLARIZATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; NONHUMAN; PRIORITY JOURNAL; PROTEIN DETERMINATION; PROTEIN DOMAIN; RADIOACTIVITY;

ANIMALS; CATTLE; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; DOSE-RESPONSE RELATIONSHIP, DRUG; FLUORESCENCE POLARIZATION; HUMANS; NUCLEOTIDES; RECEPTORS, G-PROTEIN-COUPLED; REPRODUCIBILITY OF RESULTS;

EID: 36549039577     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057107308881     Document Type: Article

References (35)

1. Carnero A.: High throughput screening in drug discovery. Clin Transl Oncol 2006 ; 8: 482-490.
2. Koehn FE, Carter GT: The evolving role of natural products in drug discovery. Nat Rev Drug Discov 2005 ; 4: 206-220.
3. Geysen HM, Schoenen F., Wagner D., Wagner R.: Combinatorial compound libraries for drug discovery: an ongoing challenge. Nat Rev Drug Discov 2003 ; 2: 222-230.
4. Sportsman JR, Daijo J., Gaudet EA: Fluorescence polarization assays in signal transduction discovery. Comb Chem High Throughput Screen 2003 ; 6: 195-200.
5. Eglen RM: Functional G protein-coupled receptor assays for primary and secondary screening. Comb Chem High Throughput Screen 2005 ; 8: 311-318.
6. Lundstrom K.: Latest development in drug discovery on G protein-coupled receptors. Curr Protein Pept Sci 2006 ; 7: 465-470.
7. Luttrell LM: Transmembrane signaling by G protein-coupled receptors. Methods Mol Biol 2006 ; 332: 3-49.
8. Scott JD: Compartmentalized cAMP signalling: a personal perspective. Biochem Soc Trans 2006 ; 34: 465-467.
9. Jacoby E., Bouhelal R., Gerspacher M., Seuwen K.: The 7 TM G-protein-coupled receptor target family. ChemMedChem 2006 ; 1: 761-782.
10. Gales C., Rebois RV, Hogue M., Trieu P., Breit A., Hebert TE,, et al. Real-time monitoring of receptor and G-protein interactions in living cells. Nat Methods 2005 ; 2: 177-184.
11. Williams C.: cAMP detection methods in HTS: selecting the best from the rest. Nat Rev Drug Discov 2004 ; 3: 125-135.
12. Prystay L., Gagne A., Kasila P., Yeh LA, Banks P.: Homogeneous cell-based fluorescence polarization assay for the direct detection of cAMP. J Biomol Screen 2001 ; 6: 75-82.
13. Allen M., Hall D., Collins B., Moore K.: A homogeneous high throughput nonradioactive method for measurement of functional activity of Gscoupled receptors in membranes. J Biomol Screen 2002 ; 7: 35-44.
14. Passani MB, Lin JS, Hancock A., Crochet S., Blandina P.: The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 2004 ; 25: 618-625.
15. Bakker RA: Histamine H3-receptor isoforms. Inflamm Res 2004 ; 53: 509-516.
16. Leurs R., Bakker RA, Timmerman H., de Esch IJ: The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov 2005 ; 4: 107-120.
17. Nordstedt C., Fredholm BB: A modification of a protein-binding method for rapid quantification of cAMP in cell-culture supernatants and body fluid. Anal Biochem 1990 ; 189: 231-234.
18. Takeda T., Kuno T., Shuntoh H., Tanaka C.: A rapid filtration assay for cAMP. J Biochem (Tokyo) 1989 ; 105: 327-329.
19. Das R., Esposito V., Abu-Abed M, Anand GS, Taylor SS, Melacini G: cAMP activation of PKA defines an ancient signaling mechanism. Proc Natl Acad Sci USA 2007 ; 104: 93-98.
20. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999 ; 4: 67-73.
21. Kariv II, Stevens ME, Behrens DL, Oldenburg KR: High throughput quantitation of cAMP production mediated by activation of seven transmembrane domain receptors. J Biomol Screen 1999 ; 4: 27-32.
22. Lim HD, van Rijn RM, Ling P., Bakker RA, Thurmond RL, Leurs R.: Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 2005 ; 314: 1310-1321.
23. Burke TJ, Loniello KR, Beebe JA, Ervin KM: Development and application of fluorescence polarization assays in drug discovery. Comb Chem High Throughput Screen 2003 ; 6: 183-194.
24. Allen M., Reeves J., Mellor G.: High throughput fluorescence polarization: a homogeneous alternative to radioligand binding for cell surface receptors. J Biomol Screen 2000 ; 5: 63-69.
25. Schopfer U., Engeloch C., Stanek J., Girod M., Schuffenhauer A., Jacoby E.,, et al. The Novartis compound archive: from concept to reality. Comb Chem High Throughput Screen 2005 ; 8: 513-519.
26. Ellson R., Stearns R., Mutz M., Brown C., Browning B., Harris D.,, et al. In situ DMSO hydration measurements of HTS compound libraries. Comb Chem High Throughput Screen 2005 ; 8: 489-498.
27. Suzuki S., Ohno K., Santa T., Imai K.: Study on interactions of endocrine disruptors with estrogen receptor-beta using fluorescence polarization. Anal Sci 2003 ; 19: 1103-1108.
28. van Elswijk DA, Schobel UP, Lansky EP, Irth H., van der Greef J.: Rapid dereplication of estrogenic compounds in pomegranate (Punica granatum) using on-line biochemical detection coupled to mass spectrometry Phytochemistry 2004 ; 65: 233-241.
29. Hesley J., Daijo J., Ferguson AT: Stable, sensitive, fluorescence-based method for detecting cAMP. Biotechniques 2002 ; 33: 691-694.
30. Blommel P., Hanson GT, Vogel KW: Multiplexing fluorescence polarization assays to increase information content per screen: applications for screening steroid hormone receptors. J Biomol Screen 2004 ; 9: 294-302.
31. Ozers MS, Hill JJ, Ervin K., Wood JR, Nardulli AM, Royer CA,, et al. Equilibrium binding of estrogen receptor with DNA using fluorescence anisotropy. J Biol Chem 1997 ; 272: 30405-30411.
32. Wang SY, Ahn BS, Harris R., Nordeen SK, Shapiro DJ: Fluorescence anisotropy microplate assay for analysis of steroid receptor-DNA interactions. Biotechniques 2004 ; 37: 807-808.
33. Kool J., van Liempd SM, Ramautar R., Schenk T., Meerman JH, Irth H.,, et al. Development of a novel cytochrome p450 bioaffinity detection system coupled online to gradient reversed-phase high-performance liquid chromatography. J Biomol Screen 2005 ; 10: 427-436.
34. Kool J., Eggink M., van Rossum H., van Liempd SM, van Elswijk DA, Irth H.,, et al. Online biochemical detection of glutathione-S-transferase P1-specific inhibitors in complex mixtures. J Biomol Screen 2007 ; 12: 396-405.
35. Derks RJ, Hogenboom AC, van der Zwan G., Irth H.: On-line continuous-flow, multi-protein biochemical assays for the characterization of bioaffinity compounds using electrospray quadrupole time-of-flight mass spectrometry. Anal Chem 2003 ; 75: 3376-3384.