Functional assay and high throughput screening for G-protein coupled receptors

Chinese Pharmacological Bulletin

Volumn 19, Issue 12, 2003, Pages 1330-1336

  Xu, Zhi Liang ^a,c   Gao, Hong ^a   Ou Yang, Ke Qing ^a   Zheng, Xu Xu ^a   Cai, Zhao Xi ^a   Hu, Ying He ^b  

^a CHONGQING UNIVERSITY   (China)

^b EAST CHINA NORMAL UNIVERSITY   (China)

^c Chem Department of Huaihua College   (China)

Author keywords

Functional assay; G protein coupled receptor; High throughput screening(HTS)

Indexed keywords

G PROTEIN COUPLED RECEPTOR;

ARTICLE; ASSAY; DRUG TARGETING; ENZYME LINKED IMMUNOSORBENT ASSAY; FLUORESCENCE POLARIZATION; FLUOROMETRY; HIGH THROUGHPUT SCREENING; LIGAND BINDING; PROTEIN DETERMINATION; PROTEIN TARGETING; RECEPTOR INTRINSIC ACTIVITY; REPORTER GENE; SCINTILLATION; SIGNAL TRANSDUCTION;

EID: 0347024363     PISSN: 10011978     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (25)

1. Landro JA, Taylor IC, Stirtan WG et al. HTS in the new millennium: The role of pharmacology and flexibility. J Pharmacol Toxicol Methods. 2000;44(1):273-89
2. Mellentin-Michelotti J, Evangelista LT, Swartzman EE et al. Determination of ligand binding affinities for endogenous seven-transmembrane receptors using fluorometric microvolume assay technology. Anal Biochem, 1999;272(2):182-90
3. Banks P, Gosselin M, Prystay L. Fluorescence polarization assays for high throughput screening of G protein-coupled receptors. J Biomol Screen, 2000;5(3):159-68
4. Chiulli AC, Trompeter K, Palmer M. A novel high throughput chemiluminescent assay for the measurement of cellular cyclic adenosine monophosphate levels. J Biomol Screen, 2000;5(4): 239-48
5. Cook ND, Jessop RA, Robinson PS et al. Scintillation proximity enzyme assay. A rapid and novel assay technique applied to HIV proteinase. Adv Exp Med Biol, 1991;306:525-8
6. Nuttall ME, Lee JC, Murdock PR et al. Amphibian melanophore technology as a functional screen for antagonists of G-protein coupled 7-transmembrane receptors. J Biomol Screen, 1999;4(5):269-78
7. Lerner MR. Tools for investigating functional interactions between ligands and G-protein-coupled receptors. Trends Neurosci, 1994;17(4):142-6
8. Terstappen GC, Giacometti A, Ballini E, Aldegheri L. Development of a functional reporter gene HTS assay for the identification of mGluR7 modulators. J Biomol Screen, 2000;5(4): 255-62
9. Goetz AS, Andrews JL, Littleton TR, Ignar DM. Development of a facile method for high throughput screening with reporter gene assays. J Biomol Screen, 2000;5(5):377-84
10. Weyer U, Schafer R, Himmler A et al. Establishment of a cellular assay system for G protein-linked receptors: Coupling of human NK2 and 5-HT2 receptors to phospholipase C activates a luciferase reporter gene. Receptors Channels, 1993;1(3):193-200
11. Kotarsky K, Owman C, Olde B. A chimeric reporter gene allowing for clone selection and high-throughput screening of reporter cell lines expressing G-protein-coupled receptors. Anal Biochem, 2001;288(2):209-15
12. Durocher Y, Perret S, Thibaudeau E et al. A reporter gene assay for high-throughput screening of G-protein-coupled receptors stably or transiently expressed in HEK293 EBNA cells grown in suspension culture. Anal Biochem, 2000;284(2):316-26
13. Fitzgerald LR, Mannan IJ, Dytko GM et al. Measurement of responses from Gi-, Gs-, or Gq-coupled receptors by a multiple response element/cAMP response element-directed reporter assay. Anal Biochem, 1999;275(1):54-61
14. Li X, Zhao X, Fang Y et al. Generation of destabilized green fluorescent protein as a transcription reporter. J Biol Chem, 1998;273(52):34970-5
15. Stratowa C, Machat H, Burger E et al. Functional characterization of the human neurokinin receptors NK1, NK2, and NK3 based on a cellular assay system. J Recept Signal Transduct Res, 1995;15(1-4):617-30
16. Naylor LH. Reporter gene technology: The future looks bright. Biochem Pharmacol, 1999;58(5):749-57
17. Zlokarnik G, Negulescu PA, Knapp TE et al. Quantitation of transcription and clonal selection of single living cells with beta-lactamase as reporter. Science, 1998;279(5347):84-8
18. Jiang C, Chen G, Zeng X et al. Generation of a bioactive neuropeptide in a cell-free system. Anal Biochem, 2003;316(1):34 -40
19. Takahashi A, Camacho P, Lechleiter JD, Herman B. Measurement of intracellular calcium. Physiol Rev, 1999;79(4):1089-125
20. 2+] using the fluorometric imaging plate reader (FLIPR). Methods Mol Biol, 1999;114:125-33
21. George CH, Kendall JM, Campbell AK, Evans WH. Connexin-aequorin chimerae report cytoplasmic calcium environments along trafficking pathways leading to gap junction biogenesis in living COS-7 cells. J Biol Chem, 1998;273(45):29822-9
22. 2+ mobilization. Cell Calcium, 1993;14 (9):663-71
23. Sandberg K, Markwick AJ, Trinh DP, Catt KJ. Calcium mobilization by angiotensin II and neurotransmitter receptors expressed in Xenopus laevis oocytes. FEBS Lett, 1988;241(12):177-80
24. Grant SK, Bansal A, Mitra A et al. Delay of intracellular calcium transients using a calcium chelator: application to high-throughput screening of the capsaicin receptor ion channel and G-protein-coupled receptors. Anal Biochem, 2001;294(1):27-35