A short-incubation reporter-gene assay for high-throughput screening of estrogen receptor-α antagonists

Assay and Drug Development Technologies

Volumn 3, Issue 4, 2005, Pages 393-400

  Shi, Xiaoqing ^a   Zheng, Wei ^a   Schneeweis, Jonathan E ^a   Fischer, Paul A ^a   Strulovici, Berta ^a   Peekhaus, Norbert T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIESTROGEN; CELL NUCLEUS RECEPTOR; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FULVESTRANT; LIGAND; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN;

ANIMAL CELL; ARTICLE; BREAST CANCER; CELL ASSAY; CONTROLLED STUDY; DRUG DETERMINATION; DRUG SYNTHESIS; ENZYME ASSAY; HIGH THROUGHPUT SCREENING; HUMAN; INCUBATION TIME; NONHUMAN; OSTEOPOROSIS; REPORTER GENE; SIDE EFFECT;

ANIMALS; BETA-LACTAMASES; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ESTRADIOL; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; FLUORESCENCE RESONANCE ENERGY TRANSFER; GENETIC VECTORS; RALOXIFENE; RECOMBINANT FUSION PROTEINS; SELECTIVE ESTROGEN RECEPTOR MODULATORS; TAMOXIFEN; TRANS-ACTIVATION (GENETICS); TRANSCRIPTION FACTORS; TRANSCRIPTIONAL ACTIVATION; TRANSFECTION;

EID: 27144458781     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2005.3.393     Document Type: Article

References (20)

1. Gruber CJ, Tschugguel W, Schneeberger C, Huber JC: Production and actions of estrogens. N Engl J Med 2002; 346:340-352.
2. Gustafsson J-A: What pharmacologists can learn from recent advances in estrogen signaling. Trends Pharmacol Sci 2003;24:479-485.
3. Korach KS, Migiaccio S, Davis VL. Estrogens. In: Principles of Pharmacology (Munson PL, ed.), pp. 809-825. Chapman & Hall, New York, 1996.
4. Kuiper GGJM, Enmark E, Petto-Huikko M, Nilson S, Gustafsson J-A: Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci U S A 1996;93:5925-5930.
5. Katzenellenbogen BS, Montano MM, Ediger TR, Sun J, Ekena K, Lazennec G, Martini PG, Delage-Mourroux R, Weis K, Katzenellenbogen JA: Estrogen receptors: Selective ligands, partners, and distinctive pharmacology. Recent Prog Horm Res 2000;55:163-193.
6. Cowley SM, Hoare S, Mosselman S, Parker MG: Estrogen receptors alpha and beta form heterodimers on DNA. J Biol Chem 1997;272:19858-19862.
7. Paech K, Webb P, Kuiper GG, Nilson S, Gustafsson J, Kushner PJ, Scanlan TS: Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP-I sites. Science 1997;277:1508-1510.
8. Webb PP, Nguyen C, Valentine G, Lopez N, Kwok GR, McInerney E, Katzenellenbogen BS, Enmark E, Gustafsson J-A, Nilson S, Kushner PJ: The estrogen receptor enhances AP-1 activity by two distinct mechanisms with different requirements for receptor transactivation functions. Mol Endocrinol 1999;13:1672-1685.
9. Mosselman S, Polman J, Dijkema R: ERbeta: Identification and characterization of a novel human estrogen receptor. FEBS Lett 1996;392:49-53.
10. Lindberg MK, Moverare S, Skrtic S, Gao H, Dahlman-Wright K, Gustafsson J-A, Ohlsson C: Estrogen receptor-β reduces estrogen receptor-α regulated gene transcription, supporting a "ying-yang" relationship between estrogen receptor α and β in mice. Mol Endocrinol 2003; 17:203-208.
11. Katzenellenbogen BS, Katzenellenbogen JA: Estrogen receptor transcription and transactivation: Estrogen receptor alpha and estrogen receptor beta: Regulation by selective estrogen receptor modulators and importance in breast cancer. Breast Cancer Res 2000;2:335-344.
12. Mobley JA, L'Esperance JO, Wu M, Friel CJ, Hanson RH, Ho SM: The novel estrogen 17alpha-20Z-21-[(4-amino) phenyl]-19-norpregna-1,3,5(10),20-tetraene-3,17beta-diol induces apoptosis in prostate cancer cell lines at nanomolar concentrations in vitro. Mol Cancer Ther 2004;3:587-595.
13. Prestwood KM, Gunness M, Muchmore DB, Lu Y, Wong M, Raisz LG: A comparison of the effects of raloxifene and estrogen on bone in postmenopausal women. J Clin Endocrinol Metab 2000;85:2197-2202.
14. Zlokarnik G, Negulescu PA, Knapp TE, Mere L, Burres N, Feng L, Whitney M, Roemer K, Tsein RY: Quantitation of transcription and clonal selection of single living cells with beta-lactamase as reporter. Science 1998;279:84-88.
15. Kunapuli P, Ransom R, Murphy KL, Pettibone D, Kerby J, Grimwood S, Zuck P, Hodder P, Lacson R, Hoffman I, Inglese J, Strulovici B: Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening. Anal Biochem 2003;314:16-29.
16. Cacace A, Banks M, Spicer T, Civoli F, Watson J: An ultra-HTS process for the identification of small molecule modulators of orphan G-protein-coupled receptors. Drug Discov Today 2003;8:785-792.
17. Lavery P, Brown MJ, Pope AJ: Simple absorbance-based assays for ultra-high throughput screening. J Biomol Screen 2001;6:3-9.
18. Chin J, Adams AD, Bouffard A, Green A, Lacson RG, Smith T, Fischer PA, Menke JG, Sparrow CP, Mitnaul LJ: Miniaturization of cell-based β-lactamase-dependent FRET assays to ultra-high throughput formats to identify agonists of human liver X receptors. Assay Drug Dev Technol 2003;1:777-787.
19. Peekhaus NT, Ferrer M, Chang T, Komienko O, Schneeweis JE, Smith TS, Hoffman I, Mitnaul U, Chin J, Fischer PA, Blizzard TA, Birzin ET, Chan W, Inglese J, Strulovici B, Rohrer SP, Schaeffer JM: A β-lactamase-dependent Gal4-estrogen receptor β transactivation assay for the ultra-high throughput screening of estrogen receptor β agonists in a 3,456-well format. Assay Drug Dev Technol 2003; 1:789-800.
20. Kornienko O, Lacson R, Kunapuli P, Schneeweis J, Hoffman I, Smith T, Alberts M, Inglese J, Strulovici B: Miniaturization of whole live cell-based GPCR assays using microdispensing and detection systems. J Biomol Screen 2004;9:186-189.