Combination of receptor-binding assays and designed mutant receptors for discerning agonists and antagonists

Journal of Pharmaceutical and Biomedical Analysis

Volumn 43, Issue 3, 2007, Pages 822-828

  Matsui, Kazuhiro ^a  

^a Yokohama Laboratory   (Japan)

Author keywords

Agonist; Antagonist; Endocrine disrupting chemicals; High throughput screening; Human estrogen receptor; Ligand binding domain; Mutant receptors; Pharmaceutical drug; Receptor binding assay; Relative binding affinity

Indexed keywords

17ALPHA ESTRADIOL; 4,4' ISOPROPYLIDENEDIPHENOL; DAIDZEIN; DIETHYLSTILBESTROL; ENDOCRINE DISRUPTOR; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; GENISTEIN; HYBRID PROTEIN; HYDROXYTAMOXIFEN; MALTOSE BINDING PROTEIN; MUTANT PROTEIN; NONYLPHENOL; TAMOXIFEN;

ARTICLE; BINDING AFFINITY; BINDING ASSAY; DRUG DETERMINATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; IC 50; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN STRUCTURE; STRUCTURE ANALYSIS; WILD TYPE;

BINDING, COMPETITIVE; CARRIER PROTEINS; DNA; DNA PRIMERS; DNA, COMPLEMENTARY; ENDOCRINE DISRUPTORS; ESCHERICHIA COLI; ESTRADIOL CONGENERS; ESTROGEN RECEPTOR ALPHA; GENETIC VECTORS; HUMANS; MUTATION; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECOMBINANT FUSION PROTEINS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION;

EID: 33846700711     PISSN: 07317085     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jpba.2006.09.023     Document Type: Article

References (27)

1. McLeod D.G. Cancer 71 (1993) 1046-1049
2. Katzenellenbogen B.S., Choi I., Delage-Mourroux R., Ediger T.R., Martini P.G., Montano M., Sun J., Weis K., and Katzenellenbogen J.A. J. Steroid Biochem. Mol. Biol. 74 (2000) 279-285
3. Guzzo J.A. Clin. Cardiol. 23 (2000) 15-17
4. Kleerekoper M., and Schein J.R. J. Clin. Pharmacol. 41 3 (2001) 239-250
5. Dhingra K. Cancer Invest. 19 (2001) 649-659
6. Ahrens H., Schuh T.J., Rainish B.L., Furlow J.D., Gorski J., and Mueller C. Receptor 2 (1992) 77-92
7. Apriletti J.W., Baxter J.D., Lau K.H., and West B.L. Protein Expr. Purif. 6 (1995) 363-370
8. Chang C., Wang C., Deluca H.F., Ross T.K., and Shih C.C.-Y. Proc. Natl. Acad. Sci. U.S.A. 89 (1992) 5946-5950
9. Pakdel F., Petit F., Anglade I., Kah O., Delaunay F., Bailhache T., and Valotaire Y. Mol. Cell. Endocrinol. 104 (1994) 81-93
10. Roehrborn C.G., Zoppi S., Gruber J.A., Wilson C.M., and McPhaul M.J. Mol. Cell. Endocrinol. 2 (1992) 1-14
11. Brozozowski A.M., Pike A.C.W., Dauter Z., Hubbard R.E., Bonn T., Engstöm O., Öhman L., Greene G.L., Gustafsson J., and Cariquist M. Nature 389 (1997) 753-758
12. Lally J.M., Newman R.H., Knowles P.P., Islam S., Coffer A.I., Parker M., and Freemont P.S. Acta Crystallogr. D54 (1997) 423-426
13. Shiau A.K., Barstad D., Loria L.C., Krushner P.J., Agard D.A., and Greene G.L. Cell 95 (1998) 927-937
14. Pike A.C.W., Brzozowski A.M., Hubbard R.E., Bonn T., Thorsell A., Engstrom O., Ljunggren J., Gustafsson J., and Carlquist M. Eur. Mol. Biol. Organ. 18 (1999) 4608-4618
15. Matias P.M., Donner P., Coelho R., Thomaz M., Peixoto C., Macedo S., Otto N., Joschko P., Scholz P., Wegg A., Bäsler S., Schäfer M., Egner U., and Carrondo M.A. J. Biol. Chem. 275 (2000) 26164-26171
16. Gangloff M., Ruff M., Eiler S., Duclaud S., Wurtz J.M., and Moras D.J. J. Biol. Chem. 276 (2001) 15059-15065
17. Levenson A.S., and Jordan Y.C. Cancer Res. 58 (1998) 1872-1875
18. Coldham N., Dave M., Sivapathasundaram S., McDonnell D., Connor C., and Sauer M. Environ. Health Perspect. 105 (1997) 734-742
19. Pons M., Gagne D., Nicolas J.C., and Mehtali M. Biotechniques 9 4 (1990) 450-459
20. Reel J.R., Lamb IV J.C., and Neal B.H. Fundam. Appl. Toxicol. 34 (1996) 288-305
21. Ausubel F.M., Brent R., Kingston R., Moore D., Seidman J.J., Smith J., and Struhl K. Current Protocols in Molecular Biology (1987-1994), Greene & Wiley, New York unit 16.6.1-unit 16.6.14
22. Sambrook J., and Russell D.W. Molecular Cloning. third ed. (2001), Cold Spring Harbor Laboratory Press, Cold Spring Harbor, New York
23. Tora L., Mullick A., Metzger D., Ponglikitmongkol M., Park I., and Chambon P. EMBO 8 (1989) 1981-1986
24. Lieberman M.E., Goraki J., and Jordan V.C. J. Biol. Chem. 258 (1983) 4741-4745
25. Bissantz C., Folkers G., and Rognan D. J. Med. Chem. 43 (2000) 4759-4767
26. Orry A.J., Abagyan R.A., and Cavasotto C.N. Drug Discov. Today 11 (2006) 261-266
27. Parker G.J., Law T.L., Lenoch F.J., and Bolger R.E. J. Biomol. Screen. 5 (2000) 77-88