Minireview: Drug Discovery Using Receptors that Modulate Gene Expression

Journal of Receptor and Signal Transduction Research

Volumn 17, Issue 42007, 1997, Pages 531-543

  Lamb, Peter ^a   Rosen, Jonathan ^a  

^a LIGAND PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DEXAMETHASONE; GLUCOCORTICOID RECEPTOR;

CONFERENCE PAPER; CYTOKINE RESPONSIVE ELEMENT; GENE EXPRESSION REGULATION; GENETIC TRANSCRIPTION; HORMONE RECEPTOR INTERACTION; NONHUMAN; SIGNAL TRANSDUCTION; TRANSCRIPTION REGULATION;

ANIMALS; DNA-BINDING PROTEINS; DRUG DESIGN; GENE EXPRESSION REGULATION; HORMONES; HUMANS; LIGANDS; MODELS, MOLECULAR; PROTEIN-TYROSINE KINASES; RECEPTORS, CELL SURFACE; RECEPTORS, CYTOKINE; RECEPTORS, CYTOPLASMIC AND NUCLEAR; TRANS-ACTIVATORS; TRANSCRIPTION FACTORS;

EID: 0031026737     PISSN: 10799893     EISSN: None     Source Type: Journal    
DOI: 10.3109/10799899709036626     Document Type: Article

References (33)

1. Evans R. M. The steroid and thyroid hormone receptor superfamily. Science 1989; 240: 889 – 895
2. Mangelsdorf D. J., Thummel C., Beato M., Herrlich P., Schutz G., Umesone K., Blumberg B., Kastner P., Mark M., Chambon P., Evans R. M. The nuclear receptor superfamily: The second decade. Cell 1995; 83: 835 – 839
3. Beato M., Herrlich P., Schutz G. Steroid hormone receptors: Many actors in search of a plot. Cell 1995; 83: 851 – 857
4. Miyajama A., Kitamura T., Harada N., Yokata T., Arai K. Cytokine receptors and signal transduction. Annu. Rev. Immunol. 1992; 10: 295
5. Darnell J. E., Jr., Kerr I. M., Stark G. R. JAK-STAT pathways and transcriptional activation in response IFNs and other extracellular signaling proteins. Science 1994; 264: 1415 – 1421
6. Ihle J. N., Witthuhn B. A., Quelle F. W., Yamamoto K., Thierfelder W. E., Kreider B., Silvennoinen O. Signaling by the cytokine receptor superfamily: JAKs and STATs. Trends in Biochemical Sciences 1994; 19: 222 – 227
7. Ihle J. N. Cytokine receptor signaling. Nature 1995; 377: 591 – 594
8. Pratt W. B. Interaction of hsp90 with steroid hormone receptors: Organizing some diverse observations and presenting the newest concepts. Mol. Cell. Endocrinol. 1995; 74: C69 – C76
9. Allan G. F., Leng K., Tsai S.-Y., Weigel N. L., Edwards D. P., Tsai M.-J., O'Malley B. W. Hormone and Anti-hormone induce distinct conformational changes which are central to steroid receptor activation. J. Biol. Chem. 1992; 267: 19513 – 19520
10. Allan G. F., Tsai S.-Y., O'Malley B. W., Tsai M.-J. Steroid hormone receptors and in vitro transcription. BioEssays 1991; 13: 73 – 78
11. Glass C. K. Differential recognition of target genes by nuclear receptor monomers, dimers and heterodimers. Endocrinol. Rev. 1994; 15: 391 – 407
12. Naar A. M., Boutin J.-M., Lipkin S. M., Yu V. C., Holloway J M., Glass C. K., Rosenfeld M. G. The orientation and spacing of core DNA-binding motifs dictate selective transcriptional responses to three nuclear receptors. Cell 1991; 65: 1267 – 1279
13. Yu V. C., Delseret C., Anderson B., Hollowly J. M., Devary O. V., Naar A. M., Kim S. Y., Boutin J. M., Glass C K., Rosenfeld M. G. RXRb: A coregulator that enhances binding of retinoic acid, thyroid hormone and vitamin D3 receptors to their cognate response elements. Cell 1991; 67: 1251 – 1266
14. Mangelsdorf D. J., Umesono K., Evans R. M. The Retinoid Receptors. The Retinoids, M. B. Sporn, A. B. Roberts, D. S. Goodman. Raven Press, New York 1994; 319 – 349
15. Dawson M. I., Hobbs P. D., Stein R. B., Berger T. S., Heyman R. A. Interaction of retinoids with retinoic acid nuclear receptor isoforms. Retinoids: Progress in Research and Clinical Applications, M. A. Livrea, L. Packer. Marcel Dekker, New York 1993; 205 – 221
16. Delescluse C., Cavey M. T., Martin B., Bernard B. A., Reichert U., Maignan J., Darmon M., Shroot B. Selective high affinity retinoic receptor α or β-γ ligands. Mol. Pharm. 1991; 40: 556 – 562
17. Esgleyes-Ribot T., Chandraratna R. A. S., Lew-Kaya D., Sefton J., Duvic M. J. Response of psoriasis to a new topical retinoid, AGN190168. J. Am. Acad. Dermatol. 1994; 30: 581 – 590
18. Wakeling A. E., Valcaccia B., Newboult E., Green L. R. Non-steroidal anti-estrogens-receptor binding and biological response in rat uterus, rat mammary carcinoma and human breast cancer cells. J. Steroid Biochem. 1984; 20: 111 – 120
19. Tzukerman M. T., Esty A., Santiso-Mere D., Danielian P., Parker M. G., Stein R. B., Pike J. W., McDonnell D. P. Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions. Mol. Endocrinol. 1994; 8: 21 – 30
20. Miner J. N., Diamond M. I., Yamamoto K. R. Joints in the regulatory lattice: composite regulation by steroid receptor-AP-1 complexes. Cell Growth and Diff. 1991; 2: 525 – 530
21. Jonat C., Rahmsdorf H. J., Park K.-K., Cato A. C. B., Gebel S., Ponta H., Herrlich P. Anti-tumor promotion and antiinflammation: Down modulation of AP-1 (Fos/Jun) activity by glucocorticoid hormone. Cell 1990; 62: 1189 – 1204
22. Imai E., Stromstedt P.-E., Quinn Carlstedt-Duke J., Gustafsson J.-A., Granner D. Characterization of a complex glucocorticoid response unit in the PEPCK gene. Mol. Cell. Biol. 1990; 10: 4712 – 4719
23. Heck S., Kullman M., Gast A., Ponta H., Rahmsdorf H. J., Herrlich P., Cato A. C. B. A distinct modulating domain in glucocorticoid receptor monomers in the repression of activity of the transcription factor AP-1. EMBO J. 1994; 14: 452 – 460
24. Greenland A. C., Farrar M. A., Viviano B. L., Schreiber R. D. Ligand-induced IFNΓ receptor tyrosine phosphorylation couples the receptor to its signal transduction system (p91). EMBO J. 1994; 13: 1591 – 1600
25. Shuai K., Schindler C., Prezioso V. R., Darnell J. E. Activation of transcription by IFNΓ: Tyrosine phosphorylation of a 91-kD DNA binding protein. Science 1992; 258: 1808 – 1812
26. Khan K. D., Shuai K., Lindwall G., Maher S. E., Darnell J. E., Bothwell A. L. M. Induction of the Ly-6A/E gene by interferon α/β and γ requires a DNA element to which a tyrosine-phosphorylated 91-kDa protein binds. Proc. Natl. Acad. Sci. 1993; 90: 6806 – 6810
27. Lamb P., Seidel H. M., Haslam J., Milocco L., Kessler L. V., Stein R. B., Rosen J. STAT protein complexes activated by interferon-γ and gp 130 signaling molecules differ in their sequence preferences and transcriptional induction properties. Nucl. Acids Res. 1995; 23: 3283 – 3289
28. Yuan J., Wegenka U., Lutticken C., Buschmann J., Decker T., Schindler C., Heinrich P. C., Horn F. The signaling pathways of interleukin-6 and gamma interferon converge by the activation of different transcription factors which bind to common responsive DNA elements. Mol. Cell. Biol. 1994; 14: 1657 – 1668
29. Seidel H. M., Milocco L. H., Lamb P., Darnell J. E., Jr., Stein R. B., Rosen J. Spacing of palindromic half sites as a determinant of selective DNA binding and transcriptional activity of signal transducers and activators of transcription. Proc. Natl. Acad. Sci. USA 1995; 92: 3041 – 3045
30. Lamb P., Haslam J., Kessler L., Seidel H. M., Stein R. B., Rosen J. Rapid Activaton of the interferon-γ signal transduction pathway by inhibitors of tyrosine phosphatases. J. Interferon Res. 1994; 14: 365 – 373
31. Levitzki A., Gazit A. Tyrosine kinase inhibition: An approach to drug development. Science 1995; 267: 1782 – 1788
32. Fry D. W., Kraker A. J., McMichael A., Ambroso L. A., Nelson J. M., Leopold W. R., Connors R. W., Bridges A. J. A specific inhibitor of epidermal growth factor receptor tyrosine kinase. Science 1994; 265: 1093 – 1096
33. Meydan N., Grunberger T., Dadi H., Shahar M., Arpaia E., Lapidot Z., Leeder J. S., Freedman M., Cohen A., Gazit A., Levitzki A., Roifman C. M. Inhibition of acute lymphoblastic leukemia by a Jak-2 inhibitor. Nature 1996; 379: 645 – 648