Cell type and gene-specific activity of the retinoid inverse agonist AGN 193109: Divergent effects from agonist at retinoic acid receptor γ in human keratinocytes

Cell Growth and Differentiation

Volumn 10, Issue 4, 1999, Pages 255-262

  Thacher, Scott M ^a   Nagpal, Sunil ^a   Klein, Elliott S ^a   Arefieg, Taghreed ^a   Krasinski, Glenn ^a   DiSepio, Dan ^a   Agarwal, Chapla ^b   Johnson, Alan ^a   Eckert, Richard L ^b   Chandraratna, Roshantha A S ^a  

^a ALLERGAN INC   (United States)

^b CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [2 [5,6 DIHYDRO 5,5 DIMETHYL 8 (4 METHYLPHENYL) 2 NAPHTHYL]ETHYNYL]BENZOIC ACID; CALGRANULIN; RETINOIC ACID RECEPTOR;

ARTICLE; CELL DIFFERENTIATION; GENE EXPRESSION REGULATION; KERATINOCYTE; PRIORITY JOURNAL; REGULATORY MECHANISM;

CALCIUM-BINDING PROTEINS; CALGRANULIN A; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; GENE EXPRESSION REGULATION; HUMANS; KERATINOCYTES; KERATINS; MATRIX METALLOPROTEINASE 3; NAPHTHALENES; RECEPTORS, RETINOIC ACID; RETINOIDS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; TRANSGLUTAMINASES;

EID: 0032941834     PISSN: 10449523     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (46)

1. Mangelsdorf, D. J., Umesono, K., and Evans, R. M. The retinoid receptors. In: M. B. Sporn, A. B. Roberts, and D. S. Goodman (eds.), The Retinoids: Biology, Chemistry and Medicine, pp. 319-349. Raven Press: New York, 1994.
2. Horlein, A. J., Naar, A. M., Heinzel, T., Torchia, J., Gloss, B., Kurokawa, R., Ryan, A., Kamei, Y., Soderstrom, M., Glass, C. K., and Rosenfeld, M. Ligand-independent repression by the thyroid hormone receptor mediated by a nuclear receptor co-repressor. Nature (Lond.), 377: 397-404, 1995.
3. Heinzel, T., Lavinsky, R. M., Mullen, T-M., Soderstrom, M., Laherty, C. D., Torchia, J., Yang, W-M., Brard, G., Ngo, S. D., Davie, J. R., Seto, E., Eisenman, R. N., Rose, D. W., Glass, C. K., and Rosenfeld, M. G. A complex containing N-CoR and histone deacetylase mediates transcriptional repression. Nature (Lond.), 387: 43-48, 1997.
4. Lavinsky, R. M., Jepsen, K., Heinzel, T., Torchia, J., Mullen, T-M., Schiff, R., Del-Rio, A. L., Ricote, M., Ngo, S., Gemsch, J., Hilsenbeck, S. G., Osborne, C. K., Glass, C. K., Rosenfeld, M. G., and Rose, D. W. Diverse signalling pathways modulate nuclear receptor recruitment of N-CoR and SMRT complexes. Proc. Natl. Acad. Sci. USA, 95: 2920-2925, 1998.
5. Johnson, A. T., Klein, E. S., Gillett, S. J., Wang, L., Song, T. K., Pino, M. E., and Chandraratna, R. A. S. Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. J. Med. Chem., 38: 4764-4767, 1995.
6. Standeven, A. M., Johnson, A. T., Escobar, M., and Chandraratna, R. A. S. Specific antagonist of retinoid toxicity in mice. Toxicol. Appl. Pharmacol., 138: 169-175, 1996.
7. Standeven, A. M., Beard, R. L., Johnson, A. T., Boehm, M. F., Escobar, M., Heyman, R. A., and Chandraratna, R. A. S. Retinoid-induced hypertriglyceridemia in rats is mediated by retinoic acid receptors. Fundam. Appl. Toxicol., 33: 264-271, 1996.
8. Klein, E. S., Pino, M. E., Johnson, A. T., Davies, P. J. A., Nagpal, S., Thacher, S. M., Krasinski, G., and Chandraratna, R. A. S. Identification and functional separation of retinoic acid receptor neutral antagonists and inverse agonists. J. Biol. Chem., 271: 22692-22696, 1996.
9. 2-adrenoreceptor. Nature (Lond.), 374: 272-276, 1995.
10. 2-adrenergic receptor. Mol. Pharmacol., 50: 662-669, 1996.
11. Forman, B. M., Tzameli, I., Choi, H-S., Chen, J., Simha, D., Seol, W., Evans, R. M., and Moore, D. D. Androstane metabolites bind to and deactivate the nuclear receptor CAR-β. Nature (Lond.), 395: 612-615, 1998.
12. Nagpal, S., Thacher, S. M., Patel, S., Friant, S., Malhotra, M., Shafer, J., Krasinski, G., Asano, A. T., Teng, M., Duvic, M., and Chandraratna, R. A. S. Negative regulation of two hyperproliferative keratinocyte markers by a retinoic acid receptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ., 7: 1783-1791, 1996.
13. Agarwal, C., Chandraratna, R. A. S., Johnson, A. T., Rorke, E. A., and Eckert, R. L. AGN 193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J. Biol. Chem., 271: 12209-12212, 1996.
14. Nagpal, S., Athanikar, J., and Chandraratna, R. A. S. Separation of transactivation and AP1 antagonism functions of retinoic acid receptor α. J. Biol. Chem., 270: 923-927, 1995.
15. Saunders, N. A., and Jetten, A. M. Control of growth regulatory and differentiation-specific genes in human epidermal keratinocytes by interferon γ. J. Biol. Chem., 269: 2016-2022, 1994.
16. Gilfix, B. M., and Eckert, R. L. Co-ordinate control by vitamin A of keratin gene expression in human keratinocytes. J. Biol. Chem., 260: 14026-14029, 1985.
17. Fisher, G. J., Talwar, H. S., Xiao, J-H., Datta, S. C., Reddy, A. P., Gaub, M.-P., Rochette-Egly, C., Chambon, P., and Voorhees, J. J. Immunological identification and functional quantitation of retinoic acid and retinoid X receptor proteins in human skin. J. Biol. Chem., 269: 20629-20635, 1994.
18. Crowe, D. L., Hu, L., Gudas, L. J., and Rheinwald, J. G. Variable expression of retinoic acid receptor (RARβ) messenger RNA in human oral and epidermal keratinocytes: relation to keratin-19 expression and keratinization potential. Differentiation, 48: 199-208, 1991.
19. Elder, J. T., Fisher, G. J., Zhang, Q-Y., Eisen, D., Krust, A., Kastner, P., Chambon, P., and Voorhees, J. J. Retinoic acid receptor gene expression in human skin. J. Invest. Dermatol., 96: 425-433, 1991.
20. Vollberg, T. M., Nervi, C., George, M. D., Fujimoto, W., Krust, A., and Jetten, A. M. Retinoic acid receptors as regulators of human epidermal keratinocyte differentiation. Mol. Endocrinol., 6: 667-676, 1992.
21. Xiao, J-H., Durand, B., Chambon, P., and Voorhees, J. J. Endogenous retinoic acid receptor (RAR)-retinoid X receptor (RXR) heterodimers are the major functional forms regulating retinoid-responsive elements in adult human keratinocytes. J. Biol. Chem., 270: 3001-3011, 1995.
22. Teng, M., Duong, T. T., Klein, E. S., Pino, M. E., and Chandraratna, R. A. S. Identification of a retinoic acid receptor a specific agonist. J. Med. Chem., 39: 3035-3038, 1996.
23. Madsen, P., Rasmussen, H. H., Leffers, H., Honoré, B., and Celis, J. E. Molecular cloning and expression of a novel keratinocyte protein (psoriasis-associated fatty acid-binding protein [PA-FABP]) that is highly up-regulated in psoriatic skin and that shares similarity to fatty acid-binding proteins. J. Invest. Dermatol., 99: 299-305, 1992.
24. Thacher, S. M., and Rice, R. H. Keratinocyte-specific transglutaminase of cultured epidermal cells: relation to cross-linked envelope formation and terminal differentiation. Cell, 40: 685-695, 1985.
25. Paladini, R. D., Takahashi, K., Bravo, N. S., and Coulombe, P. A. Onset of re-epithelialization after skin injury correlates with a reorganization of keratin filaments in wound edge keratinocytes: defining a potential role for keratin 16. J. Cell Biol., 132: 381-397, 1996.
26. Fitzgerald, P., Teng, M., Chandraratna, R. A., Heyman, R. A., and Allegretto, E. A. Retinoic acid receptor alpha expression correlates with retinoid-induced growth inhibition of human breast cancer cells regardless of estrogen receptor status. Cancer Res., 57: 2642-2650, 1997.
27. Soderstrom, M., Vo, A., Heinzel, T., Lavinsky, R. M., Yang, W-M., Seto, E., Peterson, D. A., Rosenfeld, M. G., and Glass, C. K. Differential effects of nuclear receptor corepressor (N-CoR) expression levels on retinoic acid receptor-mediated repression support the existence of dynamically regulated corepressor complexes. Mol. Endocrinol., 11: 682-692, 1997.
28. Westin, S., Kurokawa, R., Nolte, R. T., Wisely, G. B., McInerney, E. M., Rose, D. W., Milburn, M. V., Rosenfeld, M. G., and Glass, C. K. Interactions controlling the assembly of nuclear-receptor heterodimers and co-activators. Nature (Lond.), 395: 199-202, 1998.
29. Alland, L., Muhle, R., Hou, H., Jr., Potes, J., Chin, L., Schreiber-Agus, N., and DePinho, R. A. Role for N-CoR and histone deacetylase in Sin3-mediated transcriptional repression. Nature (Lond.), 337: 49-55, 1997.
30. Yang, N. N., Bryant, H. U., Hardikar, S., Sato, M., Galvin, R. J. S., Glasebrook, A. L., and Termine, J. D. Estrogen and raloxifene stimulate transforming growth factor-β3 gene expression in rat bone: a potential mechanism for estrogen-or raloxifene-mediated bone maintenance. Endocrinology, 137: 2075-2084, 1996.
31. Montano, M. M., and Katzenellenbogen, B. S. The quinone reductase gene: a unique estrogen-regulated gene that is activated by antiestrogens. Proc. Natl. Acad. Sci. USA, 94: 2581-2586, 1997.
32. Yang, N. N., Venugopalan, M., Hardikar, S., and Glasebrook, A. Identification of an estrogen response element activated by metabolites of 17β-estradiol and raloxifene. Science (Washington DC), 273: 1222-1225, 1996.
33. Yoh, S. M., Chatterjee, V. K., and Privalsky, M. L. Thyroid hormone resistance syndrome manifests as an aberrant interaction between mutant T3 receptors and transcriptional corepressors. Mol. Endocrinol., 11: 470-480, 1997.
34. Tagami, T., and Jameson, J. L. Nuclear corepressors enhance the dominant negative activity of mutant receptors that cause resistance to thyroid hormone. Endocrinology, 139: 640-650, 1998.
35. Maytin, E. V., and Habener, J. F. Transcription factors C/EBPα, C/EBPβ, and CHOP (Gadd153) expressed during the differentiation program of keratinocytes in vitro and in vivo. J. Invest. Dermatol., 110: 238-246, 1998.
36. Oh, H. S., and Smart, R. C. Expression of CCAAT/enhancer binding proteins (C/EBP) is associated with squamous differentiation in epidermis and isolated primary keratinocytes and is altered in skin neoplasms. J. Invest. Dermatol., 110: 939-945, 1998.
37. DiSepio, D., Malhotra, M., Chandraratna, R. A. S., and Nagpal, S. Retinoic acid receptor-nuclear factor-interleukin 6 antagonism. A novel mechanism of retinoid-dependent inhibition of a keratinocyte hyperproliferative differentiation marker. J. Biol. Chem., 272: 25555-25559, 1997.
38. McDonnell, D. P., Clemm, D. L., Hermann, T., Goldman, M. E., and Pike, J. W. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol. Endocrinol., 9: 659-669, 1995.
39. Wilkinson, M. M., Busuttil, A., Hayward, C., Brock, D. J. H., Dorin, J. R., and van Heyningen, V. Expression pattern of two related cystic-fibrosis-associated calcium-binding proteins in normal and abnormal tissues. J. Cell Sci., 91: 221-230, 1988.
40. Rheinwald, J. G. Methods for clonal growth and serial cultivation of normal human epidermal keratinocytes and mesothelial cells. In: R. Baserga (ed.) Cell Growth and Division: A Practical Approach, pp. 81-94. IRL Press: Oxford, 1989.
41. Jones, P. H., Harper, S., and Watt, F. M. Stem cell patterning and fate in human epidermis. Cell, 80: 83-93, 1995.
42. Germain, L., Rouabhia, M., Guignard, R., Carrier, L., Bouvard, V., and Auger, F. A. Improvement of human keratinocyte isolation and culture using thermolysin. Burns, 19: 99-104, 1993.
43. Randolph, R. K., and Simon, M. Characterization of retinol metabolism in cultured human epidermal keratinocytes. J. Biol. Chem., 268: 9198-9205, 1993.
44. Agarwal, C., Hembree, J. R., Rorke, E. A., and Eckert, R. L. Interferon and retinoic acid suppress the growth of human papillomavirus type 16 immortalized cervical epithelial cells. Cancer Res., 54: 2108-2112, 1994.
45. Lee, L. G., Connell, C. R., and Bloch, W. Allelic discrimination by nick-translation PCR with fluorogenic probes. Nucl. Acids Res., 21: 3761-3766, 1993.
46. Gibson, U. E. M., Heid, C. A., and Williams, P. M. A novel method for real-time quantitative RT-PCR. Genome Res., 6: 995-1001, 1996.