Global gene expression profiling of progesterone receptor modulators in T47D cells provides a new classification system

Journal of Steroid Biochemistry and Molecular Biology

Volumn 113, Issue 1-2, 2009, Pages 105-115

  Afhüppe, Wiebke ^a   Sommer, Anette ^a   Müller, Jörg ^a   Schwede, Wolfgang ^a   Fuhrmann, Ulrike ^a   Möller, Carsten ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

Affymetrix GeneChip; Coactivator; Marker; PR antagonist; SPRM

Indexed keywords

ANTIGESTAGEN; ASOPRISNIL; J 1042; J 912; LONAPRISAN; MIFEPRISTONE; ONAPRISTONE; PRA 910; PROGESTERONE RECEPTOR; PROGESTERONE RECEPTOR MODULATOR; PROMEGESTONE; UNCLASSIFIED DRUG; ZK 137316;

ARTICLE; BREAST CANCER; CONTROLLED STUDY; DRUG EFFECT; FEMALE; GENE EXPRESSION; GENETIC TRANSCRIPTION; HUMAN; HUMAN CELL; PROTEIN CONFORMATION; PROTEIN MOTIF; PROTEIN PROTEIN INTERACTION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION;

AMINO ACID MOTIFS; AMINO ACID SEQUENCE; BIOLOGICAL ASSAY; CELL LINE, TUMOR; CLUSTER ANALYSIS; ESTRENES; GENE EXPRESSION PROFILING; HUMANS; MOLECULAR SEQUENCE DATA; OLIGONUCLEOTIDE ARRAY SEQUENCE ANALYSIS; OXIMES; PEPTIDES; PRINCIPAL COMPONENT ANALYSIS; RECEPTORS, PROGESTERONE; REPRODUCIBILITY OF RESULTS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; RNA, MESSENGER; TRANSCRIPTION, GENETIC; TRANSCRIPTIONAL ACTIVATION;

MAMMALIA; ORYCTOLAGUS CUNICULUS;

EID: 59849098881     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jsbmb.2008.11.015     Document Type: Article

References (57)

1. Graham J.D., and Clarke C.L. Physiological action of progesterone in target tissues. Endocr. Rev. 18 4 (1997) 502-519
2. Lydon J.P., DeMayo F.J., Funk C.R., Mani S.K., Hughes A.R., Montgomery Jr. C.A., Shyamala G., Conneely O.M., and O'Malley B.W. Mice lacking progesterone receptor exhibit pleiotropic reproductive abnormalities. Genes Dev. 9 18 (1995) 2266-2278
3. Lessey B.A., Alexander P.S., and Horwitz K.B. The subunit structure of human breast cancer progesterone receptors: characterization by chromatography and photoaffinity labeling. Endocrinology 112 4 (1983) 1267-1274
4. Mangelsdorf D.J., Thummel C., Beato M., Herrlich P., Schutz G., Umesono K., Blumberg B., Kastner P., Mark M., Chambon P., and Evans R.M. The nuclear receptor superfamily: the second decade. Cell 83 6 (1995) 835-839
5. Kastner P., Bocquel M.T., Turcotte B., Garnier J.M., Horwitz K.B., Chambon P., and Gronemeyer H. Transient expression of human and chicken progesterone receptors does not support alternative translational initiation from a single mRNA as the mechanism generating two receptor isoforms. J. Biol. Chem. 265 21 (1990) 12163-12167
6. Conneely O.M., Mulac-Jericevic B., Lydon J.P., and De Mayo F.J. Reproductive functions of the progesterone receptor isoforms: lessons from knock-out mice. Mol. Cell Endocrinol. 179 1-2 (2001) 97-103
7. Mulac-Jericevic B., Mullinax R.A., DeMayo F.J., Lydon J.P., and Conneely O.M. Subgroup of reproductive functions of progesterone mediated by progesterone receptor-B isoform. Science 289 5485 (2000) 1751-1754
8. Beato M. Gene regulation by steroid hormones. Cell 56 3 (1989) 335-344
9. Giangrande P.H., Kimbrel E.A., Edwards D.P., and McDonnell D.P. The opposing transcriptional activities of the two isoforms of the human progesterone receptor are due to differential cofactor binding. Mol. Cell Biol. 20 9 (2000) 3102-3115
10. Klein-Hitpass L., Tsai S.Y., Weigel N.L., Allan G.F., Riley D., Rodriguez R., Schrader W.T., Tsai M.J., and O'Malley B.W. The progesterone receptor stimulates cell-free transcription by enhancing the formation of a stable preinitiation complex. Cell 60 2 (1990) 247-257
11. Smith C.L., and O'Malley B.W. Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr. Rev. 25 1 (2004) 45-71
12. Heery D.M., Kalkhoven E., Hoare S., and Parker M.G. A signature motif in transcriptional co-activators mediates binding to nuclear receptors. Nature 387 6634 (1997) 733-736
13. Tanenbaum D.M., Wang Y., Williams S.P., and Sigler P.B. Crystallographic comparison of the estrogen and progesterone receptor's ligand binding domains. Proc. Natl. Acad. Sci. U.S.A. 95 11 (1998) 5998-6003
14. Dong Y., Roberge J.Y., Wang Z., Wang X., Tamasi J., Dell V., Golla R., Corte J.R., Liu Y., Fang T., Anthony M.N., Schnur D.M., Agler M.L., Dickson Jr. J.K., Lawrence R.M., Prack M.M., Seethala R., and Feyen J.H. Characterization of a new class of selective nonsteroidal progesterone receptor agonists. Steroids 69 3 (2004) 201-217
15. Winneker R.C., Fensome A., Wrobel J.E., Zhang Z., and Zhang P. Nonsteroidal progesterone receptor modulators: structure activity relationships. Semin. Reprod. Med. 23 1 (2005) 46-57
16. Croxatto H.B., Salvatierra A.M., Croxatto H.D., and Fuentealba B. Effects of continuous treatment with low dose mifepristone throughout one menstrual cycle. Hum. Reprod. 8 2 (1993) 201-207
17. Luukkainen T., Heikinheimo O., Haukkamaa M., and Lahteenmaki P. Inhibition of folliculogenesis and ovulation by the antiprogesterone RU 486. Fertil. Steril. 49 6 (1988) 961-963
18. Ishwad P.C., Katkam R.R., Hinduja I.N., Chwalisz K., Elger W., and Puri C.P. Treatment with a progesterone antagonist ZK 98.299 delays endometrial development without blocking ovulation in bonnet monkeys. Contraception 48 1 (1993) 57-70
19. Michna H., Nishino Y., Neef G., McGuire W.L., and Schneider M.R. Progesterone antagonists: tumor-inhibiting potential and mechanism of action. J. Steroid Biochem. Mol. Biol. 41 3-8 (1992) 339-348
20. Romieu G., Maudelonde T., Ulmann A., Pujol H., Grenier J., Cavalie G., Khalaf S., and Rochefort H. The antiprogestin RU486 in advanced breast cancer: preliminary clinical trial. Bull. Cancer 74 4 (1987) 455-461
21. Kettel L.M., Murphy A.A., Morales A.J., Ulmann A., Baulieu E.E., and Yen S.S. Treatment of endometriosis with the antiprogesterone mifepristone (RU486). Fertil. Steril. 65 1 (1996) 23-28
22. Chwalisz K., Garg R., Brenner R.M., Schubert G., and Elger W. Selective progesterone receptor modulators (SPRMs): a novel therapeutic concept in endometriosis. Ann. N. Y. Acad. Sci. 955 (2002) 373-388 (discussion 389-393, 396-406)
23. Chwalisz K., Larsen L., Mattia-Goldberg C., Edmonds A., Elger W., and Winkel C.A. A randomized, controlled trial of asoprisnil, a novel selective progesterone receptor modulator, in women with uterine leiomyomata. Fertil. Steril. 87 6 (2007) 1399-1412
24. Murphy A.A., Kettel L.M., Morales A.J., Roberts V.J., and Yen S.S. Regression of uterine leiomyomata in response to the antiprogesterone RU 486. J. Clin. Endocrinol. Metab. 76 2 (1993) 513-517
25. Chwalisz K., Brenner R.M., Fuhrmann U.U., Hess-Stumpp H., and Elger W. Antiproliferative effects of progesterone antagonists and progesterone receptor modulators on the endometrium. Steroids 65 10-11 (2000) 741-751
26. Elger W., Bartley J., Schneider B., Kaufmann G., Schubert G., and Chwalisz K. Endocrine pharmacological characterization of progesterone antagonists and progesterone receptor modulators with respect to PR-agonistic and antagonistic activity. Steroids 65 10-11 (2000) 713-723
27. DeManno D., Elger W., Garg R., Lee R., Schneider B., Hess-Stumpp H., Schubert G., and Chwalisz K. Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy. Steroids 68 10-13 (2003) 1019-1032
28. Schubert G., Elger W., Kaufmann G., Schneider B., Reddersen G., and Chwalisz K. Discovery, chemistry, and reproductive pharmacology of asoprisnil and related 11beta-benzaldoxime substituted selective progesterone receptor modulators (SPRMs). Semin. Reprod. Med. 23 1 (2005) 58-73
29. Han S.J., Tsai S.Y., Tsai M.J., and O'Malley B.W. Distinct temporal and spatial activities of RU486 on progesterone receptor function in reproductive organs of ovariectomized mice. Endocrinology 148 5 (2007) 2471-2486
30. Klein-Hitpass L., Cato A.C., Henderson D., and Ryffel G.U. Two types of antiprogestins identified by their differential action in transcriptionally active extracts from T47D cells. Nucleic Acids Res. 19 6 (1991) 1227-1234
31. Fuhrmann U., Bengtson C., Repenthin G., and Schillinger E. Stable transfection of androgen receptor and MMTV-CAT into mammalian cells: inhibition of cat expression by anti-androgens. J. Steroid Biochem. Mol. Biol. 42 8 (1992) 787-793
32. Fuhrmann U., Hess-Stumpp H., Cleve A., Neef G., Schwede W., Hoffmann J., Fritzemeier K.H., and Chwalisz K. Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J. Med. Chem. 43 26 (2000) 5010-5016
33. Lundeen S.G., Zhang Z., Zhu Y., Carver J.M., and Winneker R.C. Rat uterine complement C3 expression as a model for progesterone receptor modulators: characterization of the new progestin trimegestone. J. Steroid Biochem. Mol. Biol. 78 2 (2001) 137-143
34. Zhang Z., Lundeen S.G., Zhu Y., Carver J.M., and Winneker R.C. In vitro characterization of trimegestone: a new potent and selective progestin. Steroids 65 10-11 (2000) 637-643
35. Zhang Z., Olland A.M., Zhu Y., Cohen J., Berrodin T., Chippari S., Appavu C., Li S., Wilhem J., Chopra R., Fensome A., Zhang P., Wrobel J., Unwalla R.J., Lyttle C.R., and Winneker R.C. Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget. J. Biol. Chem. 280 31 (2005) 28468-28475
36. Kamei Y., Xu L., Heinzel T., Torchia J., Kurokawa R., Gloss B., Lin S.C., Heyman R.A., Rose D.W., Glass C.K., and Rosenfeld M.G. A CBP integrator complex mediates transcriptional activation and AP-1 inhibition by nuclear receptors. Cell 85 3 (1996) 403-414
37. Onate S.A., Tsai S.Y., Tsai M.J., and O'Malley B.W. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science 270 5240 (1995) 1354-1357
38. Takeshita A., Yen P.M., Misiti S., Cardona G.R., Liu Y., and Chin W.W. Molecular cloning and properties of a full-length putative thyroid hormone receptor coactivator. Endocrinology 137 8 (1996) 3594-3597
39. Chang C., Norris J.D., Gron H., Paige L.A., Hamilton P.T., Kenan D.J., Fowlkes D., and McDonnell D.P. Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta. Mol. Cell Biol. 19 12 (1999) 8226-8239
40. Cohen R.N., Brzostek S., Kim B., Chorev M., Wondisford F.E., and Hollenberg A.N. The specificity of interactions between nuclear hormone receptors and corepressors is mediated by distinct amino acid sequences within the interacting domains. Mol. Endocrinol. 15 7 (2001) 1049-1061
41. Bray J.D., Jelinsky S., Ghatge R., Bray J.A., Tunkey C., Saraf K., Jacobsen B.M., Richer J.K., Brown E.L., Winneker R.C., Horwitz K.B., and Lyttle C.R. Quantitative analysis of gene regulation by seven clinically relevant progestins suggests a highly similar mechanism of action through progesterone receptors in T47D breast cancer cells. J. Steroid Biochem. Mol. Biol. 97 4 (2005) 328-341
42. Bray J.D., Zhang Z., Winneker R.C., and Lyttle C.R. Regulation of gene expression by PRA-910, a novel progesterone receptor modulator, in T47D cells. Steroids 68 10-13 (2003) 995-1003
43. Kester H.A., van der Leede B.M., van der Saag P.T., and van der Burg B. Novel progesterone target genes identified by an improved differential display technique suggest that progestin-induced growth inhibition of breast cancer cells coincides with enhancement of differentiation. J. Biol. Chem. 272 26 (1997) 16637-16643
44. Richer J.K., Jacobsen B.M., Manning N.G., Abel M.G., Wolf D.M., and Horwitz K.B. Differential gene regulation by the two progesterone receptor isoforms in human breast cancer cells. J. Biol. Chem. 277 7 (2002) 5209-5218
45. Madauss K.P., Grygielko E.T., Deng S.J., Sulpizio A.C., Stanley T.B., Wu C., Short S.A., Thompson S.K., Stewart E.L., Laping N.J., Williams S.P., and Bray J.D. A structural and in vitro characterization of asoprisnil: a selective progesterone receptor modulator. Mol. Endocrinol. 21 5 (2007) 1066-1081
46. Pullen M.A., Laping N., Edwards R., and Bray J. Determination of conformational changes in the progesterone receptor using ELISA-like assays. Steroids 71 9 (2006) 792-798
47. Allan G.F., Leng X., Tsai S.Y., Weigel N.L., Edwards D.P., Tsai M.J., and O'Malley B.W. Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation. J. Biol. Chem. 267 27 (1992) 19513-19520
48. Katzenellenbogen J.A., and Katzenellenbogen B.S. Nuclear hormone receptors: ligand-activated regulators of transcription and diverse cell responses. Chem. Biol. 3 7 (1996) 529-536
49. McKenna N.J., and O'Malley B.W. Combinatorial control of gene expression by nuclear receptors and coregulators. Cell 108 4 (2002) 465-474
50. Chwalisz K., Perez M.C., Demanno D., Winkel C., Schubert G., and Elger W. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Endocr. Rev. 26 3 (2005) 423-438
51. Winneker R.C., Bitran D., and Zhang Z. The preclinical biology of a new potent and selective progestin: trimegestone. Steroids 68 10-13 (2003) 915-920
52. Zhang P., Terefenko E.A., Fensome A., Wrobel J., Winneker R., Lundeen S., Marschke K.B., and Zhang Z. 6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists. J. Med. Chem. 45 20 (2002) 4379-4382
53. Liu Z., Auboeuf D., Wong J., Chen J.D., Tsai S.Y., Tsai M.J., and O'Malley B.W. Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486. Proc. Natl. Acad. Sci. U.S.A. 99 12 (2002) 7940-7944
54. Meyer M.E., Pornon A., Ji J.W., Bocquel M.T., Chambon P., and Gronemeyer H. Agonistic and antagonistic activities of RU486 on the functions of the human progesterone receptor. EMBO J. 9 12 (1990) 3923-3932
55. Sartorius C.A., Tung L., Takimoto G.S., and Horwitz K.B. Antagonist-occupied human progesterone receptors bound to DNA are functionally switched to transcriptional agonists by cAMP. J. Biol. Chem. 268 13 (1993) 9262-9266
56. Beck C.A., Weigel N.L., Moyer M.L., Nordeen S.K., and Edwards D.P. The progesterone antagonist RU486 acquires agonist activity upon stimulation of cAMP signaling pathways. Proc. Natl. Acad. Sci. U.S.A. 90 10 (1993) 4441-4445
57. Baulieu E.E. On the mechanism of action of RU486. Ann. N. Y. Acad. Sci. 626 (1991) 545-560