메뉴 건너뛰기




Volumn 119, Issue 1-2, 2010, Pages 45-55

In vitro characterization of ZK 230211-A type III progesterone receptor antagonist with enhanced antiproliferative properties

Author keywords

C Src kinase interaction; NCoR interaction; Nuclear localization; PR antagonist classification; PRE binding activity; T47D cell cycle regulation

Indexed keywords

11BETA (4 ACETYLPHENYL) 17BETA HYDROXY 17ALPHA (1,1,2,2,2 PENTAFLUOROETHYL)ESTRA 4,9 DIEN 3 ONE; ANDROGEN RECEPTOR; CYCLIN D1; ESTROGEN RECEPTOR; GLUCOCORTICOID RECEPTOR; MIFEPRISTONE; NUCLEAR RECEPTOR COREPRESSOR; ONAPRISTONE; PROGESTERONE RECEPTOR; PROMEGESTONE; PROTEIN TYROSINE KINASE;

EID: 76749101084     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jsbmb.2009.12.011     Document Type: Article
Times cited : (22)

References (46)
  • 1
    • 8544252436 scopus 로고    scopus 로고
    • Physiological action of progesterone in target tissues
    • Graham J.D., and Clarke C.L. Physiological action of progesterone in target tissues. Endocr. Rev. 18 4 (1997) 502-519
    • (1997) Endocr. Rev. , vol.18 , Issue.4 , pp. 502-519
    • Graham, J.D.1    Clarke, C.L.2
  • 3
    • 0026726806 scopus 로고
    • Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation
    • 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
    • (1992) J. Biol. Chem. , vol.267 , Issue.27 , pp. 19513-19520
    • Allan, G.F.1    Leng, X.2    Tsai, S.Y.3    Weigel, N.L.4    Edwards, D.P.5    Tsai, M.J.6    O'Malley, B.W.7
  • 5
    • 0033645919 scopus 로고    scopus 로고
    • Antiproliferative effects of progesterone antagonists and progesterone receptor modulators on the endometrium
    • 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
    • (2000) Steroids , vol.65 , Issue.10-11 , pp. 741-751
    • Chwalisz, K.1    Brenner, R.M.2    Fuhrmann, U.U.3    Hess-Stumpp, H.4    Elger, W.5
  • 6
    • 0027299883 scopus 로고
    • Growth factor, steroid, and steroid antagonist regulation of cyclin gene expression associated with changes in T-47D human breast cancer cell cycle progression
    • Musgrove E.A., Hamilton J.A., Lee C.S., Sweeney K.J., Watts C.K., and Sutherland R.L. Growth factor, steroid, and steroid antagonist regulation of cyclin gene expression associated with changes in T-47D human breast cancer cell cycle progression. Mol. Cell Biol. 13 6 (1993) 3577-3587
    • (1993) Mol. Cell Biol. , vol.13 , Issue.6 , pp. 3577-3587
    • Musgrove, E.A.1    Hamilton, J.A.2    Lee, C.S.3    Sweeney, K.J.4    Watts, C.K.5    Sutherland, R.L.6
  • 8
    • 0025572656 scopus 로고
    • Antitumor activity and mechanism of action of different antiprogestins in experimental breast cancer models
    • Schneider M.R., Michna H., Nishino Y., and el Etreby M.F. Antitumor activity and mechanism of action of different antiprogestins in experimental breast cancer models. J. Steroid Biochem. Mol. Biol. 37 6 (1990) 783-787
    • (1990) J. Steroid Biochem. Mol. Biol. , vol.37 , Issue.6 , pp. 783-787
    • Schneider, M.R.1    Michna, H.2    Nishino, Y.3    el Etreby, M.F.4
  • 9
    • 0025917499 scopus 로고
    • Inhibition of the estradiol-mediated endometrial gland formation by the antigestagen onapristone in rabbits: relationship to uterine estrogen receptors
    • Chwalisz K., Hegele-Hartung C., Fritzemeier K.H., Beier H.M., and Elger W. Inhibition of the estradiol-mediated endometrial gland formation by the antigestagen onapristone in rabbits: relationship to uterine estrogen receptors. Endocrinology 129 1 (1991) 312-322
    • (1991) Endocrinology , vol.129 , Issue.1 , pp. 312-322
    • Chwalisz, K.1    Hegele-Hartung, C.2    Fritzemeier, K.H.3    Beier, H.M.4    Elger, W.5
  • 10
    • 2442755686 scopus 로고    scopus 로고
    • Modulation of oestrogenic effects by progesterone antagonists in the rat uterus
    • Chwalisz K., Stockemann K., Fritzemeier K.H., and Fuhrmann U. Modulation of oestrogenic effects by progesterone antagonists in the rat uterus. Hum. Reprod. Update 4 5 (1998) 570-583
    • (1998) Hum. Reprod. Update , vol.4 , Issue.5 , pp. 570-583
    • Chwalisz, K.1    Stockemann, K.2    Fritzemeier, K.H.3    Fuhrmann, U.4
  • 11
    • 0033656617 scopus 로고    scopus 로고
    • Endocrine pharmacological characterization of progesterone antagonists and progesterone receptor modulators with respect to PR-agonistic and antagonistic activity
    • 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
    • (2000) Steroids , vol.65 , Issue.10-11 , pp. 713-723
    • Elger, W.1    Bartley, J.2    Schneider, B.3    Kaufmann, G.4    Schubert, G.5    Chwalisz, K.6
  • 12
    • 0026096890 scopus 로고
    • Two types of antiprogestins identified by their differential action in transcriptionally active extracts from T47D cells
    • 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
    • (1991) Nucleic Acids Res. , vol.19 , Issue.6 , pp. 1227-1234
    • Klein-Hitpass, L.1    Cato, A.C.2    Henderson, D.3    Ryffel, G.U.4
  • 13
    • 34249821078 scopus 로고    scopus 로고
    • Distinct temporal and spatial activities of RU486 on progesterone receptor function in reproductive organs of ovariectomized mice
    • 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
    • (2007) Endocrinology , vol.148 , Issue.5 , pp. 2471-2486
    • Han, S.J.1    Tsai, S.Y.2    Tsai, M.J.3    O'Malley, B.W.4
  • 14
    • 0025053671 scopus 로고
    • Agonistic and antagonistic activities of RU486 on the functions of the human progesterone receptor
    • 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
    • (1990) EMBO J. , vol.9 , Issue.12 , pp. 3923-3932
    • Meyer, M.E.1    Pornon, A.2    Ji, J.W.3    Bocquel, M.T.4    Chambon, P.5    Gronemeyer, H.6
  • 15
    • 0030273673 scopus 로고    scopus 로고
    • The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential
    • Fuhrmann U., Krattenmacher R., Slater E.P., and Fritzemeier K.H. The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception 54 4 (1996) 243-251
    • (1996) Contraception , vol.54 , Issue.4 , pp. 243-251
    • Fuhrmann, U.1    Krattenmacher, R.2    Slater, E.P.3    Fritzemeier, K.H.4
  • 16
    • 0026667686 scopus 로고
    • Stable transfection of androgen receptor and MMTV-CAT into mammalian cells: inhibition of cat expression by anti-androgens
    • 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
    • (1992) J. Steroid Biochem. Mol. Biol. , vol.42 , Issue.8 , pp. 787-793
    • Fuhrmann, U.1    Bengtson, C.2    Repenthin, G.3    Schillinger, E.4
  • 18
    • 0026559680 scopus 로고
    • Hormone-induced progesterone receptor phosphorylation consists of sequential DNA-independent and DNA-dependent stages: analysis with zinc finger mutants and the progesterone antagonist ZK98299
    • Takimoto G.S., Tasset D.M., Eppert A.C., and Horwitz K.B. Hormone-induced progesterone receptor phosphorylation consists of sequential DNA-independent and DNA-dependent stages: analysis with zinc finger mutants and the progesterone antagonist ZK98299. Proc. Natl. Acad. Sci. U.S.A. 89 7 (1992) 3050-3054
    • (1992) Proc. Natl. Acad. Sci. U.S.A. , vol.89 , Issue.7 , pp. 3050-3054
    • Takimoto, G.S.1    Tasset, D.M.2    Eppert, A.C.3    Horwitz, K.B.4
  • 19
    • 0025239785 scopus 로고
    • Two distinct estrogen-regulated promoters generate transcripts encoding the two functionally different human progesterone receptor forms A and B
    • Kastner P., Krust A., Turcotte B., Stropp U., Tora L., Gronemeyer H., and Chambon P. Two distinct estrogen-regulated promoters generate transcripts encoding the two functionally different human progesterone receptor forms A and B. EMBO J. 9 5 (1990) 1603-1614
    • (1990) EMBO J. , vol.9 , Issue.5 , pp. 1603-1614
    • Kastner, P.1    Krust, A.2    Turcotte, B.3    Stropp, U.4    Tora, L.5    Gronemeyer, H.6    Chambon, P.7
  • 20
    • 0027494065 scopus 로고
    • Antagonist-occupied human progesterone B-receptors activate transcription without binding to progesterone response elements and are dominantly inhibited by A-receptors
    • Tung L., Mohamed M.K., Hoeffler J.P., Takimoto G.S., and Horwitz K.B. Antagonist-occupied human progesterone B-receptors activate transcription without binding to progesterone response elements and are dominantly inhibited by A-receptors. Mol. Endocrinol. 7 10 (1993) 1256-1265
    • (1993) Mol. Endocrinol. , vol.7 , Issue.10 , pp. 1256-1265
    • Tung, L.1    Mohamed, M.K.2    Hoeffler, J.P.3    Takimoto, G.S.4    Horwitz, K.B.5
  • 21
    • 0032230289 scopus 로고    scopus 로고
    • A nuclear receptor corepressor modulates transcriptional activity of antagonist-occupied steroid hormone receptor
    • Zhang X., Jeyakumar M., Petukhov S., and Bagchi M.K. A nuclear receptor corepressor modulates transcriptional activity of antagonist-occupied steroid hormone receptor. Mol. Endocrinol. 12 4 (1998) 513-524
    • (1998) Mol. Endocrinol. , vol.12 , Issue.4 , pp. 513-524
    • Zhang, X.1    Jeyakumar, M.2    Petukhov, S.3    Bagchi, M.K.4
  • 22
    • 18144432142 scopus 로고    scopus 로고
    • Integration of progesterone receptor mediated rapid signaling and nuclear actions in breast cancer cell models: role of mitogen-activated protein kinases and cell cycle regulators
    • Faivre E., Skildum A., Pierson-Mullany L., and Lange C.A. Integration of progesterone receptor mediated rapid signaling and nuclear actions in breast cancer cell models: role of mitogen-activated protein kinases and cell cycle regulators. Steroids 70 5-7 (2005) 418-426
    • (2005) Steroids , vol.70 , Issue.5-7 , pp. 418-426
    • Faivre, E.1    Skildum, A.2    Pierson-Mullany, L.3    Lange, C.A.4
  • 23
    • 13544276888 scopus 로고    scopus 로고
    • Progesterone receptors induce cell cycle progression via activation of mitogen-activated protein kinases
    • Skildum A., Faivre E., and Lange C.A. Progesterone receptors induce cell cycle progression via activation of mitogen-activated protein kinases. Mol. Endocrinol. 19 2 (2005) 327-339
    • (2005) Mol. Endocrinol. , vol.19 , Issue.2 , pp. 327-339
    • Skildum, A.1    Faivre, E.2    Lange, C.A.3
  • 29
    • 33846581488 scopus 로고    scopus 로고
    • The role of extranuclear signaling actions of progesterone receptor in mediating progesterone regulation of gene expression and the cell cycle
    • Boonyaratanakornkit V., McGowan E., Sherman L., Mancini M.A., Cheskis B.J., and Edwards D.P. The role of extranuclear signaling actions of progesterone receptor in mediating progesterone regulation of gene expression and the cell cycle. Mol. Endocrinol. 21 2 (2007) 359-375
    • (2007) Mol. Endocrinol. , vol.21 , Issue.2 , pp. 359-375
    • Boonyaratanakornkit, V.1    McGowan, E.2    Sherman, L.3    Mancini, M.A.4    Cheskis, B.J.5    Edwards, D.P.6
  • 30
    • 0031032142 scopus 로고    scopus 로고
    • Antiprogestin inhibition of cell cycle progression in T-47D breast cancer cells is accompanied by induction of the cyclin-dependent kinase inhibitor p21
    • Musgrove E.A., Lee C.S., Cornish A.L., Swarbrick A., and Sutherland R.L. Antiprogestin inhibition of cell cycle progression in T-47D breast cancer cells is accompanied by induction of the cyclin-dependent kinase inhibitor p21. Mol. Endocrinol. 11 1 (1997) 54-66
    • (1997) Mol. Endocrinol. , vol.11 , Issue.1 , pp. 54-66
    • Musgrove, E.A.1    Lee, C.S.2    Cornish, A.L.3    Swarbrick, A.4    Sutherland, R.L.5
  • 32
    • 0026051580 scopus 로고
    • Progestins both stimulate and inhibit breast cancer cell cycle progression while increasing expression of transforming growth factor alpha, epidermal growth factor receptor, c-fos, and c-myc genes
    • Musgrove E.A., Lee C.S., and Sutherland R.L. Progestins both stimulate and inhibit breast cancer cell cycle progression while increasing expression of transforming growth factor alpha, epidermal growth factor receptor, c-fos, and c-myc genes. Mol. Cell Biol. 11 10 (1991) 5032-5043
    • (1991) Mol. Cell Biol. , vol.11 , Issue.10 , pp. 5032-5043
    • Musgrove, E.A.1    Lee, C.S.2    Sutherland, R.L.3
  • 34
    • 0030986236 scopus 로고    scopus 로고
    • A signature motif in transcriptional co-activators mediates binding to nuclear receptors
    • 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
    • (1997) Nature , vol.387 , Issue.6634 , pp. 733-736
    • Heery, D.M.1    Kalkhoven, E.2    Hoare, S.3    Parker, M.G.4
  • 36
    • 0029794881 scopus 로고    scopus 로고
    • SMRT isoforms mediate repression and anti-repression of nuclear receptor heterodimers
    • Chen J.D., Umesono K., and Evans R.M. SMRT isoforms mediate repression and anti-repression of nuclear receptor heterodimers. Proc. Natl. Acad. Sci. U.S.A. 93 15 (1996) 7567-7571
    • (1996) Proc. Natl. Acad. Sci. U.S.A. , vol.93 , Issue.15 , pp. 7567-7571
    • Chen, J.D.1    Umesono, K.2    Evans, R.M.3
  • 38
    • 33744792310 scopus 로고    scopus 로고
    • Sensors and signals: a coactivator/corepressor/epigenetic code for integrating signal-dependent programs of transcriptional response
    • Rosenfeld M.G., Lunyak V.V., and Glass C.K. Sensors and signals: a coactivator/corepressor/epigenetic code for integrating signal-dependent programs of transcriptional response. Genes Dev. 20 11 (2006) 1405-1428
    • (2006) Genes Dev. , vol.20 , Issue.11 , pp. 1405-1428
    • Rosenfeld, M.G.1    Lunyak, V.V.2    Glass, C.K.3
  • 39
    • 0029938795 scopus 로고    scopus 로고
    • Activation and repression by nuclear hormone receptors: hormone modulates an equilibrium between active and repressive states
    • Schulman I.G., Juguilon H., and Evans R.M. Activation and repression by nuclear hormone receptors: hormone modulates an equilibrium between active and repressive states. Mol. Cell Biol. 16 7 (1996) 3807-3813
    • (1996) Mol. Cell Biol. , vol.16 , Issue.7 , pp. 3807-3813
    • Schulman, I.G.1    Juguilon, H.2    Evans, R.M.3
  • 40
    • 0030998328 scopus 로고    scopus 로고
    • The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT
    • Jackson T.A., Richer J.K., Bain D.L., Takimoto G.S., Tung L., and Horwitz K.B. The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT. Mol. Endocrinol. 11 6 (1997) 693-705
    • (1997) Mol. Endocrinol. , vol.11 , Issue.6 , pp. 693-705
    • Jackson, T.A.1    Richer, J.K.2    Bain, D.L.3    Takimoto, G.S.4    Tung, L.5    Horwitz, K.B.6
  • 41
    • 0037062484 scopus 로고    scopus 로고
    • Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486
    • 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
    • (2002) Proc. Natl. Acad. Sci. U.S.A. , vol.99 , Issue.12 , pp. 7940-7944
    • Liu, Z.1    Auboeuf, D.2    Wong, J.3    Chen, J.D.4    Tsai, S.Y.5    Tsai, M.J.6    O'Malley, B.W.7
  • 42
    • 0038657687 scopus 로고    scopus 로고
    • Progesterone receptor interacting coregulatory proteins and cross talk with cell signaling pathways
    • Edwards D.P., Wardell S.E., and Boonyaratanakornkit V. Progesterone receptor interacting coregulatory proteins and cross talk with cell signaling pathways. J. Steroid Biochem. Mol. Biol. 83 1-5 (2002) 173-186
    • (2002) J. Steroid Biochem. Mol. Biol. , vol.83 , Issue.1-5 , pp. 173-186
    • Edwards, D.P.1    Wardell, S.E.2    Boonyaratanakornkit, V.3
  • 43
    • 33751538254 scopus 로고    scopus 로고
    • Progesterone receptors (PR)-B and -A regulate transcription by different mechanisms: AF-3 exerts regulatory control over coactivator binding to PR-B
    • Tung L., Abdel-Hafiz H., Shen T., Harvell D.M., Nitao L.K., Richer J.K., Sartorius C.A., Takimoto G.S., and Horwitz K.B. Progesterone receptors (PR)-B and -A regulate transcription by different mechanisms: AF-3 exerts regulatory control over coactivator binding to PR-B. Mol. Endocrinol. 20 11 (2006) 2656-2670
    • (2006) Mol. Endocrinol. , vol.20 , Issue.11 , pp. 2656-2670
    • Tung, L.1    Abdel-Hafiz, H.2    Shen, T.3    Harvell, D.M.4    Nitao, L.K.5    Richer, J.K.6    Sartorius, C.A.7    Takimoto, G.S.8    Horwitz, K.B.9
  • 44
    • 0034852802 scopus 로고    scopus 로고
    • Progesterone receptor contains a proline-rich motif that directly interacts with SH3 domains and activates c-Src family tyrosine kinases
    • Boonyaratanakornkit V., Scott M.P., Ribon V., Sherman L., Anderson S.M., Maller J.L., Miller W.T., and Edwards D.P. Progesterone receptor contains a proline-rich motif that directly interacts with SH3 domains and activates c-Src family tyrosine kinases. Mol. Cell 8 2 (2001) 269-280
    • (2001) Mol. Cell , vol.8 , Issue.2 , pp. 269-280
    • Boonyaratanakornkit, V.1    Scott, M.P.2    Ribon, V.3    Sherman, L.4    Anderson, S.M.5    Maller, J.L.6    Miller, W.T.7    Edwards, D.P.8
  • 45
    • 0027156480 scopus 로고
    • Antagonist-occupied human progesterone receptors bound to DNA are functionally switched to transcriptional agonists by cAMP
    • 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
    • (1993) J. Biol. Chem. , vol.268 , Issue.13 , pp. 9262-9266
    • Sartorius, C.A.1    Tung, L.2    Takimoto, G.S.3    Horwitz, K.B.4
  • 46
    • 59849098881 scopus 로고    scopus 로고
    • Global gene expression profiling of progesterone receptor modulators in T47D cells provides a new classification system
    • Afhuppe W., Sommer A., Muller J., Schwede W., Fuhrmann U., and Moller C. Global gene expression profiling of progesterone receptor modulators in T47D cells provides a new classification system. J. Steroid Biochem. Mol. Biol. 113 1-2 (2009) 105-115
    • (2009) J. Steroid Biochem. Mol. Biol. , vol.113 , Issue.1-2 , pp. 105-115
    • Afhuppe, W.1    Sommer, A.2    Muller, J.3    Schwede, W.4    Fuhrmann, U.5    Moller, C.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.