Molecular properties and preclinical pharmacology of JNJ-1250132, a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro

Steroids

Volumn 71, Issue 7, 2006, Pages 578-584

  Allan, George F ^a   Palmer, Elizabeth ^a   Musto, Amy ^a   Lai, Muh Tsann ^a   Clancy, Joanna ^a   Palmer, Stephen ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Antagonist; DNA binding; Preclinical pharmacology; Progesterone receptor; Receptor conformation; Steroid

Indexed keywords

ALKALINE PHOSPHATASE; GESTAGEN; GLUCOCORTICOID ANTAGONIST; JNJ 1250132; LIGAND; MIFEPRISTONE; ONAPRISTONE; PROGESTERONE RECEPTOR; PROMEGESTONE; STEROID RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BREAST CANCER; CANCER CELL; CELL PROLIFERATION; CONTROLLED STUDY; CROSS REACTION; DNA BINDING; DNA RESPONSIVE ELEMENT; DRUG ANTAGONISM; DRUG BINDING; DRUG EFFICACY; DRUG INHIBITION; DRUG STRUCTURE; ENDOMETRIUM; FEMALE; GENE EXPRESSION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; PREGNANCY; PROTEIN CONFORMATION; PROTEIN DEGRADATION; RAT; RECEPTOR BINDING;

ANIMALS; DNA; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; FEMALE; GONANES; HORMONE ANTAGONISTS; HUMANS; MALE; MIFEPRISTONE; PROGESTINS; PROTEIN BINDING; RABBITS; RATS; RECEPTORS, PROGESTERONE; STEROIDS; TUMOR CELLS, CULTURED;

ORYCTOLAGUS CUNICULUS;

EID: 33747210932     PISSN: 0039128X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.steroids.2006.02.002     Document Type: Article

References (30)

1. Brogden R.N., Goa K.L., and Faulds D. Mifepristone: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential. Drugs 45 (1993) 384-409
2. Kettel L.M., Murphy A.A., Morales A.J., and Yen S.S.C. Preliminary report on the treatment of endometriosis with low-dose mifepristone (RU 486). Am J Obstet Gynecol 178 (1998) 1151-1156
3. Perrault D., Eisenhauer E.A., Pritchard K.I., Panasci L., Norris B., Vandenburg T., et al. Phase II study of the progesterone antagonist mifepristone in patients with untreated metastatic breast carcinoma: a National Cancer Institute of Canada Clinical Trials Group study. J Clin Oncol 14 (1996) 2709-2712
4. Robertson J.F.R., Willsher P.C., Winterbottom L., Blamey R.W., and Thorpe S. Onapristone, a progesterone receptor antagonist, as first-line therapy in primary breast cancer. Eur J Cancer 35 (1999) 214-218
5. DeManno D., Elger W., Garg R., Lee R., Schneider B., Hess-Stumpp H., et al. Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy. Steroids 68 (2003) 1019-1032
6. Baird D.T., Brown A., Critchley H.O.D., Williams A.R., Lin S., and Cheng L. Effect of long-term treatment with low-dose mifepristone on the endometrium. Hum Reprod (2003) 1861-1868
7. Steinauer J., Pritts E.A., Jackson R., and Jacoby A.F. Systematic review of mifepristone for the treatment of uterine leiomyomata. Obstet Gynecol 103 (2004) 1331-1336
8. Grow D.R., Reece M.T., Hsiu J.G., Adams L., Newcomb P.M., Williams R.F., et al. Chronic antiprogestin therapy produces a stable atrophic endometrium with decreased fibroblast growth factor: a 1-year primate study on contraception and amenorrhea. Fertil Steril 69 (1998) 936-943
9. 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 (2000) 741-751
10. Cameron S.T., Glasier A.F., Narvekar N., Gebbie A., Critchley H.O.D., and Baird D.T. Effects of onapristone on postmenopausal endometrium. Steroids 68 (2003) 1053-1059
11. Chwalisz K., DeManno D., Garg R., Larsen L., Mattia-Goldberg C., and Stickler T. Therapeutic potential for the selective progesterone receptor modulator asoprisnil in the treatment of leiomyomata. Semin Reprod Med 22 (2004) 113-119
12. Klein-Hitpass L., Cato A.C.B., 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 (1991) 1227-1234
13. Bocquel M.T., Ji J., Ylikomi T., Benhamou B., Vergezac A., Chambon P., et al. Type II antagonists impair the DNA binding of steroid hormone receptors without affecting dimerization. J Steroid Biochem Mol Biol 45 (1993) 205-215
14. Allan G.F., Leng X., Tsai S.Y., Weigel N.L., Edwards D.P., Tsai M.-J., et al. Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation. J Biol Chem 267 (1992) 19513-19520
15. Allan G.F., Lombardi E., Haynes-Johnson D., Palmer S., Kiddoe M., Kraft P., et al. Induction of a novel conformation in the progesterone receptor by ZK299 involves a defined region of the carboxyl-terminal tail. Mol Endocrinol 10 (1996) 1206-1213
16. Wagner B.L., Norris J.D., Knotts T.A., Weigel N.L., and McDonnell D.P. The nuclear corepressors NcoR and SMRT are key regulators of both ligand- and 8-bromo-cyclic AMP-dependent transcriptional activity of the human progesterone receptor. Mol Cell Biol 18 (1998) 1369-1378
17. Liu Z., Auboeuf D., Wong J., Chen J.D., Tsai S.Y., Tsai M.-J., et al. Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486. Proc Natl Acad Sci USA 99 (2002) 794-7944
18. Palmer S., Campen C.A., Allan G.F., Rybczynski P., Haynes-Johnson D., Hutchins A., et al. Nonsteroidal progesterone receptor ligands with unprecedented receptor selectivity. J Steroid Biochem Mol Biol 75 (2000) 33-42
19. Allan G.F., Hutchins A., and Clancy J. An ultrahigh-throughput screening assay for estrogen receptor ligands. Anal Biochem 275 (1999) 243-247
20. McPhail M.K. The assay of progestin. J Physiol 83 (1934) 145-156
21. Hissom J.R., Bowden R.T., and Moore M.R. Effects of progestins, estrogens, and antihormones on growth and lactate dehydrogenase in the human breast cancer cell line T47D. Endocrinology 125 (1989) 418-423
22. Robertson J.F.R., Willsher P.C., Winterbottom L., Blamey R.W., and Thorpe S. Onapristone, a progesterone receptor antagonist, as first-line therapy in primary breast cancer. Eur J Cancer 35 (1999) 214-218
23. 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 USA 90 (1993) 4441-4445
24. 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 (1993) 9262-9266
25. Taylor R.N., Savouret J.-F., Vaisse C., Vigne J.-L., Ryan I., Hornung D., et al. Promegestone (R5020) and mifepristone (RU486) both function as progestational agonists of human glycodelin gene expression in isolated human epithelial cells. J Clin Endocrinol Metab 83 (1998) 4006-4012
26. 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 USA 89 (1992) 3050-3054
27. Delabre K., Guiochon-Mantel A., and Milgrom E. In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Proc Natl Acad Sci USA 90 (1993) 4421-4425
28. Gass E.K., Leonhardt S.A., Nordeen S.K., and Edwards D.P. The antagonists RU486 and ZK98299 stimulate progesterone receptor binding to deoxyribonucleic acid in vitro and in vivo, but have distinct effects on receptor conformation. Endocrinology 139 (1998) 1905-1919
29. Clemm D.L., Macy B.L., Santiso-Mere D., and McDonnell D.P. Definition of the critical cellular components which distinguish between hormone and antihormone activated progesterone receptor. J Steroid Biochem Mol Biol 53 (1995) 487-495
30. 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 (2000) 713-723