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Chemical Compound Review

AC1MHU59     (9S,17S)-17-hydroxy-7,13,17- trimethyl-1,2...

Synonyms: LS-64855, BRN 5565683, AC1L2E5G, EINECS 223-046-5, Cheque (Veterinary), ...
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Disease relevance of CDB 904


High impact information on CDB 904

  • In addition, polysome run-off translation assays demonstrated an increase in PCNA protein after a 6-h stimulation of LNCaP cells with 10(-9)M mibolerone [6].
  • A time course study demonstrated that PSA mRNA was induced by mibolerone (a nonmetabolizable synthetic androgen) and reached maximal levels after 9 h [7].
  • Following incubation with androgen (2 nM mibolerone) for 72 h, luciferase activity in normal fibroblasts increased > 10-fold (range 11-200-fold) in a manner that corresponded with the level of androgen receptor detected in ligand-binding assays [8].
  • For this purpose, NIS mRNA and protein expression levels were examined in NP-1 cells by Northern and Western blot analysis, respectively, after incubation with Dex (10(-8)-10(-6) M) in the presence of 10(-9) M mibolerone [9].
  • Binding studies with the mutant receptor in transfected COS-7 cells, with mibolerone as ligand, exhibited equal Kd (0.7 vs. 1.0 nmol/ L), IC50 (0.8 vs. 1.1 nmol/L), and maximum binding (7.1 vs. 8.9 fmol/ 10(6) cells), as compared with the wild-type (WT) receptor [10].

Biological context of CDB 904


Anatomical context of CDB 904


Associations of CDB 904 with other chemical compounds


Gene context of CDB 904

  • Time course analysis revealed that hGK-1 mRNA levels increased significantly at 5 h of mibolerone treatment and reached maximal levels by 9 h [23].
  • There were no effects on cyclin D1 protein or mRNA expression with mibolerone treatments [22].
  • Degradation rate of 35S-labeled AR was significantly increased by GA in the presence or absence of mibolerone [24].
  • The induction of PSA mRNA required as little as 0.3 nM mibolerone [7].
  • Surprisingly, mibolerone was found to bind with high affinity to the progesterone receptor in both human prostate (Kd = 5.9 nM) and rabbit uterus (Kd = 1.1 nM) [25].

Analytical, diagnostic and therapeutic context of CDB 904


  1. Peroxisome proliferator-activated receptor alpha is an androgen-responsive gene in human prostate and is highly expressed in prostatic adenocarcinoma. Collett, G.P., Betts, A.M., Johnson, M.I., Pulimood, A.B., Cook, S., Neal, D.E., Robson, C.N. Clin. Cancer Res. (2000) [Pubmed]
  2. Delayed development of humoral immunity in chickens following in ovo treatment with mibolerone. Bhanushali, J.K., Murthy, K.K., Ragland, W.L. Dev. Comp. Immunol. (1985) [Pubmed]
  3. Response of mibolerone-treated chickens to infectious bursal disease virus. Lucio, B., Hitchner, S.B. Avian Dis. (1980) [Pubmed]
  4. Efficacy and dosage titration study of mibolerone for treatment of pseudopregnancy in the bitch. Brown, J.M. J. Am. Vet. Med. Assoc. (1984) [Pubmed]
  5. Canine ovarian fibroma associated with prolonged exposure to mibolerone. Seaman, W.J. Toxicologic pathology. (1985) [Pubmed]
  6. Androgens regulate the expression of proliferating cell nuclear antigen posttranscriptionally in the human prostate cancer cell line, LNCaP. Perry, J.E., Tindall, D.J. Cancer Res. (1996) [Pubmed]
  7. Hormonal regulation of prostate-specific antigen messenger RNA in human prostatic adenocarcinoma cell line LNCaP. Young, C.Y., Montgomery, B.T., Andrews, P.E., Qui, S.D., Bilhartz, D.L., Tindall, D.J. Cancer Res. (1991) [Pubmed]
  8. The adenovirus-mediated delivery of a reporter gene permits the assessment of androgen receptor function in genital skin fibroblast cultures. Stimulation of Gs and inhibition of G(o). McPhaul, M.J., Deslypere, J.P., Allman, D.R., Gerard, R.D. J. Biol. Chem. (1993) [Pubmed]
  9. Dexamethasone enhances the cytotoxic effect of radioiodine therapy in prostate cancer cells expressing the sodium iodide symporter. Scholz, I.V., Cengic, N., Göke, B., Morris, J.C., Spitzweg, C. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  10. Preserved male fertility despite decreased androgen sensitivity caused by a mutation in the ligand-binding domain of the androgen receptor gene. Giwercman, A., Kledal, T., Schwartz, M., Giwercman, Y.L., Leffers, H., Zazzi, H., Wedell, A., Skakkebaek, N.E. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  11. A mutation of the androgen receptor associated with partial androgen resistance, familial gynecomastia, and fertility. Grino, P.B., Griffin, J.E., Cushard, W.G., Wilson, J.D. J. Clin. Endocrinol. Metab. (1988) [Pubmed]
  12. The human ovarian surface epithelium is an androgen responsive tissue. Edmondson, R.J., Monaghan, J.M., Davies, B.R. Br. J. Cancer (2002) [Pubmed]
  13. Role of microsomal receptors in steroid hormone action. Steinsapir, J., Muldoon, T.G. Steroids (1991) [Pubmed]
  14. Evidence for a novel mechanism of androgen resistance in the human prostate cancer cell line, PC-3. Tilley, W.D., Bentel, J.M., Aspinall, J.O., Hall, R.E., Horsfall, D.J. Steroids (1995) [Pubmed]
  15. Relative binding properties of microsomal and cytosolic androgen receptor species of the ventral prostate. Steinsapir, J., Bryhan, M., Muldoon, T.G. Endocrinology (1989) [Pubmed]
  16. Retinoic acid-induced stimulation of sodium iodide symporter expression and cytotoxicity of radioiodine in prostate cancer cells. Spitzweg, C., Scholz, I.V., Bergert, E.R., Tindall, D.J., Young, C.Y., Göke, B., Morris, J.C. Endocrinology (2003) [Pubmed]
  17. Follicle-stimulating hormone and androgens increase the concentration of the androgen receptor in Sertoli cells. Verhoeven, G., Cailleau, J. Endocrinology (1988) [Pubmed]
  18. Binding of 7 alpha, 17 alpha-dimethyl-19-nortestosterone (mibolerone) to androgen and progesterone receptors in human and animal tissues. Traish, A.M., Müller, R.E., Wotiz, H.H. Endocrinology (1986) [Pubmed]
  19. Discordant measures of androgen-binding kinetics in two mutant androgen receptors causing mild or partial androgen insensitivity, respectively. Shkolny, D.L., Beitel, L.K., Ginsberg, J., Pekeles, G., Arbour, L., Pinsky, L., Trifiro, M.A. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  20. Androgens inhibit estradiol-17beta synthesis in Atlantic croaker (Micropogonias undulatus) ovaries by a nongenomic mechanism initiated at the cell surface. Braun, A.M., Thomas, P. Biol. Reprod. (2003) [Pubmed]
  21. An autoregulatory process for androgen production in rat thecal-interstitial cells. Simone, D.A., Mahesh, V.B. Biol. Reprod. (1993) [Pubmed]
  22. Epidermal growth factor induces cyclin D1 in a human prostate cancer cell line. Perry, J.E., Grossmann, M.E., Tindall, D.J. Prostate (1998) [Pubmed]
  23. Tissue-specific and hormonal regulation of human prostate-specific glandular kallikrein. Young, C.Y., Andrews, P.E., Montgomery, B.T., Tindall, D.J. Biochemistry (1992) [Pubmed]
  24. Effect of geldanamycin on androgen receptor function and stability. Vanaja, D.K., Mitchell, S.H., Toft, D.O., Young, C.Y. Cell Stress Chaperones (2002) [Pubmed]
  25. Characterization of steroid receptors in human prostate using mibolerone. Murthy, L.R., Johnson, M.P., Rowley, D.R., Young, C.Y., Scardino, P.T., Tindall, D.J. Prostate (1986) [Pubmed]
  26. Partial androgen insensitivity caused by an androgen receptor mutation at amino acid 907 (Gly-->Arg) that results in decreased ligand binding affinity and reduced androgen receptor messenger ribonucleic acid levels. Choong, C.S., Sturm, M.J., Strophair, J.A., McCulloch, R.K., Tilley, W.D., Leedman, P.J., Hurley, D.M. J. Clin. Endocrinol. Metab. (1996) [Pubmed]
  27. Effects of androgen on intracellular calcium of LNCaP cells. Steinsapir, J., Socci, R., Reinach, P. Biochem. Biophys. Res. Commun. (1991) [Pubmed]
  28. Chickens bursectomized with mibolerone have Ig-positive cells which lack bursal cell specific antigens. Bhanushali, J.K., Ragland, W.L. Vet. Immunol. Immunopathol. (1985) [Pubmed]
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