779
Views
8
CrossRef citations to date
0
Altmetric
Research Article

In vivo and in vitro effect of androstene derivatives as 5α-reductase type 1 enzyme inhibitors

, , , , &
Pages 1247-1254 | Received 11 Jul 2012, Accepted 11 Sep 2012, Published online: 10 Oct 2012

References

  • Russell DW, Wilson JD. Steroid 5 alpha-reductase: two genes/two enzymes. Annu Rev Biochem 1994;63:25–61.
  • Bonkhoff H, Stein U, Aumüller G, Remberger K. Differential expression of 5 alpha-reductase isoenzymes in the human prostate and prostatic carcinomas. Prostate 1996;29:261–267.
  • Cabeza M, Heuze Y, Quintana H, Bratoeff E. Comparison between two different hamster models used for the determination of testosterone and finasteride activity. Asian Journal Animal and Veterinary Advances 2010;5:202–209.
  • Takayasu S, Adachi K. The in vivo and in vitro conversion of testosterone to 17 -hydroxy-5 -adrosten-3-one (dihydrotestosterone) by the sebaceous gland of hamsters. Endocrinology 1972;90:73–80.
  • Shiba K, Hamaguchi T, Kataoka K, Yamaguchi Y, Handa H, Adachi K. Cloning of the hamster androgen receptor gene. J Dermatol Sci 2001;26:163–168.
  • Chen C, Puy LA, Simard J, Li X, Singh SM, Labrie F. Local and systemic reduction by topical finasteride or flutamide of hamster flank organ size and enzyme activity. J Invest Dermatol 1995;105:678–682.
  • Arellano Y, Bratoeff E, Garrido M, Soriano J, Heuze Y, Cabeza M. New ester derivatives of dehydroepiandrosterone as 5a-reductase inhibitors. Steroids 2011;76:1241–1246.
  • Long BJ, Grigoryev DN, Nnane IP, Liu Y, Ling YZ, Brodie AM. Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer. Cancer Res 2000;60:6630–6640.
  • Marwah P, Marwah A, Lardy HA, Miyamoto H, Chang C. C19-steroids as androgen receptor modulators: design, discovery, and structure-activity relationship of new steroidal androgen receptor antagonists. Bioorg Med Chem 2006;14:5933–5947.
  • Bradford MM. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 1976;72:248–254.
  • Levy MA, Brandt M, Greway AT. Mechanistic studies with solubilized rat liver steroid 5 alpha-reductase: elucidation of the kinetic mechanism. Biochemistry 1990;29:2808–2815.
  • Davies P, Thomas P, Griffiths K. Measurement of free and occupied cytoplasmic and nuclear androgen receptor sites in rat ventral prostate gland. J Endocrinol 1977;74:393–404.
  • Cabeza M, Vilchis F, Lemus AE, Díaz de León L, Pérez-Palacios G. Molecular interactions of levonorgestrel and its 5 alpha-reduced derivative with androgen receptors in hamster flanking organs. Steroids 1995;60:630–635.
  • Hirosumi J, Nakayama O, Fagan T, Sawada K, Chida N, Inami M et al. FK143, a novel nonsteroidal inhibitor of steroid 5 alpha-reductase: (1) In vitro effects on human and animal prostatic enzymes. J Steroid Biochem Mol Biol 1995;52:357–363.
  • Bratoeff E, Sainz T, Cabeza M, Heuze I, Recillas S, Pérez V et al. Steroids with a carbamate function at C-17, a novel class of inhibitors for human and hamster steroid 5alpha-reductase. J Steroid Biochem Mol Biol 2007;107:48–56.
  • Weisser H, Krieg M. Kinetic analysis of androstenedione 5 alpha-reductase in epithelium and stroma of human prostate. Steroids 1997;62:589–594.
  • Hechter O, Mechaber D, Zwick A, Campfield LA, Eychenne B, Baulieu EE et al. Optimal radioligand exchange conditions for measurement of occupied androgen receptor sites in rat ventral prostate. Arch Biochem Biophys 1983;224:49–68.
  • Normington K, Russell DW. Tissue distribution and kinetic characteristics of rat steroid 5 alpha-reductase isozymes. Evidence for distinct physiological functions. J Biol Chem 1992;267:19548–19554.
  • Segel IH. Enzyme kinetics. Behavior and analysis of rapid equilibrium and steady state enzyme systems. New York: John Wiley & Sons, Inc., 1993.
  • Cabeza M, Trejo KV, González C, García P, Soriano J, Heuze Y et al. Steroidal 5a-reductase inhibitors using 4-androstenedione as substrate. J Enzyme Inhib Med Chem 2011;26:712–719.
  • Thomas LN, Douglas RC, Rittmaster RS, Too CK. Overexpression of 5 alpha-reductase type 1 increases sensitivity of prostate cancer cells to low concentrations of testosterone. Prostate 2009;69:595–602.
  • Dadras SS, Cai X, Abasolo I, Wang Z. Inhibition of 5alpha-reductase in rat prostate reveals differential regulation of androgen-response gene expression by testosterone and dihydrotestosterone. Gene Expr 2001;9:183–194.
  • Goldenberg L, So A, Fleshner N, Rendon R, Drachenberg D, Elhilali M. The role of 5-alpha reductase inhibitors in prostate pathophysiology: Is there an additional advantage to inhibition of type 1 isoenzyme? Can Urol Assoc J 2009;3:S109–S114.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.