The nature of inhibition of steroid sulphatase activity by tibolone and its metabolites

Journal of Steroid Biochemistry and Molecular Biology

Volumn 94, Issue 1-3 SPEC. ISS., 2005, Pages 229-237

  Raobaikady, B ^a   Day, J M ^a   Purohit, A ^a   Potter, B V L ^b   Reed, M J ^a  

^a ST MARY S HOSPITAL   (United Kingdom)

^b University of Bath   (United Kingdom)

Author keywords

Hormone replacement therapy; Menopause; Steroid; Sulphatase; Tibolone

Indexed keywords

STERYL SULFATASE; TIBOLONE;

ARTICLE; BREAST CANCER; CANCER CELL; CELL ACTIVITY; CHORIOCARCINOMA; CONCENTRATION RESPONSE; CONTROLLED STUDY; CULTURE MEDIUM; DRUG ACTIVITY; DRUG INHIBITION; ENZYME ACTIVITY; ENZYME KINETICS; HUMAN; HUMAN CELL; OSTEOBLAST;

ILEX COOKII; MINK CELL FOCUS-FORMING VIRUS;

EID: 18144375199     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jsbmb.2005.01.021     Document Type: Article

References (29)

1. K. Modelska, and S. Cummings Tibolone for postmenopausal women: systematic review of randomised trials J. Clin. Endocrinol. Metab. 87 2002 16 23
2. P. Albertazzi, R. Di Micco, and E. Zanardi Tibolone: a review Maturitas 30 1989 295 305
3. H.L. Kloosterboer Intracrinology: the secret of the tissue-specificity of tibolone J. Br. Menopause Soc. 6 2000 23 27
4. L. Markiewicz, and E. Gurpide In vitro evaluation of estrogenic, estrogen antagonistic and progestagenic effects of a steroidal drug (Org OD14) and its metabolites on human endometrium J. Steroid Biochem. 35 1990 535 541
5. M.J. Reed, and H.L. Kloosterboer Tibolone: a selective tissue estrogenic activity regulator (STEAR) Maturitas 48 Suppl. 1 2004 S4 S6
6. M.J. Reed Role of enzymes and tissue-specific actions of steroids Maturitas 48 Suppl. 1 2004 S18 S23
7. B. Tang, L. Markiewicz, H.J. Kloosterboer, and E. Gurpide Human endometrial 3β-hydroxysteroid dehydrogenase/isomerase can locally reduce intrinsic estrogenic/progestogenic activity ratios of a steroidal drug (Org 14) J. Steroid Biochem. Mol. Biol. 45 1993 345 351
8. I. Valdivia, and D. Ortega Mammographic density in postmenopausal women treated with tibolone, estriol or conventional hormone replacement therapy Clin. Drug Invest. 20 2000 101 107
9. R.A. Moore Livial: a review of clinical studies Br. J. Obstet. Gynaecol. 106 Suppl. 19 1999 1 21
10. G. Chetrite, H.J. Kloosterboer, and J.R. Pasqualini Effect of tibolone (Org OD14) and its metabolites on estrone sulphatase activity in MCF-7 and T-47D mammary cancer cells Anticancer Res. 17 1997 135 140
11. A. Purohit, B. Malini, and C. Hooymans Inhibition of oestrone sulphatase activity by tibolone and its metabolites Horm. Metab. Res. 34 2002 1 6
12. Y. Miki, T. Nakata, T. Suzuki, A.D. Darnel, T. Moriya, C. Kaneko, K. Hidaka, Y. Shiotsu, H. Kusaka, and H. Sasano Systemic distribution of steroid sulfatase and estrogen sulfotransferase in human adult and fetal tissues J. Clin. Endocrinol. Metab. 87 2002 5760 5768
13. Y. Miyoshi, A. Ando, S. Hasegawa, M. Ishitobi, T. Taguchi, Y. Tamaki, and S. Noguchi High expression of steroid sulfatase mRNA predicts poor prognosis in patients with estrogen receptor-positive breast cancer Clin. Cancer Res. 9 2003 2288 2293
14. R.C. Bonney, M.J. Reed, K. Davidson, P.A. Beranek, and V.H.T. James The relationship between 17β-hydroxysteroid dehydrogenase activity and oestrogen concentrations in human breast tumours and in normal breast tissue Clin. Endocrinol. 19 1983 727 739
15. M.J. Reed, A. Purohit, L.W.L. Woo, and B.V.L. Potter The development of steroid sulphatase inhibitors Endocr. Relat. Cancer 3 1996 9 23
16. L. Delbressine, M. De Gooyer, and H.L. Kloosterboer Sulphated metabolites of tibolone show sulphatase inhibiting activity Prog. ENDO 2000 396
17. N.M. Howarth, A. Purohit, M.J. Reed, and B.V.L. Potter Estrone sulfamates: potent inhibitors of estrone sulfatase activity with therapeutic potential J. Med. Chem. 37 1994 219 221
18. L. Duncan, A. Purohit, N.M. Howarth, B.V.L. Potter, and M.J. Reed Inhibition of estrone sulfatase activity by estrone-3-methylthiophosphonate - a potential therapeutic agent in breast cancer Cancer Res. 53 1993 298 303
19. A. Purohit, and M.J. Reed Oestrogen sulphatase activity in hormone-dependent breast cancer cells: modulation by steroidal and non-steroidal therapeutic agents Int. J. Cancer 50 1992 901 905
20. A. Purohit, G.A. Williams, N.-M. Howarth, B.V.L. Potter, and M.J. Reed Inactivation of steroid sulfatase by an active site-directed inhibitor, estrone-3-O-sulfamate Biochemistry 34 1995 11508 11514
21. H.J. Kloosterboer Tibolone: a steroid with a tissue-specific mode of action J. Steroid Biochem. Mol. Biol. 76 2001 231 238
22. G.S. Chetrite, H.J. Kloosterboer, J.-C. Philippe, and J.R. Pasqualini Effects of Org OD14 (Livial) and its metabolties on 17β-hydroxysteroid dehydrogenase activity in hormone-dependent MCF-7 and T-47D breast cancer cells Anticancer Res. 19 1999 261 268
23. G.S. Chetrite, H.J. Kloosterboer, J.-C. Philippe, and J.R. Pasqualini Effect of Org OD14 (Livial) and its metabolites on hormone-dependent MCF-7 and T-47D, and hormone-independent MDA-MB-231 breast cancer cell lines Anticancer Res. 19 1999 269 276
24. T. Nakata, S. Takashima, Y. Shiotsu, C. Murakata, H. Ishida, S. Akinaga, P.K. Li, H. Sasano, T. Suzuki, and T. Saeki Role of steroid sulfatase in local formation of estrogen in post-menopausal breast cancer patients J. Steroid Biochem. Mol. Biol. 86 2003 455 460
25. J. Desreux, H.J. Kloosterboer, A. Noel, F. Frankenne, M. Lemaire, J.M. Foidart, Effects of tibolone (Org OD14) on steroid sulfatase activity and growth of MCF-7 human breast tumors implanted in ovariectomised nude mice, in press.
26. M.E. De Gooyer, G.T. Overklift, V. Kleyn, K.C. Smits, A.G.H. Ederreen, H.A.M. Verheal, and H.J. Kloosterboer Tibolone: a compound with tissue specific inhibitory effects on sulfatase Mol. Cell Endocrinol. 183 2001 55 62
27. R. Hobkirk Steroid sulfation Trends Endocrinol. Metab. 4 1993 69 74
28. J.L. Falany, N. Maerina, and C.N. Falany Sulfation of tibolone metabolites by expressed human cytosolic sulfotransferases J. Steroid Biochem. Mol. Biol. 88 2004 383 391
29. J.I. Raeside, H.L. Christie, L. Forster, and R.L. Renaud Estradiol-17β sulfotransferase activity in canine osteosarcoma D17 cells Biochem. Biophys. Res. Comm. 273 2000 505 508