Sulfation of tibolone and tibolone metabolites by expressed human cytosolic sulfotransferases

@article{Falany2004SulfationOT,
  title={Sulfation of tibolone and tibolone metabolites by expressed human cytosolic sulfotransferases},
  author={Josie L. Falany and Nancy Macrina and Charles N. Falany},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2004},
  volume={88},
  pages={383-391}
}
Tibolone is an important therapeutic agent used in the treatment of menopausal symptoms in many countries and has beneficial effects on menopausal and postmenopausal vasomotor, bone, vaginal and mood symptoms without affecting the endometrial, breast or cardiovascular systems. The rapid metabolism of tibolone to active metabolites including 3alpha-OH-tibolone, 3beta-OH-tibolone and Delta(4)-tibolone may be important in its tissue-specific effects. Sulfation also has a major role in the… Expand
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Effect of tibolone and its principal metabolites (3α- and 3β-hydroxy, 3α-sulfate, and 4-ene derivatives) on estrone sulfatase activity in normal and cancerous human breast tissue
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  • J. Falany, C. Falany
  • Chemistry, Medicine
  • The Journal of Steroid Biochemistry and Molecular Biology
  • 2007
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Progestagenic Effects of Tibolone are Target Gene—Specific In Human Endometrial Cells
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The data showed that Tib and Δ4Tib exhibited clear progestagenic effects in endometrial glandular cells by inducing 17βHSD and SULT1E1, while in stromal cells the response was weaker in the induction of PRL and had little effect on IGFBP1. Expand
Effects of Human Sulfotransferase 2A1 Genetic Polymorphisms 3 on the Sulfation of Tibolone
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Kinetic analysis revealed that different SULT2A1 allozymes exhibited differential substrate affinity and catalytic efficiency toward the two substrates tested, which provided useful information concerning the differential metabolism of tibolone through sulfation in individuals with different Sult2A 1 genotypes. Expand
Levels of Tibolone and Estradiol and their Nonsulfated and Sulfated Metabolites in Serum, Myometrium, and Vagina of Postmenopausal Women Following Treatment for 21 Days With Tibolone, Estradiol, or Estradiol Plus Medroxyprogestrone Acetate
TLDR
Serum and tissue levels of endogenous and exogenous E1, E2, and E 1S were markedly increased 20 hours after E2 or E2 + MPA; the percentage of E1S and tissue:serum ratios were not affected. Expand
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