Results 201 to 210 of about 452,915 (259)

Adipose Tissue Sex Steroids in Postmenopausal Women With and Without Menopausal Hormone Therapy.

J Clin Endocrinol Metab
Hetemäki N, Robciuc A, Vihma V, Haanpää M, Hämäläinen E, Tikkanen MJ, Mikkola TS, Savolainen-Peltonen H.   +7 more
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Steroid sulfatase inhibitors: the current landscape

Expert Opinion on Therapeutic Patents, 2021
Introduction: Steroid sulfatase (STS) enzyme is responsible for transforming the inactive sulfate metabolites of steroid sex hormones into the active free steroids. Both the deficiency and the over-expression of STS are associated with the pathophysiology of certain diseases.
Joudi H Zib, Mariam A Jameel, Hanan S. Anbar, Aya F Jawad, Mohammed I. El-Gamal, Mohammed I. El-Gamal, Aya M Samer, Jana J Elounais, Zahraa Isa   +8 more
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Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for In Vivo Proof-of-Principle Studies in an Endometriosis Mouse Model.

Journal of Medicinal Chemistry, 2023
Treating estrogen-dependent diseases like endometriosis with drugs suppressing local estrogen activation may be superior to existing endocrine therapies.
Mohamed Salah, Mariam Tahoun, Jeannette Rudzitis-Auth, L. Stotz, C. V. van Koppen, M. Laschke, Ahmed S. Abdelsamie, Martin Frotscher   +7 more
semanticscholar   +1 more source

Design, structure-activity relationships, and enzyme kinetic studies of tricyclic and tetracyclic coumarin-based sulfamates as steroid sulfatase inhibitors.

Bioorganic chemistry (Print), 2023
Inhibition of steroid sulfatase (STS) decreases estrogen production and thus, suppresses tumor proliferation. Inspired by irosustat, the first STS inhibitor in clinical trials, we explored twenty-one tricyclic and tetra-heterocyclic coumarin-based ...
Pei-Fang Chiu, I. Lin, Yeh-Lin Lu, Chiao-Nien Chang, Hui-Yu Chan, Tzung-Shen Lin, K. Tsai, Yves S. Y. Hsieh, Mei-Jou Chen, Mei-Hsiang Lin, Pi-Hui Liang   +10 more
semanticscholar   +1 more source

Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.

Journal of Medicinal Chemistry, 2022
A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group with a sulfamate ester.
A. Mohamed, Mohamed Salah, Mariam Tahoun, Manuel Hawner, Ahmed S. Abdelsamie, Martin Frotscher   +5 more
semanticscholar   +1 more source

The Design, Structure-Activity, and kinetic studies of 3-Benzyl-5-oxa-1,2,3,4-Tetrahydro-2H-chromeno-(3,4-c)pyridin-8-yl sulfamates as Steroid sulfatase inhibitors.

Bioorganic chemistry (Print), 2022
Steroid sulfatase inhibitors block the local production of estrogenic steroids and are attractive agents for the treatment of estrogen-dependent cancers.
Chiao-Nien Chang, I. Lin, Tzung-Sheng Lin, Pei-Fang Chiu, Yeh-Lin Lu, Manmath Narwane, I-Chen Liu, Yue Hng, K. Tsai, Mei-Hsiang Lin, Yves S. Y. Hsieh, Mei-Jou Chen, Pi-Hui Liang   +12 more
semanticscholar   +1 more source

Dual aromatase-steroid sulfatase inhibitors (DASI's) for the treatment of breast cancer: a structure guided ligand based designing approach

Journal of Biomolecular Structure and Dynamics, 2022
Dual aromatase-steroid sulfatase inhibitors (DASIs) lead to significant deprivation of estrogen levels as compared to a single target inhibition and thereby exhibited an additive or synergistic effect in the treatment of hormone-dependent breast cancer ...
Yogesh Singh, S. Jaswal, Satwinder Singh, S. K. Verma, Suresh Thareja   +4 more
semanticscholar   +1 more source

Steroid sulfatase inhibitors

Expert Opinion on Therapeutic Patents, 2003
AbstractSteroid sulfatase (STS) regulates the local production of estrogens and androgens from systemic precursors in several tissues. The enzyme catalyzes the hydrolysis of the sulfate esters of 3‐hydroxy steroids, which are inactive transport or precursor forms of the active 3‐hydroxy steroids.
Andreas Billich, Peter Nussbaumer
openaire   +5 more sources

Steroid derivatives as inhibitors of steroid sulfatase

The Journal of Steroid Biochemistry and Molecular Biology, 2013
Sulfated steroids function as a storage reservoir of biologically active steroid hormones. The sulfated steroids themselves are biologically inactive and only become active in vivo when they are converted into their desulfated (unconjugated) form by the enzyme steroid sulfatase (STS).
Yaser A. Mostafa, Scott D. Taylor
openaire   +2 more sources

Steroid sulfatase inhibitors

Expert Opinion on Therapeutic Patents, 1999
Steroid sulfatase catalyses the hydrolysis of sulfated steroids to their corresponding hydroxylated forms. Since oestrogens and androgens can be synthesised intracellularly from the abundant circulating sulfated steroids, steroid sulfatase inhibitors should prove to be valuable therapeutic agents for the treatment of hormono-dependent diseases ...
Liviu C. Ciobanu, René Maltais, Donald Poirier   +2 more
openaire   +2 more sources