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

Mohamed, Abdelrahman, Salah, Mohamed, Tahoun, Mariam, Hawner, Manuel, Abdelsamie, Ahmed S., Frotscher, Martin
2022 · doi:10.22028/d291-43386 · W6907822068
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This study developed novel drug-prodrugs targeting steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 as a potential therapeutic strategy for endometriosis.

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This study developed a novel drug-prodrug strategy to simultaneously inhibit steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1, two enzymes critical for local estrogen production. The researchers synthesized and evaluated specific compounds that demonstrated potent dual inhibition capabilities in biochemical assays compared to single-target agents. Preclinical evaluations indicated that these dual inhibitors effectively reduced cell proliferation in models relevant to hormone-dependent tissues. This paper is centrally about endometriosis — specifically proposing a targeted enzymatic inhibition approach as a potential therapeutic option for treating the condition by lowering local estrogen levels.

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Please use this identifier to cite or link to this item: Volltext verfügbar? / Dokumentlieferung doi:10.22028/D291-43386 | Title: | 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 | | Author(s): | Mohamed, Abdelrahman Salah, Mohamed Tahoun, Mariam Hawner, Manuel Abdelsamie, Ahmed S. Frotscher, Martin | | Language: | English | | Title: | Journal of Medicinal Chemistry | | Volume: | 65 | | Issue: | 17 | | Pages: | 11726-11744 | | Publisher/Platform: | ACS | | Year of Publication: | 2022 | | DDC notations: | 500 Science | | Publikation type: | Journal Article | | DOI of the first publication: | 10.1021/acs.jmedchem.2c00589 | | URL of the first publication: | https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c00589 | | Link to this record: | urn:nbn:de:bsz:291--ds-433864 hdl:20.500.11880/38906 http://dx.doi.org/10.22028/D291-43386 | | ISSN: | 1520-4804 0022-2623 | | Date of registration: | 7-Nov-2024 | | Description of the related object: | Supporting Information | | Related object: | https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.2c00589/suppl_file/jm2c00589_si_001.pdf https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.2c00589/suppl_file/jm2c00589_si_002.csv | | Faculty: | NT - Naturwissenschaftlich- Technische Fakultät | | Department: | NT - Pharmazie | | Professorship: | NT - Prof. Dr. Christian Ducho NT - Prof. Dr. Rolf W. Hartmann | | Collections: | SciDok - Der Wissenschaftsserver der Universität des Saarlandes | Files for this record: There are no files associated with this item. Items in SciDok are protected by copyright, with all rights reserved, unless otherwise indicated.

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