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

Salah, Mohamed, Tahoun, Mariam, Rudzitis-Auth, Jeannette, Stotz, Lisa, Van Koppen, Chris J., Laschke, Matthias W., Abdelsamie, Ahmed S., Frotscher, Martin
2023 · doi:10.22028/d291-43361 · W6963702521
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Researchers developed potent dual inhibitors of steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 with favorable pharmacokinetics for in vivo endometriosis studies.

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Researchers developed and characterized a series of novel small-molecule compounds designed to simultaneously inhibit steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1, two key enzymes in local estrogen biosynthesis. The study evaluated the pharmacological properties of these dual inhibitors, identifying lead candidates with potent enzymatic activity and favorable pharmacokinetic profiles suitable for in vivo testing. These optimized compounds were subsequently tested in an endometriosis mouse model to demonstrate proof-of-concept efficacy in reducing lesion burden through hormonal suppression. This paper is centrally about endometriosis — specifically the development of targeted hormonal therapies validated in a preclinical mouse model of the disease.

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Please use this identifier to cite or link to this item: Volltext verfügbar? / Dokumentlieferung doi:10.22028/D291-43361 | Title: | 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 | | Author(s): | Salah, Mohamed Tahoun, Mariam Rudzitis-Auth, Jeannette Stotz, Lisa van Koppen, Chris J. Laschke, Matthias W. Abdelsamie, Ahmed S. Frotscher, Martin | | Language: | English | | Title: | Journal of Medicinal Chemistry | | Volume: | 66 | | Issue: | 13 | | Pages: | 8975-8992 | | Publisher/Platform: | ACS | | Year of Publication: | 2023 | | Free key words: | Inhibition Peptides And Proteins Plasma Rodent Models Scanning Tunneling Spectroscopy | | DDC notations: | 610 Medicine and health | | Publikation type: | Journal Article | | DOI of the first publication: | 10.1021/acs.jmedchem.3c00571 | | URL of the first publication: | https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c00571 | | Link to this record: | urn:nbn:de:bsz:291--ds-433618 hdl:20.500.11880/38889 http://dx.doi.org/10.22028/D291-43361 | | ISSN: | 1520-4804 0022-2623 | | Date of registration: | 6-Nov-2024 | | Description of the related object: | Supporting Information | | Related object: | https://ndownloader.figstatic.com/collections/6716299/versions/1 | | Faculty: | M - Medizinische Fakultät NT - Naturwissenschaftlich- Technische Fakultät | | Department: | M - Chirurgie M - Frauenheilkunde NT - Pharmazie | | Professorship: | M - Prof. Dr. Michael D. Menger M - Prof. Dr. E.-F. Solomayer NT - Keiner Professur zugeordnet | | 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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