Targeting Steroid-Metabolizing Enzymes with 15β-Substituted Estrone Analogues: Dual Discovery of AKR1C2/17β-HSD1 Inhibitors and a Fluorescent 17β-HSD1 Ligand

Resch, Vivien Erzsébet and Gjorgoska, Marija and Hafner, Eva and Bacsa, Ildikó and Kovács, Benjamin and Büdefeld, Tomaž and Hunyadi, Attila and Huliák, Ildikó and Csontné Kiricsi, Mónika and Paragi, Gábor and Lanišnik Rižner, Tea and Mernyák, Erzsébet (2026) Targeting Steroid-Metabolizing Enzymes with 15β-Substituted Estrone Analogues: Dual Discovery of AKR1C2/17β-HSD1 Inhibitors and a Fluorescent 17β-HSD1 Ligand. CANCERS, 18 (12). no.-1889. ISSN 2072-6694

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Abstract

Hormone-dependent cancers such as breast, endometrial, and ovarian cancers often rely on enzymes that control estrogen production and activity, making these enzymes attractive targets for new treatments. This study aimed to evaluate structurally modified estrone derivatives that can block key enzymes involved in estrogen metabolism, with the goal of reducing cancer cell growth and improving target selectivity. The present findings identify D-ring-modified estrone derivatives as promising single- and dual-target inhibitors and introduce a fluorescent probe suitable for investigating intracellular steroid metabolism in hormone-dependent malignancies.

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