Identification of Xenobiotics Interfering with 5α-Reductase (SRD5A2) Activity

    February 2026 in “ Toxicology Letters ”
    Jacek Kędzierski, Rianne E van Diest, Julien Arthur Allard … Martin Smieko
    Studysummary This study used an in silico/in vitro approach to identify potential inhibitors of the enzyme SRD5A2, finding that the androgen receptor modulator MK-0773 is a moderate inhibitor, although it does not act as a covalent inhibitor like finasteride.
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    Research cited in this study 11

    1. Evolution, Classification, Structure, and Functional Diversification of Steroid 5α-Reductase Family in Eukaryotes Heliyon · 2024
    2. 5α-Reduction of Epitestosterone Is Catalyzed by Human SRD5A1 and SRD5A2 and Increases Androgen Receptor Transactivation The Journal of Steroid Biochemistry and Molecular Biology · 2024
    3. Structure of Human Steroid 5α-Reductase 2 with the Anti-Androgen Drug Finasteride Nature Communications · 2020
    4. Consequences of Steroid-5α-Reductase Deficiency and Inhibition in Vertebrates General and Comparative Endocrinology · 2020
    5. Post-Finasteride Syndrome: A Surmountable Challenge for Clinicians Fertility and Sterility · 2020
    6. Subcellular Localization of the Five Members of the Human Steroid 5α-Reductase Family Biochimie open · 2017
    7. A Phase IIA Randomized, Placebo-Controlled Clinical Trial to Study the Efficacy and Safety of the Selective Androgen Receptor Modulator (SARM), MK-0773 in Female Participants with Sarcopenia Journal of Nutrition Health & Aging · 2013
    8. The 5 Alpha-Reductase Isozyme Family: A Review of Basic Biology and Their Role in Human Diseases Advances in Urology · 2011
    9. Human Type 3 5α-Reductase Is Expressed in Peripheral Tissues at Higher Levels Than Types 1 and 2 and Its Activity Is Potently Inhibited by Finasteride and Dutasteride Hormone Molecular Biology and Clinical Investigation · 2010
    10. Discovery and Clinical Development of Dutasteride, a Potent Dual 5α-Reductase Inhibitor Current topics in medicinal chemistry · 2006
    11. The Clinical Development of a 5α-Reductase Inhibitor, Finasteride The Journal of Steroid Biochemistry and Molecular Biology · 1990