Three-Dimensional Proteome-Wide Scale Screening for the 5-Alpha Reductase Inhibitor Finasteride: Identification of a Novel Off-Target

    April 2021 in “ Journal of Medicinal Chemistry ”
    Silvia Giatti, Alessandro Di Domizio, Silvia Diviccaro … Roberto Cosimo Melcangi
    Studysummary This study suggests that finasteride may inhibit the enzyme PNMT, potentially contributing to its sexual and psychological side effects.
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    Research cited in this study 17

    1. Structure of Human Steroid 5α-Reductase 2 with the Anti-Androgen Drug Finasteride Nature Communications · 2020
    2. Evaluation of Long-Term Efficacy of Finasteride in Korean Men with Androgenetic Alopecia Using the Basic and Specific Classification System Journal of Dermatology · 2018
    3. Safety Concerns When Using Novel Medications to Treat Alopecia Expert Opinion on Drug Safety · 2018
    4. Androgens in Women: Hormone-Modulating Therapies for Androgen-Mediated Cutaneous Disorders Journal of The American Academy of Dermatology · 2018
    5. Treatment of Male Rats with Finasteride, an Inhibitor of 5alpha-Reductase Enzyme, Induces Long-Lasting Effects on Depressive-Like Behavior, Hippocampal Neurogenesis, Neuroinflammation, and Gut Microbiota Composition Psychoneuroendocrinology · 2018
    6. A Review of the FAERS Data on 5-Alpha Reductase Inhibitors: Implications for Postfinasteride Syndrome Urology · 2018
    7. Androgenetic Alopecia: Drug Safety and Therapeutic Strategies Expert Opinion on Drug Safety · 2018
    8. Assessing Finasteride-Associated Sexual Dysfunction Using the FAERS Database Journal of The European Academy of Dermatology and Venereology · 2017
    9. Cinnamomi Cortex (Cinnamomum Verum) Suppresses Testosterone-Induced Benign Prostatic Hyperplasia by Regulating 5α-Reductase Scientific Reports · 2016
    10. Long-Term Safety and Efficacy of Dutasteride in the Treatment of Male Patients with Androgenetic Alopecia Journal of Dermatology · 2016
    11. Effects of Subchronic Finasteride Treatment and Withdrawal on Neuroactive Steroid Levels and Their Receptors in the Male Rat Brain Neuroendocrinology · 2015
    12. Adverse Event Reporting in Clinical Trials of Finasteride for Androgenic Alopecia: A Meta-Analysis PubMed · 2015
    13. Depressive Symptoms and Suicidal Thoughts Among Former Users of Finasteride With Persistent Sexual Side Effects The Journal of Clinical Psychiatry · 2012
    14. Inhibition of Human Steroid 5β-Reductase (AKR1D1) by Finasteride and Structure of the Enzyme-Inhibitor Complex Journal of Biological Chemistry · 2009
    15. Depression Related to Finasteride Administration for Androgenetic Alopecia Journal of Dermatology · 2002
    16. Finasteride in the Treatment of Men with Androgenetic Alopecia Journal of The American Academy of Dermatology · 1998
    17. Effects of the 5α-Reductase Inhibitor Finasteride on Serum Levels of Gonadal, Adrenal, and Hypophyseal Hormones and Its Clinical Significance: A Prospective Clinical Study Steroids · 1998

    Related research 3

    1. Intraethnic Variation in Steroid-5-Alpha-Reductase Polymorphisms in Prostate Cancer Patients: A Potential Factor Implicated in 5-Alpha-Reductase Inhibitor Treatment Journal of Genetics/Journal of genetics · 2015
    2. Determination of Rat 5α-Reductase Type 1 Isozyme Activity and Its Inhibition by Novel Steroidal Oxazolines Acta Biologica Hungarica · 2010
    3. Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor Journal of the American Chemical Society · 1996