Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor

    Herbert G. Bull, Margarita Garcia-Calvo, Stefan Andersson, Walter F. Baginsky, H. Karen Chan, Dina E. Ellsworth, Randall F. Miller, Ralph A. Stearns, Raman K. Bakshi, Gary H. Rasmusson, Richard M. Tolman, Robert C. Myers, and John W. Kozarich, Georgianna Harris
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    TLDR Finasteride effectively blocks enzyme causing male pattern baldness.
    This scientific paper from 1996 explores the mechanism by which finasteride inhibits human steroid 5α-reductase, an enzyme involved in the production of dihydrotestosterone (DHT), which is linked to male pattern baldness. The study found that finasteride acts as a potent bisubstrate analog inhibitor, forming a noncovalent complex with the enzyme that is irreversible and has a dissociation constant of K₁* ≤ 3 × 10-13 M. The study provides important insights into the mechanism of action of finasteride, which is commonly used to treat male pattern baldness and benign prostatic hyperplasia.
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