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

February 2026 in “ Toxicology Letters ”

Jacek Kędzierski, Rianne E van Diest, Julien Arthur Allard, Andreas M. Erharter, Alex Odermatt, Martin Smieko

5α-reductase SRD5A2 androgen receptor modulator MK-0773 finasteride 5-alpha-reductase Propecia

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 Evolution, Classification, Structure, and Functional Diversification of Steroid 5α-Reductase Family in Eukaryotes

6 citations , July 2024 in “Heliyon”

This study examined the evolutionary and functional homology of steroid 5α-reductase and DET2 proteins, identifying protists as a common ancestor, and discovered a new subclass DET2-like in plants, potentially involved in polyprenol reduction.

research 5α-Reduction of Epitestosterone Is Catalyzed by Human SRD5A1 and SRD5A2 and Increases Androgen Receptor Transactivation

14 citations , April 2024 in “The Journal of Steroid Biochemistry and Molecular Biology”

This study found that epitestosterone, a stereoisomer of testosterone, is metabolized to 5α-dihydroepitestosterone by human 5α-reductase enzymes, which enhances its androgenic activity and reduces its antagonistic effect on testosterone-driven androgen receptor signaling.

research Structure of Human Steroid 5α-Reductase 2 with the Anti-Androgen Drug Finasteride

30 citations , October 2020 in “Nature Communications”

This study provides the first crystal structure of the human SRD5A2 enzyme, revealing key insights into its function and inhibition which may aid future drug development.

research Consequences of Steroid-5α-Reductase Deficiency and Inhibition in Vertebrates

21 citations , January 2020 in “General and Comparative Endocrinology”

This review examines the diverse roles of SRD5α enzymes across species, focusing on their involvement in steroid synthesis, sexual development, and various physiological processes, but reports no new clinical results.

research Post-Finasteride Syndrome: A Surmountable Challenge for Clinicians

30 citations , January 2020 in “Fertility and Sterility”

This review discusses the evidence for post-finasteride syndrome as a condition potentially induced by finasteride and dutasteride, associating them with sexual dysfunction, depression, anxiety, and suicidal ideation in a subset of men, and reports no new clinical results.

research Subcellular Localization of the Five Members of the Human Steroid 5α-Reductase Family

13 citations , June 2017 in “Biochimie open”

This study determined that the human steroid 5α-reductase enzymes localize to the endoplasmic reticulum in HeLa cells, with protein tagging affecting expression and inducing protein aggregates for some isoforms.

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

research 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

211 citations , May 2013 in “Journal of Nutrition Health & Aging”

This study found that while MK-0773 significantly increased lean body mass in sarcopenic frail elderly women, it did not significantly improve muscle strength or physical function compared to placebo.

research The 5 Alpha-Reductase Isozyme Family: A Review of Basic Biology and Their Role in Human Diseases

218 citations , December 2011 in “Advances in Urology”

This review discusses the biochemical properties and clinical significance of 5 alpha-reductase isozymes and reports no new clinical results.

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

research 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

45 citations , August 2010 in “Hormone Molecular Biology and Clinical Investigation”

This study found that SRD5a-3 is a highly efficient enzyme for converting hormones into androgens, with dutasteride being a much more potent inhibitor of SRD5a-3 than SRD5a-2.

research Discovery and Clinical Development of Dutasteride, a Potent Dual 5α-Reductase Inhibitor

58 citations , March 2006 in “Current topics in medicinal chemistry”

This review describes how dutasteride, a dual 5alpha-reductase inhibitor, has improved outcomes in benign prostatic hyperplasia and is being studied for prostate cancer prevention, without new data reported.

research The Clinical Development of a 5α-Reductase Inhibitor, Finasteride

211 citations , November 1990 in “The Journal of Steroid Biochemistry and Molecular Biology”

Finasteride effectively treats BPH, but needs more trials to understand potential.