Target intelligence / Profile preview

Steroid 5α-reductase type 1 (SRD5A1)

Target
SRD5A1
Molecular classification
Enzyme, Oxidoreductase, Membrane protein
01

Overview

Steroid 5α-reductase type 1 (SRD5A1) is a membrane-bound, NADPH-dependent oxidoreductase that catalyzes the 5α-reduction of 3-oxo-Δ4 steroids such as testosterone and androstenedione, converting them to dihydrotestosterone (DHT) and related 5α-reduced metabolites. SRD5A1 is expressed in a wide range of tissues, including peripheral tissues (skin, liver) and the central nervous system, where it plays a critical role in steroid hormone metabolism and neurosteroid synthesis. The enzyme is implicated in various pathophysiological conditions, particularly those related to androgen signaling and neurosteroid balance, including prostate cancer, BPH, androgenetic alopecia, and certain CNS disorders. Pharmacological inhibitors of SRD5A1, such as dutasteride, are clinically utilized to modulate androgenic activity for the treatment of BPH and related conditions

Other names
5α-reductase 15 alpha-reductase type ISRD5A1Type 1 5α-reductase
02

Mechanism of action

Competitive inhibition of the enzyme’s active site, preventing the binding and reduction of steroid substrates (e.g., dutasteride and finasteride bind to the reductase, inhibiting the conversion of testosterone and other steroids to their 5α-reduced forms)

03

Biological functions

Steroid hormone metabolism5α-reduction of 3-oxo-Δ4 steroids (e.g., converting testosterone and androstenedione to 5α-dihydro-forms)Neurosteroid synthesis in the central nervous systemModulation of hormonal activity in peripheral and central tissues
04

Disease associations

Cancer (particularly prostate cancer and castration-resistant prostate cancer)Androgen disorders (e.g., androgenic alopecia, hirsutism)Benign prostatic hyperplasia (BPH)Neuropsychiatric and neurodegenerative diseases (by alteration of neurosteroid synthesis)
05

Safety considerations

Off-target hormonal effects (sexual dysfunction, decreased libido, gynecomastia from hormone imbalance)Potential impact on neurosteroid synthesis and related CNS functionsVariable inhibition efficacy and side effect profiles across different patient populationsPotential long-term effects of hormonal suppression remain incompletely understood
06

Interacting drugs

Dutasteride (inhibits both SRD5A1 and SRD5A2)

2 more in the full profile.

07

Biomarkers

SRD5A1 mRNA or protein expression in tissues (especially in malignancies)Enzyme activity levels (can indicate disease progression, especially in prostate cancer)

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