Target intelligence / Profile preview

Steroid 5-alpha-reductase enzyme (5α-reductase)

Target
5α-reductase
Molecular classification
Enzyme, Oxidoreductase
01

Overview

Steroid 5-alpha-reductase enzyme is a family of membrane-bound oxidoreductase enzymes that catalyze the irreversible reduction of the Δ⁴,⁵ double bond in 3-oxo (3-keto) C19 or C21 steroids, converting testosterone into the more potent androgen dihydrotestosterone (DHT) using NADPH as a cofactor[1][5]. There are three main human isozymes (types 1, 2, and 3) encoded by SRD5A1, SRD5A2, and SRD5A3 genes, each with distinctive tissue distributions and roles[1][4][5]. Type 2 is critical in male sexual differentiation and external genital development, and its deficiency causes 5-alpha-reductase deficiency. Inhibition of these enzymes is a validated therapeutic approach in prostate disorders (BPH, cancer), androgenetic alopecia, and hirsutism, with finasteride and dutasteride being principal drugs[7]. The enzyme is expressed in the skin, prostate, reproductive organs, liver, and nervous system[5]. Safety concerns for inhibitors include sexual dysfunction, fertility effects, and potential teratogenic risk.

Other names
3-oxo-5α-steroid 4-dehydrogenase5-alpha-reductase5α-RSRD5A (gene family abbreviation)Steroid 5α-reductase isoenzyme 1 (SRD5A1)Steroid 5α-reductase isoenzyme 2 (SRD5A2)Steroid 5α-reductase isoenzyme 3 (SRD5A3)
02

Mechanism of action

Enzyme inhibition (prevents conversion of testosterone to DHT) Selective blockade (Type 1, Type 2, or both isoenzymes, depending on the drug)

03

Biological functions

Steroid metabolismAndrogen metabolismConversion of testosterone to dihydrotestosterone (DHT)Bile acid biosynthesisEstrogen metabolism
04

Disease associations

Prostate cancerBenign prostatic hyperplasia (BPH)Androgenetic alopecia (male-pattern baldness)AcnePolycystic ovarian syndrome (PCOS)Disorders of sexual differentiation (e.g., 5-alpha-reductase deficiency)Hirsutism
05

Safety considerations

Sexual dysfunction (e.g., decreased libido, erectile dysfunction)Reduced fertilityPossible psychiatric effects (e.g., depression, rarely reported)Potential impact on fetal male genital development (teratogenicity risk in pregnancy)Effects on metabolic parameters (e.g., insulin sensitivity, hepatic steatosis with certain inhibitors)
06

Interacting drugs

Finasteride

3 more in the full profile.

07

Biomarkers

DHT (dihydrotestosterone) levelsChanges in serum or tissue testosterone:DHT ratios

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