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Steroid 5α-reductase 2 is an integral membrane enzyme that catalyzes the NADPH-dependent reduction of testosterone and other Δ^4-3-keto steroids to their corresponding 5α-reduced forms, notably converting testosterone into dihydrotestosterone (DHT), a more potent androgen critical for male sexual development and prostate growth. Mutations in the SRD5A2 gene cause 5α-reductase deficiency, leading to undervirilization and other developmental disorders. Inhibition of SRD5A2 by agents such as finasteride and dutasteride is a mainstay therapy for benign prostatic hyperplasia and is also used to treat androgen-dependent conditions. The enzyme is a seven-transmembrane protein, structurally related to other steroid/sterol reductases, uses NADPH as a cofactor, and is subject to pathological mutations that can lead to disease[1][2][3][4][5][7].
Competitive inhibition of SRD5A2, blocking conversion of testosterone to DHT and thereby lowering androgenic activity in target tissues
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