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The testosterone biosynthetic pathway details the multi-step enzymatic conversion of cholesterol to testosterone. Key steps include cholesterol side-chain cleavage (CYP11A1), 17α-hydroxylation/lyase activity of CYP17A1, and the reduction of androstenedione to testosterone via 17β-hydroxysteroid dehydrogenase (HSD17B3 in the testes). The process includes Δ4 and Δ5 sub-pathways, with humans predominantly using the Δ5 variant. This pathway is essential for androgen production in the testes, adrenal glands, ovaries, and placenta, with dysregulation implicated in prostate cancer, androgen deficiency, and other endocrine conditions[1][2][3][4][5].\n\nNote:\nThis entry is not a target in the strict drug discovery or pharmacology sense; rather, it is a pathway encompassing multiple true molecular targets (enzymes such as CYP17A1, HSD17B3, etc.)[2]. For target-level information, refer to specific enzymes or proteins within the pathway.
Inhibition of key enzymatic steps (e.g., CYP17A1, 5α-reductase) to reduce endogenous testosterone production; androgen supplementation increases pathway output[5][1].
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