3β-HSD3 Inhibitors

The class of chemicals known as HSD3 inhibitors primarily targets the enzymatic activity of 3β-hydroxysteroid dehydrogenases. These inhibitors play a role in disrupting the normal biosynthesis of steroid hormones by either directly blocking the active site of the enzyme or by altering the availability of substrates and cofactors required for the enzymatic reactions that 3β-HSD catalyzes.

Trilostane and Epostane, for instance, directly inhibit the conversion of pregnenolone to progesterone, a critical step in steroidogenesis mediated by 3β-HSD. Cyanoketone functions as an irreversible inhibitor, thus causing a long-term decrease in steroid hormone production. Other compounds such as Metyrapone and Ketoconazole affect the activity of 3β-HSD by inhibiting other enzymes in the steroid biosynthesis pathway, which can lead to a decrease in the overall production of steroids. Abiraterone, by inhibiting CYP17A1, reduces the levels of steroid precursors necessary for 3β-HSD activity.