Target intelligence / Profile preview

Cytochrome P450 enzyme involved in steroidogenesis (CYP (with specific isoforms such as CYP11A1, CYP17A1, CYP19A1 commonly referenced))

Target
CYP (with specific isoforms such as CYP11A1, CYP17A1, CYP19A1 commonly referenced)
Molecular classification
Enzyme, Oxidoreductase, Heme-containing monooxygenase
01

Overview

Cytochrome P450 enzymes involved in steroidogenesis are a subset of the large cytochrome P450 superfamily responsible for catalyzing key oxidative reactions required for converting cholesterol into biologically active steroid hormones. These heme-containing monooxygenases are primarily expressed in endocrine tissues like the adrenal glands and gonads. They mediate multiple steps including side-chain cleavage and hydroxylations essential for producing glucocorticoids, mineralocorticoids, estrogens, and androgens. Dysregulation or genetic defects affecting these enzymes can result in various endocrine diseases or contribute to hormone-dependent cancers. Pharmacological inhibition is a validated therapeutic strategy for conditions where suppression of endogenous steroids is beneficial.

Other names
Cytochrome P450 steroidogenic enzymeSteroidogenic cytochrome P450Steroidogenic CYPSteroid hormone-synthesizing cytochrome P450
02

Mechanism of action

Drugs targeting these enzymes typically act by inhibiting the enzymatic conversion steps in the biosynthesis of steroid hormones. For example, - Inhibition of androgen or estrogen synthesis by blocking key hydroxylation/lyase/aromatization steps catalyzed by specific CYPs. - Competitive inhibition at the heme active site.

03

Biological functions

Steroidogenesis (biosynthesis of steroid hormones from cholesterol)Metabolism of endogenous and exogenous compoundsHydroxylation and epoxidation reactions
04

Disease associations

Cancer (e.g., hormone-dependent cancers such as breast and prostate cancer)Endocrine disorders (e.g., congenital adrenal hyperplasia)Reproductive disordersMetabolic syndrome
05

Safety considerations

Disruption of normal hormonal balance leading to side effects such as adrenal insufficiency, sexual dysfunction, metabolic disturbancesPotential drug-drug interactions due to broad substrate specificity
06

Interacting drugs

Ketoconazole (broad-spectrum inhibitor)

2 more in the full profile.

07

Biomarkers

Levels of circulating steroids such as cortisol, testosterone, estradiolExpression levels or mutations in specific CYP genesResponse to drug therapy targeting these pathways

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