Target intelligence / Profile preview

Cholesterol 7 alpha-hydroxylase

Molecular classification
Enzyme, Cytochrome P450
01

Overview

Cholesterol 7 alpha-hydroxylase (CYP7A1) is a cytochrome P450 heme enzyme that catalyzes the first and rate-limiting step in the classic pathway of bile acid synthesis from cholesterol. It is essential for cholesterol catabolism, bile acid production, and overall cholesterol homeostasis. Mutations or dysregulation of CYP7A1 are associated with hyperlipidemia, gallstone disease, and resistance to statin therapy. It's also a potential therapeutic target for various metabolic and liver diseases.

02

Mechanism of action

Inhibition of CYP7A1 leads to reduced bile acid synthesis and increased cholesterol levels. Activation leads to increased bile acid synthesis.

03

Biological functions

Cholesterol catabolismBile acid synthesisRegulation of cholesterol homeostasis
04

Disease associations

HyperlipidemiaGallstone diseaseCardiovascular diseaseMetabolic diseaseNAFLD/NASHDiabetesObesityCirrhosisHepatocellular carcinoma
05

Safety considerations

Drug-drug interactions due to CYP450 involvementPotential for liver toxicityGallstone formation
06

Interacting drugs

Statins

2 more in the full profile.

07

Biomarkers

7α-hydroxycholesterol levelsBile acid levels

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