Molecular Classification
Enzyme, Cytochrome P450 oxidoreductase
Other Names
Cholesterol 7-alpha hydroxylase, Cytochrome P450 7A1, CYP7A, 7alpha-hydroxylase
Disease Roles
HypercholesterolemiaGallstone diseaseStatin-resistant dyslipidemia

Cholesterol 7alpha-hydroxylase Overview

Cholesterol 7alpha-hydroxylase (CYP7A1) is a cytochrome P450 enzyme that catalyzes the rate-limiting step in bile acid synthesis. It is essential for cholesterol homeostasis and is a potential therapeutic target for hyperlipidemia, gallstone disease, and metabolic disorders. CYP7A1 expression is regulated by LXR and FXR, and genetic deficiencies can lead to hypercholesterolemia and increased risk of gallstones.

Mechanism of Action

CYP7A1 catalyzes the first and rate-limiting step in the classic pathway of bile acid synthesis from cholesterol in the liver. It converts cholesterol to 7α-hydroxycholesterol, initiating its catabolism and facilitating cholesterol excretion via bile acids.

Biological Functions

Bile acid synthesis
Cholesterol homeostasis
Regulation of glucose metabolism
Regulation of energy expenditure

Disease Associations

Hypercholesterolemia
Gallstone disease
Statin-resistant dyslipidemia
Non-alcoholic fatty liver disease (NAFLD)
Non-alcoholic steatohepatitis (NASH)
Obesity
Diabetes mellitus type 2

Safety Considerations

  • Potential for drug-drug interactions due to cytochrome P450 activity
  • Overexpression may lead to altered bile acid composition with unknown long-term consequences

Interacting Drugs

Bile acids
Statins

Associated Biomarkers

Biomarker
7α-hydroxycholesterol levels
Bile acid levels
Cholesterol levels
CYP7A1 expression levels