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Target intelligence / Profile preview
Cholesterol 7alpha-hydroxylase (CYP7A1)
- Target
- CYP7A1
- Molecular classification
- Enzyme, Cytochrome P450 oxidoreductase
01
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.
- Other names
- Cholesterol 7-alpha hydroxylaseCytochrome P450 7A1CYP7A7alpha-hydroxylase
02
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.
03
Biological functions
Bile acid synthesisCholesterol homeostasisRegulation of glucose metabolismRegulation of energy expenditure
04
Disease associations
HypercholesterolemiaGallstone diseaseStatin-resistant dyslipidemiaNon-alcoholic fatty liver disease (NAFLD)Non-alcoholic steatohepatitis (NASH)ObesityDiabetes mellitus type 2
05
Safety considerations
Potential for drug-drug interactions due to cytochrome P450 activityOverexpression may lead to altered bile acid composition with unknown long-term consequences
06
Interacting drugs
Bile acids
1 more in the full profile.
07
Biomarkers
7α-hydroxycholesterol levelsBile acid levelsCholesterol levelsCYP7A1 expression levels
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