Target intelligence / Profile preview

Bile salt homeostasis pathway enzymes

Molecular classification
Enzyme, Transporter, Receptor
01

Overview

Bile salt homeostasis pathway enzymes refers to a set of enzymes and regulatory proteins responsible for the synthesis, modification, and recycling of bile acids and bile salts predominantly in the liver, and their subsequent modification in the intestine. The key enzymes include cholesterol 7 alpha-hydroxylase (CYP7A1, rate-limiting), sterol 27-hydroxylase (CYP27A1, alternative pathway), and additional cytochrome P450 enzymes, along with conjugating enzymes for glycine/taurine addition. Regulation is tightly controlled via feedback from nuclear and membrane receptors (FXR, TGR5), and further modification occurs via gut microbial bile salt hydrolases. Disruption of this pathway is implicated in many hepatic, metabolic, and inflammatory diseases. This name does not correspond to a single molecular entity, but to a collection of well-defined molecule classes in a pathway essential for cholesterol metabolism and enterohepatic nutrient homeostasis.

Other names
Bile acid synthesis enzymesBile acid pathway enzymesBile acid homeostasis enzymes
02

Mechanism of action

FXR agonism (negative feedback inhibition of bile acid synthesis); Bile acid sequestration (removal from enterohepatic circulation); Enzyme inhibition (e.g., CYP7A1 inhibition); Bile acid conversion (microbial bile salt hydrolases; BSH activity in probiotics)

03

Biological functions

Cholesterol catabolismBile acid synthesisLipid digestion and absorptionMetabolic regulationFeedback regulation of bile acid synthesisEndocrine signaling
04

Disease associations

Cholestatic liver diseasesGallstone diseaseMetabolic syndromeNonalcoholic fatty liver diseaseInflammatory and neoplastic diseases (when BA signaling is disrupted)
05

Safety considerations

Disruption may cause cholestasis, liver toxicity, hyperlipidemia, pruritusBile acid accumulation can trigger hepatotoxicityExcess sequestration may affect absorption of fat-soluble vitamins
06

Interacting drugs

Obeticholic acid

3 more in the full profile.

07

Biomarkers

Serum bile acid levelsLiver function tests (ALT, AST, ALP, bilirubin)Expression/activity of CYP7A1, CYP8B1, CYP27A1FGF19 (feedback regulator from intestine to liver)

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