Target intelligence / Profile preview

Hepatocyte bile acid transporters

Molecular classification
Transporter, Membrane protein, Solute carrier (for NTCP, OATP), ATP-binding cassette transporter (for BSEP, MRP2)
01

Overview

Hepatocyte bile acid transporters are a family of membrane proteins essential for the uptake, intracellular shifting, and canalicular export of bile acids in the liver. The key uptake transporter is the Na+ taurocholate co-transporting polypeptide (NTCP), which imports bile acids from portal blood. Bile acids are then shuttled within the hepatocyte and actively secreted into bile by the bile salt export pump (BSEP) and multidrug resistance protein MRP2, among others. These transporters regulate bile acid, cholesterol, and phospholipid homeostasis, bile formation, and are centrally involved in the enterohepatic circulation. Dysfunction or inhibition of these proteins leads to impaired bile acid and cholesterol clearance, cholestatic liver disease, and other metabolic disturbances.

Other names
Bile acid transporters in hepatocytesHepatic bile acid transport proteinsNTCPBSEPMRP2
02

Mechanism of action

Inhibition or modulation of transporter activity to alter bile acid flow (e.g., NTCP inhibition prevents hepatitis B/D virus entry, BSEP inhibition causes cholestasis) Induced expression or activation to promote bile acid clearance

03

Biological functions

Bile acid uptake (NTCP, OATPs)Bile acid efflux into bile canaliculus (BSEP, MRP2)Maintenance of lipid and bile acid homeostasisCholesterol eliminationRegulation of bile flow
04

Disease associations

Cholestatic liver disease (e.g., mutations or dysfunction of BSEP)Liver injury from drug-induced cholestasisHyperbilirubinemia (MRP2 dysfunction)Bile acid malabsorptionOther metabolic and hepatic disorders
05

Safety considerations

Drug-induced liver injury (cholestasis or hepatitis with inhibition)Impaired fat-soluble vitamin absorption (A, D, E, K) in transporter dysfunctionPortal hypertension and liver failure in genetic defects
06

Interacting drugs

Bile acid sequestrants (indirectly)

4 more in the full profile.

07

Biomarkers

Serum/plasma bile acid levels (measure hepatobiliary function)Genetic variants (e.g., ABCB11 mutations in inherited cholestasis)Liver function tests (ALT, AST, bilirubin)

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