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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.
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
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