Target intelligence / Profile preview

Phosphatidylcholine translocator ABCB4 (ABCB4)

Target
ABCB4
Molecular classification
Transporter, ATP-binding cassette (ABC) transporter, Floppase
01

Overview

Phosphatidylcholine translocator ABCB4 is a member of the ATP-binding cassette (ABC) transporter family, specifically mediating the ATP-dependent translocation ("flop") of phosphatidylcholine from the inner to the outer leaflet of the canalicular membrane in hepatocytes, thereby facilitating the secretion of phosphatidylcholine into bile. This activity is essential for normal bile formation and protects biliary epithelium from detergent effects of bile salts. Structural studies reveal conformational states where lipid binding, recruitment, and extrusion are coupled to ATP binding and hydrolysis. Mutations in ABCB4 cause inherited cholestatic disorders, and its function can be inhibited by drugs such as posaconazole, leading to adverse hepatic effects[3][7]. ABCB4 activity is crucial for lipid homeostasis and liver health.

Other names
ATP-binding cassette sub-family B member 4MDR3Multidrug resistance protein 3
02

Mechanism of action

Inhibition of phosphatidylcholine translocation (e.g., by binding and blocking lipid recruitment or extrusion)[3]

03

Biological functions

Phosphatidylcholine translocation ("floppase" activity) from inner to outer membrane leafletBile formationLipid homeostasis
04

Disease associations

CholestasisDrug-induced liver injuryOther liver and biliary diseases (e.g., progressive familial intrahepatic cholestasis type 3)
05

Safety considerations

Risk of cholestasis or drug-induced liver injury from inhibition or malfunction[3]
06

Interacting drugs

Posaconazole (azole class drug, inhibitor)[3]
07

Biomarkers

ABCB4 gene mutations for cholestasis diagnosis

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