Hepatic uptake and biliary excretion of organic anions (eg, bile acids and bilirubin) is
mediated by hepatobiliary transport systems. Defects in transporter expression and function …

Because ATP-binding cassette (ABC) transporters are important for normal bile secretion,
hereditary and acquired ABC transporter defects play a central role in the pathogenesis of …

The Nrf2 (nuclear factor-erythroid 2 p45-related factor 2) transcription factor regulates gene
expression of the GCLC (glutamate–cysteine ligase catalytic subunit), which is a key …

Cholestasis results in intrahepatic accumulation of cytotoxic bile acids, which cause liver
damage ultimately leading to biliary fibrosis and cirrhosis. Cholestatic liver injury is …

Peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that controls
expression of genes involved in lipid metabolism and is activated by fatty acids and …

Nuclear receptors (NRs) play a key role in the transcriptional control of critical steps of
hepatobiliary transport and phase I/II metabolism of endo-and xenobiotics such as bile acids …

Multidrug resistance transporter 3/ATP‐binding cassette protein subfamily B4
(MDR3/ABCB4) is a critical determinant of biliary phosphatidylcholine (PC) secretion …

Human membrane drug transporters are recognized as major actors of pharmacokinetics;
they also handle endogenous compounds, including hormones and metabolites. Chemical …

Nuclear receptors are key regulators of various processes including reproduction,
development, and metabolism of xeno-and endobiotics such as bile acids and drugs …

Major determinants of the bioavailability of drugs are the degree of intestinal absorption and
the hepatic first-pass effect. Drugs need to overcome several membrane barriers before …