Function and regulation of ATP-binding cassette transport proteins involved in hepatobiliary transport

Eur J Pharm Sci. 2001 Feb;12(4):525-43. doi: 10.1016/s0928-0987(01)00101-4.


Hepatobiliary transport of endogenous and exogenous compounds is mediated by the coordinated action of multiple transport systems present at the sinusoidal (basolateral) and canalicular (apical) membrane domains of hepatocytes. During the last few years many of these transporters have been cloned and functionally characterized. In addition, the molecular bases of several forms of cholestatic liver disease have been defined. Combined, this has greatly expanded our understanding of the normal physiology of bile formation, the pathophysiology of intrahepatic cholestasis, as well as of drug elimination and disposition processes. In this review recent advances, with respect to function and regulation of ATP binding cassette transport proteins expressed in liver, are summarized and discussed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review
  • Corrected and Republished Article

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / drug effects
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
  • ATP-Binding Cassette Transporters / drug effects
  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology
  • Cations / pharmacology
  • DNA-Binding Proteins / drug effects
  • DNA-Binding Proteins / metabolism*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology
  • Gene Expression / drug effects
  • Gene Expression / physiology
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism*
  • Humans
  • Multidrug Resistance-Associated Proteins*
  • MutS Homolog 3 Protein
  • Steroids / metabolism
  • Steroids / pharmacology


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP-Binding Cassette Transporters
  • Anti-Bacterial Agents
  • Cations
  • DNA-Binding Proteins
  • Enzyme Inhibitors
  • MSH3 protein, human
  • Multidrug Resistance-Associated Proteins
  • MutS Homolog 3 Protein
  • Steroids
  • multidrug resistance-associated protein 1