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      Bile salt export pump (BSEP/ABCB11): trafficking and sorting disturbances.

      1 ,
      Current molecular pharmacology

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          Abstract

          Bile salt export pump (BSEP/ABCB11), a member of the family of ATP-binding cassette transporters, is localized on the canalicular membrane of hepatocytes and mediates the efficient biliary excretion of bile acid. The secretion of bile acid into bile by BSEP provides the primary osmotic driving force for bile flow generation. Intrahepatic cholestasis resulting from dysfunction of BSEP can be caused by a mutation in the gene encoding this protein or by acquired factors, such as the side effects of xenobiotics and drugs. In some pathophysiological states, inhibition of BSEP function is associated with its reduced expression on the canalicular membrane caused by impaired trafficking and sorting of BSEP. This fact has generated interest in better understanding the trafficking and sorting mechanism of BSEP. This review describes the molecular characteristics and physiological roles of BSEP, the trafficking and sorting machinery of BSEP, and the mechanisms responsible for disturbance of BSEP, which causes intrahepatic cholestasis.

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          Author and article information

          Journal
          Curr Mol Pharmacol
          Current molecular pharmacology
          1874-4702
          1874-4672
          Jul 2013
          : 6
          : 2
          Affiliations
          [1 ] Laboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113-0033, Japan. hayapi@mol.f.u-tokyo.ac.jp
          Article
          CMP-EPUB-54429
          23876151
          f935df35-a1e0-41ae-aa61-df0dcf877d28
          History

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