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Cuperus, FJ; Claudel, T; Gautherot, J; Halilbasic, E; Trauner, M.
The role of canalicular ABC transporters in cholestasis.
Drug Metab Dispos. 2014; 42(4):546-560 Doi: 10.1124/dmd.113.056358 [OPEN ACCESS]
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Führende Autor*innen der Med Uni Graz
Trauner Michael
Co-Autor*innen der Med Uni Graz
Claudel Thierry
Halilbasic Emina
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Abstract:
Cholestasis, a hallmark feature of hepatobiliary disease, is characterized by the retention of biliary constituents. Some of these constituents, such as bile acids, inflict damage to hepatocytes and bile duct cells. This damage may lead to inflammation, fibrosis, cirrhosis, and eventually carcinogenesis, sequelae that aggravate the underlying disease and deteriorate clinical outcome. Canalicular ATP-binding cassette (ABC) transporters, which mediate the excretion of individual bile constituents, play a key role in bile formation and cholestasis. The study of these transporters and their regulatory nuclear receptors has revolutionized our understanding of cholestatic disease. This knowledge has served as a template to develop novel treatment strategies, some of which are currently already undergoing phase III clinical trials. In this review we aim to provide an overview of the structure, function, and regulation of canalicular ABC transporters. In addition, we will focus on the role of these transporters in the pathogenesis and treatment of cholestatic bile duct and liver diseases.
Find related publications in this database (using NLM MeSH Indexing)
ATP-Binding Cassette Transporters - chemistry ATP-Binding Cassette Transporters - metabolism
Animals -
Bile - metabolism
Bile Canaliculi - metabolism
Cholestasis - etiology Cholestasis - metabolism
Humans -
Models, Biological -
Pharmaceutical Preparations - metabolism
Receptors, Cytoplasmic and Nuclear - metabolism

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