Recent insights into the function and regulation of the bile salt export pump (ABCB11)
نویسندگان
چکیده
منابع مشابه
Recent advances in the exploration of the bile salt export pump (BSEP/ABCB11) function.
INTRODUCTION The bile salt export pump (BSEP/ABCB11), residing in the apical membrane of hepatocyte, mediates the secretion of bile salts into the bile. A range of human diseases is associated with the malfunction of BSEP, including fatal hereditary liver disorders and mild cholestatic conditions. Manifestation of these diseases primarily depends on the mutation type; however, other factors suc...
متن کاملAnalysis of the Bile Salt Export Pump (ABCB11) Interactome Employing Complementary Approaches
The bile salt export pump (BSEP, ABCB11) plays an essential role in the formation of bile. In hepatocytes, BSEP is localized within the apical (canalicular) membrane and a deficiency of canalicular BSEP function is associated with severe forms of cholestasis. Regulation of correct trafficking to the canalicular membrane and of activity is essential to ensure BSEP functionality and thus normal b...
متن کاملPosttranslational regulation of the bile salt export pump
Bile plays an essential role in the nutrient uptake of the human body. It consists mostly of amphipathic bile salts, phospholipids and cholesterol in mixed micelles. The bile solubilizes lipophilic nutrients, such as lipids and fat-soluble vitamins, and facilitates their uptake. The formation of bile depends on the activity of various ATP-binding cassette (ABC) transporters localized in the api...
متن کاملActivity of the bile salt export pump (ABCB11) is critically dependent on canalicular membrane cholesterol content.
Mutations in ATP8B1 cause severe inherited liver disease. The disease is characterized by impaired biliary bile salt excretion (cholestasis), but the mechanism whereby impaired ATP8B1 function results in cholestasis is poorly understood. ATP8B1 is a type 4 P-type ATPase and is a flippase for phosphatidylserine. Atp8b1-deficient mice display a dramatic increase in the biliary extraction of chole...
متن کاملEarly Identification of Clinically Relevant Drug Interactions With the Human Bile Salt Export Pump (BSEP/ABCB11)
A comprehensive analysis was performed to investigate how inhibition of the human bile salt export pump (BSEP/ABCB11) relates to clinically observed drug-induced liver injury (DILI). Inhibition of taurocholate (TA) transport was investigated in BSEP membrane vesicles for a data set of 250 compounds, and 86 BSEP inhibitors were identified. Structure-activity modeling identified BSEP inhibition t...
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ژورنال
عنوان ژورنال: Current Opinion in Lipidology
سال: 2009
ISSN: 0957-9672
DOI: 10.1097/mol.0b013e32832b677c