Polymorphic variants in the human bile salt export pump (BSEP; ABCB11): functional characterization and interindividual variability
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چکیده
منابع مشابه
Early 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...
متن کاملRecent 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 کاملBile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.
Pravastatin is a well known 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor. Cumulative studies have shown that pravastatin is taken up into hepatocytes by the organic anion transporting polypeptide family transporters and excreted into the bile as an intact form by multidrug resistance-associated protein 2 (MRP2). It is generally accepted that the bile salt export pump (BSEP/ABCB11) mainly ...
متن کاملThe feline bile salt export pump: a structural and functional comparison with canine and human Bsep/BSEP
BACKGROUND The bile salt export pump (BSEP/ABCB11) is the primary transporter for the excretion of bile acids from hepatocytes into bile. In human, inhibition of BSEP by drugs has been related to drug-induced cholestasis and subsequent cytotoxic effects. The role of BSEP in canine and feline liver diseases has not been studied in detail, but the same mechanism of inhibition by drugs as in human...
متن کاملGenetic and Proteomic characterization of Bile Salt Export Pump (BSEP) in Snake Liver
Snake gallbladder, a traditional Chinese medicine, has been believed in various Asian countries to improve visual acuity and alleviate rheumatism. Bile acids, a major component of the gallbladder, are toxic to the liver and kidney in humans and animals due to its detergent effects, while also exhibiting therapeutic effects due to an increase in the gallbladder contractions of muscle strips in p...
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ژورنال
عنوان ژورنال: Pharmacogenetics and Genomics
سال: 2010
ISSN: 1744-6872
DOI: 10.1097/fpc.0b013e3283349eb0