2012
DOI: 10.1016/j.tiv.2011.11.002
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BSEP inhibition – In vitro screens to assess cholestatic potential of drugs

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Cited by 48 publications
(42 citation statements)
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“…While this protein is also found in many cell types, porphyrin release is the most common function found in hepatocytes [92, 93]. BSEP is a protein localized to hepatocytes that functions in the transport of bile salts into the bile canaliculi [94]. As a result, BSEP is an important regulatory in bile flow.…”
Section: Mechanisms For Idiosyncratic Hepatotoxicitymentioning
confidence: 99%
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“…While this protein is also found in many cell types, porphyrin release is the most common function found in hepatocytes [92, 93]. BSEP is a protein localized to hepatocytes that functions in the transport of bile salts into the bile canaliculi [94]. As a result, BSEP is an important regulatory in bile flow.…”
Section: Mechanisms For Idiosyncratic Hepatotoxicitymentioning
confidence: 99%
“…Mutations in ABC transporters mean that metabolized drugs cannot leave the hepatocytes, leading to impaired canalicular bile flow. This generally manifests in the form of cholestasis and fatty liver disease [94, 95]. MDR1, BSEP, BCRP, and MRP2 all have polymorphisms that have been associated with idiosyncratic ADRs.…”
Section: Mechanisms For Idiosyncratic Hepatotoxicitymentioning
confidence: 99%
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“…Kis et al . () have summarized appropriate in vitro methods that could predict BSEP–drug candidate interactions in humans.…”
Section: Developments In Safety Testing Paradigmmentioning
confidence: 99%
“…7 Intrahepatic accumulation of drug or cytotoxic bile acids caused by drug interference of either bile formation or bile flow is one of the major mechanisms contributing to DILI. 8 Both hepatic sinusoidal uptake transporters and canalicular efflux transporters have essential roles in mediating the translocation of drug and bile salts from the blood to the hepatocytes and from the hepatocytes to the canalicular space, respectively; the latter is considered to be a rate-controlling step of vectorial transport. 9 Drugs can potentially cause intrahepatic cholestasis by modulating bile formation at many levels.…”
Section: Introductionmentioning
confidence: 99%