Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
Ryan E. Morgan,Michael Trauner,Carlo van Staden,Paul H. Lee,Bharath Ramachandran,Michael Eschenberg,Cynthia A. Afshari,Charles W. Qualls,Ruth Lightfoot-Dunn,Hisham K. Hamadeh +9 more
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TL;DR: In this study, membrane vesicles harvested from BSEP-transfected insect cells were used to assess the activity of more than 200 benchmark compounds to thoroughly investigate the relationship between interference with BSEp function and liver injury, and suggest a relatively strong association between the pharmacological interference with bile salt export pump function and human hepatotoxicity.
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About: This article is published in Toxicological Sciences. The article was published on 01 Dec 2010. and is currently open access. The article focuses on the topics: Bile Salt Export Pump & Progressive familial intrahepatic cholestasis.
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Citations
Recent advances in 2D and 3D in vitro systems using primary hepatocytes, alternative hepatocyte sources and non-parenchymal liver cells and their use in investigating mechanisms of hepatotoxicity, cell signaling and ADME.
Patricio Godoy,Nicola J. Hewitt,Ute Albrecht,Melvin E. Andersen,Nariman Ansari,Sudin Bhattacharya,Johannes G. Bode,Jennifer Bolleyn,Christoph Borner,J Böttger,Albert Braeuning,Robert A. Budinsky,Britta Burkhardt,Neil R. Cameron,Giovanni Camussi,Chong Su Cho,Yun Jaie Choi,J. Craig Rowlands,Uta Dahmen,Georg Damm,Olaf Dirsch,María Teresa Donato,Jian Dong,Steven Dooley,Dirk Drasdo,Dirk Drasdo,Dirk Drasdo,Rowena Eakins,Karine Sá Ferreira,Valentina Fonsato,Joanna Fraczek,Rolf Gebhardt,Andrew Gibson,Matthias Glanemann,Christopher E. Goldring,María José Gómez-Lechón,Geny M. M. Groothuis,Lena Gustavsson,Christelle Guyot,David Hallifax,Seddik Hammad,Adam S. Hayward,Dieter Häussinger,Claus Hellerbrand,Philip Hewitt,Stefan Hoehme,Hermann-Georg Holzhütter,J. Brian Houston,Jens Hrach,Kiyomi Ito,Hartmut Jaeschke,Verena Keitel,Jens M. Kelm,B. Kevin Park,Claus Kordes,Gerd A. Kullak-Ublick,Edward L. LeCluyse,Peng Lu,Jennifer Luebke-Wheeler,Anna Lutz,Daniel J. Maltman,Madlen Matz-Soja,Patrick D. McMullen,Irmgard Merfort,Simon Messner,Christoph Meyer,Jessica Mwinyi,Dean J. Naisbitt,Andreas K. Nussler,Peter Olinga,Francesco Pampaloni,Jingbo Pi,Linda J. Pluta,Stefan Przyborski,Anup Ramachandran,Vera Rogiers,Cliff Rowe,Celine Schelcher,Kathrin Schmich,Michael Schwarz,Bijay Singh,Ernst H. K. Stelzer,Bruno Stieger,Regina Stöber,Yuichi Sugiyama,Ciro Tetta,Wolfgang E. Thasler,Tamara Vanhaecke,Mathieu Vinken,Thomas S. Weiss,Agata Widera,Courtney G. Woods,Jinghai James Xu,Kathy Yarborough,Jan G. Hengstler +94 more
TL;DR: This review encompasses the most important advances in liver functions and hepatotoxicity and analyzes which mechanisms can be studied in vitro and how closely hepatoma, stem cell and iPS cell–derived hepatocyte-like-cells resemble real hepatocytes.
EASL Clinical Practice Guidelines: Drug-induced liver injury
Raúl J. Andrade,Guruprasad P. Aithal,Einar Björnsson,Neil Kaplowitz,Gerd A. Kullak-Ublick,Dominique Larrey,Tom H. Karlsen +6 more
TL;DR: These Clinical Practice Guidelines summarize the available evidence on risk factors, diagnosis, management and risk minimization strategies for drug-induced liver jury.
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Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States.
Antonia F. Stepan,Daniel P. Walker,Daniel P. Walker,Jonathan Bauman,Jonathan Bauman,David A. Price,David A. Price,Thomas A. Baillie,Thomas A. Baillie,Amit S. Kalgutkar,Amit S. Kalgutkar,Michael D. Aleo,Michael D. Aleo +12 more
TL;DR: While RM elimination may be a useful and pragmatic starting point in mitigating idiosyncratic toxicity risks, the analysis suggests a need for a more integrated screening paradigm for chemical hazard identification in drug discovery.
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Drug-induced liver injury
Raúl J. Andrade,Naga Chalasani,Einar Bjornsson,Ayako Suzuki,Ayako Suzuki,Gerd A. Kullak-Ublick,Gerd A. Kullak-Ublick,Paul B. Watkins,Harshad Devarbhavi,Michael Merz,Michael Merz,M. Isabel Lucena,Neil Kaplowitz,Guruprasad P. Aithal +13 more
- 22 Aug 2019
TL;DR: Drug-induced liver injury (DILI) is an adverse reaction to drugs or other xenobiotics that occurs either as a predictable event when an individual is exposed to toxic doses of some compounds or as an unpredictable event with many drugs in common use as discussed by the authors.
Drug-induced liver injury: recent advances in diagnosis and risk assessment
Gerd A. Kullak-Ublick,Raúl J. Andrade,Michael Merz,Peter End,Andreas Benesic,Alexander L. Gerbes,Guruprasad P. Aithal +6 more
TL;DR: The provision of more advanced scientific and regulatory guidance for liver safety assessment will depend on validating the new diagnostic markers in the ongoing DILI registries, biobanks and public–private partnerships.
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References
Bile acids: regulation of synthesis.
TL;DR: Bile acids are able to induce FGF 19 in human hepatocytes, and the FGF19 autocrine pathway may exist in the human livers, andThe mechanism by which FXR/FGF19/FGFR4 signaling inhibits CYP7A1 remains unknown.
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Bile Salt Transporters: Molecular Characterization, Function, and Regulation
Michael Trauner,James L. Boyer +1 more
TL;DR: This review is a comprehensive summary of current knowledge of the molecular characterization, function, and regulation of bile salt transporters in normal physiology and in cholestatic liver disease and liver regeneration.
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A gene encoding a liver-specific ABC transporter is mutated in progressive familial intrahepatic cholestasis
S S Strautnieks,Laura N. Bull,A.S. Knisely,S A Kocoshis,Niklas Dahl,H Arnell,Etienne Sokal,Karin Dahan,Sarah J. Childs,Ling,M. S. Tanner,Amir F. Kagalwalla,Antal Nemeth,Joanna Pawłowska,Amie Baker,Giorgina Mieli-Vergani,Nelson B. Freimer,R M Gardiner,Richard J. Thompson +18 more
TL;DR: Data provide evidence that SPGP is the human bile salt export pump (BSEP), and the product of the orthologous rat gene has been shown to be an effective bile acid transporter in vitro.
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The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver.
Thomas Gerloff,Bruno Stieger,Bruno Hagenbuch,Jerzy Madon,Lukas Landmann,Jürgen Roth,Alan F. Hofmann,Peter J. Meier +7 more
TL;DR: Results indicate that the sister of P-glycoprotein is the major canalicular bile salt export pump of mammalian liver.
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