The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds

Tim Brecklinghaus; Wiebke Albrecht; Franziska Kappenberg; Julia Duda; Nachiket Vartak; Karolina Edlund; Rosemarie Marchan; Ahmed Ghallab; Cristina Cadenas; Georgia Günther; Marcel Leist; Mian Zhang; Iain Gardner; Jörg Reinders; Frans GM Russel; Alison J. Foster; Dominic P. Williams; Amruta Damle-Vartak; Melanie Grandits; Gerhard Ecker; Naim Kittana; Jörg Rahnenführer; Jan G. Hengstler

doi:10.1016/j.cbi.2021.109728

The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds

Tim Brecklinghaus
, Wiebke Albrecht
, Franziska Kappenberg
, Julia Duda
, Nachiket Vartak
, Karolina Edlund
, Rosemarie Marchan
, Ahmed Ghallab
, Cristina Cadenas
, Georgia Günther
, Marcel Leist
, Mian Zhang
, Iain Gardner
, Jörg Reinders
, Frans GM Russel
, Alison J. Foster
, Dominic P. Williams
, Amruta Damle-Vartak
, Melanie Grandits
, Gerhard Ecker

Naim Kittana, Jörg Rahnenführer, Jan G. Hengstler

Department of Pharmaceutical Sciences

Publications: Contribution to journal › Article › Peer Reviewed

Original language	English
Article number	109728
Number of pages	16
Journal	Chemico-Biological Interactions
Volume	351
DOIs	https://doi.org/10.1016/j.cbi.2021.109728
Publication status	Published - 5 Jan 2022

Funding

This work has been supported in part by the Research Training Group “Biostatistical Methods for High-Dimensional Data in Toxicology” ( RTG 2624 , Project P1 and P2) funded by the Deutsche Forschungsgemeinschaft (DFG, German Research Foundation - Project Number 427806116 ). Furthermore, this work has received funding from the European Union's Horizon 2020 research and innovation programme under grant agreement no. 681002 (EU-ToxRisk) and LivSysTransfer ( BMBF, 031L0119 ).

Austrian Fields of Science 2012

301207 Pharmaceutical chemistry

Keywords

Cholestasis
DILI
Transport
IN-VITRO
TRANSPORTER
GLUTATHIONE
LIVER
Cell Culture Techniques/methods
Humans
Cells, Cultured
Cytotoxins/toxicity
Hepatocytes/drug effects
Toxicity Tests/methods
Fluoresceins/metabolism
Multidrug Resistance-Associated Protein 2/antagonists & inhibitors
ATP Binding Cassette Transporter, Subfamily B, Member 11/antagonists & inhibitors
Mitochondria/drug effects
Chemical and Drug Induced Liver Injury

Access to Document

10.1016/j.cbi.2021.109728

Cite this

Brecklinghaus, T., Albrecht, W., Kappenberg, F., Duda, J., Vartak, N., Edlund, K., Marchan, R., Ghallab, A., Cadenas, C., Günther, G., Leist, M., Zhang, M., Gardner, I., Reinders, J., Russel, F. GM., Foster, A. J., Williams, D. P., Damle-Vartak, A., Grandits, M., ... Hengstler, J. G. (2022). The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds. Chemico-Biological Interactions, 351, Article 109728. https://doi.org/10.1016/j.cbi.2021.109728

@article{1705e07139144f72a799290ff2dfc424,

title = "The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds",

keywords = "Cholestasis, DILI, Transport, IN-VITRO, TRANSPORTER, GLUTATHIONE, LIVER, Cell Culture Techniques/methods, Humans, Cells, Cultured, Cytotoxins/toxicity, Hepatocytes/drug effects, Toxicity Tests/methods, Fluoresceins/metabolism, Multidrug Resistance-Associated Protein 2/antagonists \& inhibitors, ATP Binding Cassette Transporter, Subfamily B, Member 11/antagonists \& inhibitors, Mitochondria/drug effects, Chemical and Drug Induced Liver Injury",

author = "Tim Brecklinghaus and Wiebke Albrecht and Franziska Kappenberg and Julia Duda and Nachiket Vartak and Karolina Edlund and Rosemarie Marchan and Ahmed Ghallab and Cristina Cadenas and Georgia G{\"u}nther and Marcel Leist and Mian Zhang and Iain Gardner and J{\"o}rg Reinders and Russel, \{Frans GM\} and Foster, \{Alison J.\} and Williams, \{Dominic P.\} and Amruta Damle-Vartak and Melanie Grandits and Gerhard Ecker and Naim Kittana and J{\"o}rg Rahnenf{\"u}hrer and Hengstler, \{Jan G.\}",

note = "Funding Information: This work has been supported in part by the Research Training Group “Biostatistical Methods for High-Dimensional Data in Toxicology” ( RTG 2624 , Project P1 and P2) funded by the Deutsche Forschungsgemeinschaft (DFG, German Research Foundation - Project Number 427806116 ). Furthermore, this work has received funding from the European Union's Horizon 2020 research and innovation programme under grant agreement no. 681002 (EU-ToxRisk) and LivSysTransfer ( BMBF, 031L0119 ). Publisher Copyright: {\textcopyright} 2021 The Authors Copyright: Copyright 2021 Elsevier B.V., All rights reserved.",

year = "2022",

month = jan,

day = "5",

doi = "10.1016/j.cbi.2021.109728",

language = "English",

volume = "351",

journal = "Chemico-Biological Interactions",

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Brecklinghaus, T, Albrecht, W, Kappenberg, F, Duda, J, Vartak, N, Edlund, K, Marchan, R, Ghallab, A, Cadenas, C, Günther, G, Leist, M, Zhang, M, Gardner, I, Reinders, J, Russel, FGM, Foster, AJ, Williams, DP, Damle-Vartak, A, Grandits, M , Ecker, G, Kittana, N, Rahnenführer, J & Hengstler, JG 2022, 'The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds', Chemico-Biological Interactions, vol. 351, 109728. https://doi.org/10.1016/j.cbi.2021.109728

TY - JOUR

T1 - The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds

AU - Brecklinghaus, Tim

AU - Albrecht, Wiebke

AU - Kappenberg, Franziska

AU - Duda, Julia

AU - Vartak, Nachiket

AU - Edlund, Karolina

AU - Marchan, Rosemarie

AU - Ghallab, Ahmed

AU - Cadenas, Cristina

AU - Günther, Georgia

AU - Leist, Marcel

AU - Zhang, Mian

AU - Gardner, Iain

AU - Reinders, Jörg

AU - Russel, Frans GM

AU - Foster, Alison J.

AU - Williams, Dominic P.

AU - Damle-Vartak, Amruta

AU - Grandits, Melanie

AU - Ecker, Gerhard

AU - Kittana, Naim

AU - Rahnenführer, Jörg

AU - Hengstler, Jan G.

N1 - Funding Information: This work has been supported in part by the Research Training Group “Biostatistical Methods for High-Dimensional Data in Toxicology” ( RTG 2624 , Project P1 and P2) funded by the Deutsche Forschungsgemeinschaft (DFG, German Research Foundation - Project Number 427806116 ). Furthermore, this work has received funding from the European Union's Horizon 2020 research and innovation programme under grant agreement no. 681002 (EU-ToxRisk) and LivSysTransfer ( BMBF, 031L0119 ). Publisher Copyright: © 2021 The Authors Copyright: Copyright 2021 Elsevier B.V., All rights reserved.

PY - 2022/1/5

Y1 - 2022/1/5

KW - Cholestasis

KW - DILI

KW - Transport

KW - IN-VITRO

KW - TRANSPORTER

KW - GLUTATHIONE

KW - LIVER

KW - Cell Culture Techniques/methods

KW - Humans

KW - Cells, Cultured

KW - Cytotoxins/toxicity

KW - Hepatocytes/drug effects

KW - Toxicity Tests/methods

KW - Fluoresceins/metabolism

KW - Multidrug Resistance-Associated Protein 2/antagonists & inhibitors

KW - ATP Binding Cassette Transporter, Subfamily B, Member 11/antagonists & inhibitors

KW - Mitochondria/drug effects

KW - Chemical and Drug Induced Liver Injury

UR - https://www.scopus.com/pages/publications/85118490353

U2 - 10.1016/j.cbi.2021.109728

DO - 10.1016/j.cbi.2021.109728

M3 - Article

C2 - 34717914

AN - SCOPUS:85118490353

SN - 0009-2797

VL - 351

JO - Chemico-Biological Interactions

JF - Chemico-Biological Interactions

M1 - 109728

ER -

The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds

Funding

Austrian Fields of Science 2012

Keywords

Access to Document

Other files and links

Fingerprint

EU-ToxRisk: EU-ToxRisk

Cite this

The hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds

Funding

Austrian Fields of Science 2012

Keywords

Access to Document

Other files and links

Fingerprint

Projects

EU-ToxRisk: EU-ToxRisk

Cite this