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OtherArticle

Nelfinavir and its active metabolite M8 are partial agonists and competitive antagonists of the human pregnane X receptor

Oliver Burk, Thales Kronenberger, Oliver Keminer, Serene M.L. Lee, Tobias S. Schiergens, Matthias Schwab and Björn Windshügel
Molecular Pharmacology January 22, 2021, MOLPHARM-AR-2020-000116; DOI: https://doi.org/10.1124/molpharm.120.000116
Oliver Burk
1Cellular and Molecular Biology, Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Germany
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Thales Kronenberger
2Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Germany
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Oliver Keminer
2Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Germany
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Serene M.L. Lee
3Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital LMU Munich, Germany
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Tobias S. Schiergens
4Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital LMU Munich,, Germany
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Matthias Schwab
5Dr Margerte Fischer Bosch Institute of Clinical Pharmacology, Germany
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Björn Windshügel
6ScreeningPort, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Germany
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  • For correspondence: bjoern.windshuegel@ime.fraunhofer.de

Data Supplement

  • Supplemental Data -

    Supplemental Materials and Methods

    Supplemental Table S1 - Hepatocyte donor data.

    Supplemental Table S2 - Overview of binding site characteristics and docking scores.

    Supplemental Table S3 - Number of docking poses per cluster and their ranking according to the docking score within the set of 100 docking conformations.

    Supplemental Table S4 - Rifampin EC50 with increasing doses of nelfinavir and M8.

    Supplemental Fig. S1 - Cell toxicity of nelfinavir and M8. HepG2 and H-P cells were treated with increasing concentrations of nelfinavir or M8 metabolite for 24 h. Means ± SD (N=2) are shown.

    Supplemental Fig. S2 - Concentration response analyses of the effects of nelfinavir and/or M8 on nuclear receptors beside PXR.

    Supplemental Fig. S3 - Effect of nelfinavir on the GAL4-PXR-LBD fusion protein.

    Supplemental Fig. S4 - Effect of nelfinavir on PXR activation by the high affinity agonist T0901317.

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