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Rapid CommunicationShort Communication

Rosuvastatin and Atorvastatin Are Ligands of the Human Constitutive Androstane Receptor/Retinoid X Receptor α Complex

Tadeja Režen, Mateja Hafner, Sandhya Kortagere, Sean Ekins, Vesna Hodnik and Damjana Rozman
Drug Metabolism and Disposition August 2017, 45 (8) 974-976; DOI: https://doi.org/10.1124/dmd.117.075523
Tadeja Režen
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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Mateja Hafner
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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Sandhya Kortagere
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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Sean Ekins
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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Vesna Hodnik
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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Damjana Rozman
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine (T.R., M.H., D.R.), and Department of Biology, Biotechnical Faculty (V.H.), University of Ljubljana, Ljubljana, Slovenia; Department of Microbiology and Immunology, College of Medicine, Drexel University, Philadelphia, Pennsylvania (S.K.); Collaborations Pharmaceuticals, Inc., Fuquay Varina, North Carolina (S.E.)
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    Fig. 1.

    SPR analysis of atorvastatin, rosuvastatin, and CITCO binding to hCAR/hRXRα-LBD heterodimer. Different concentrations (1.56, 3.125, 12.5, 25, and 50 µM for CITCO and 6, 12.5, 25, 50, 75, 100, and 150 µM for atorvastatin and rosuvastatin) of analytes were tested for the binding (left panels). The binding curves (right panels) were generated by fitting the steady-state response levels at the end of the association phase versus the concentration of the injected analyte. The KD values were obtained by fitting the data to the steady-state affinity model. For each analyte six or seven independent titration experiments were performed.

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    TABLE 1

    KD values and theoretical and measured maximal responses of atorvastatin, rosuvastatin, and CITCO binding to hCAR/hRXRα-LBD heterodimer as measured by surface plasmon resonance and by scores of ligand-based (CAR pharmacophore) and structure-based (CAR score docking) in silico calculations

    CompoundKD (µM)CARMaximal Response
    Score DockingPharmacophoreTheoreticalMeasured
    Atorvastatin0.225 ± 0.0673.182.0784251
    Rosuvastatin0.144 ± 0.0367.09—7086
    CITCO0.045 ± 0.0463.02—3074

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      Supplemental methods, 3 figures, 1 table.

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Drug Metabolism and Disposition: 45 (8)
Drug Metabolism and Disposition
Vol. 45, Issue 8
1 Aug 2017
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Rapid CommunicationShort Communication

Statins Are Ligands of Human CAR/RXRα Complex

Tadeja Režen, Mateja Hafner, Sandhya Kortagere, Sean Ekins, Vesna Hodnik and Damjana Rozman
Drug Metabolism and Disposition August 1, 2017, 45 (8) 974-976; DOI: https://doi.org/10.1124/dmd.117.075523

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Rapid CommunicationShort Communication

Statins Are Ligands of Human CAR/RXRα Complex

Tadeja Režen, Mateja Hafner, Sandhya Kortagere, Sean Ekins, Vesna Hodnik and Damjana Rozman
Drug Metabolism and Disposition August 1, 2017, 45 (8) 974-976; DOI: https://doi.org/10.1124/dmd.117.075523
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