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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 March 2021, 99 (3) 184-196; DOI: https://doi.org/10.1124/molpharm.120.000116
Oliver Burk
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Thales Kronenberger
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Oliver Keminer
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Serene M. L. Lee
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Tobias S. Schiergens
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Matthias Schwab
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
Björn Windshügel
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, and University of Tübingen, Tübingen, Germany (O.B., M.S.); Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany (T.K., O.K., B.W.); Biobank of the Department of General, Visceral, and Transplantion Surgery, University Hospital, Ludwig-Maximilians University, Munich, Munich, Germany (S.M.L.L., T.S.S.); Departments of Clinical Pharmacology, and Pharmacy and Biochemistry, University of Tübingen, Tübingen, Germany (M.S.); and Department of Chemistry, Institute for Biochemistry and Molecular Biology, Universität Hamburg, Hamburg, Germany (B.W.)
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Nelfinavir and PXR
Oliver Burk, Thales Kronenberger, Oliver Keminer, Serene M. L. Lee, Tobias S. Schiergens, Matthias Schwab and Björn Windshügel
Molecular Pharmacology March 1, 2021, 99 (3) 184-196; DOI: https://doi.org/10.1124/molpharm.120.000116
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