Research ArticleArticle
Inhibition of Human Sterol Δ7-Reductase and Other Postlanosterol Enzymes by LK-980, a Novel Inhibitor of Cholesterol Synthesis
Jure Ačimovič, Tina Korošec, Matej Seliškar, Ingemar Bjorkhem, Katalin Monostory, Pal Szabo, Jean-Marc Pascussi, Ales Belič, Uroš Urleb, Darko Kocjan and Damjana Rozman
Drug Metabolism and Disposition January 2011, 39 (1) 39-46; DOI: https://doi.org/10.1124/dmd.110.035840
Jure Ačimovič
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Tina Korošec
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Matej Seliškar
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Ingemar Bjorkhem
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Katalin Monostory
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Pal Szabo
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Jean-Marc Pascussi
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Ales Belič
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Uroš Urleb
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Darko Kocjan
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
Damjana Rozman
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia (J.A., D.R.); Lek Pharmaceuticals d.d., Drug Discovery, Ljubljana, Slovenia (T.K., M.S., U.U.); Division of Clinical Chemistry, Karolinska Institutet, Division of Clinical Chemistry, Stockholm, Huddinge, Sweden (I.B.); Chemical Research Center, Hungarian Academy of Sciences, Budapest, Hungary (K.M., P.S.); Institute of Functional Genomics, Centre National de la Recherche Scientifique Unité Mixte de Recherche 5203 and Institut National de la Santé et de la Recherche Médicale U661, University Montpellier 1 and 2, Montpellier, France (J.-M.P.), Faculty of Electrical Engineering, University of Ljubljana, Ljubljana, Slovenia (A.B.); and L14 Laboratory for Biomolecular Structure, National Institute of Chemistry, EN→FIST Center of Excellence, Ljubljana, Slovenia (D.K.)
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Research ArticleArticle
Inhibition of Human Sterol Δ7-Reductase and Other Postlanosterol Enzymes by LK-980, a Novel Inhibitor of Cholesterol Synthesis
Jure Ačimovič, Tina Korošec, Matej Seliškar, Ingemar Bjorkhem, Katalin Monostory, Pal Szabo, Jean-Marc Pascussi, Ales Belič, Uroš Urleb, Darko Kocjan and Damjana Rozman
Drug Metabolism and Disposition January 1, 2011, 39 (1) 39-46; DOI: https://doi.org/10.1124/dmd.110.035840
Research ArticleArticle
Inhibition of Human Sterol Δ7-Reductase and Other Postlanosterol Enzymes by LK-980, a Novel Inhibitor of Cholesterol Synthesis
Jure Ačimovič, Tina Korošec, Matej Seliškar, Ingemar Bjorkhem, Katalin Monostory, Pal Szabo, Jean-Marc Pascussi, Ales Belič, Uroš Urleb, Darko Kocjan and Damjana Rozman
Drug Metabolism and Disposition January 1, 2011, 39 (1) 39-46; DOI: https://doi.org/10.1124/dmd.110.035840
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