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Discovery of PXR Antagonist MI891 and PXR Degrader MI1013 and Their Roles in Hepatic Gene Regulation.

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Title: Discovery of PXR Antagonist MI891 and PXR Degrader MI1013 and Their Roles in Hepatic Gene Regulation.
Authors: Kamaraj R; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Mejdrová I; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic., Krutakova M; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Smutny T; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Škach K; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic., Dohnalova K; Czech Centre for Phenogenomics, Institute of Molecular Genetics of the Czech Academy of Sciences, Vídeňská 1083, 142 20 Prague, Czech Republic.; First Faculty of Medicine, Charles University, Katerinska 32, 112 08 Prague, Czech Republic., Smutna L; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Nellore DSS; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Dusek J; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic., Chalupsky K; Czech Centre for Phenogenomics, Institute of Molecular Genetics of the Czech Academy of Sciences, Vídeňská 1083, 142 20 Prague, Czech Republic., Hricová J; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic., Kronenberger T; DZIF Tübingen Partner Site, University Hospital Tübingen, 72076 Tuebingen, Germany., Stahl A; NMI - Natural and Medical Sciences Institute at the University of Tuebingen, Markwiesenstr. 55, 72770 Reutlingen, Germany., Templin M; NMI - Natural and Medical Sciences Institute at the University of Tuebingen, Markwiesenstr. 55, 72770 Reutlingen, Germany., Braeuning A; Department Food Safety, German Federal Institute for Risk Assessment, Max-Dohrn-Str. 8-10, Berlin 10589, Germany., Nencka R; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic., Pavek P; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
Source: Journal of medicinal chemistry [J Med Chem] 2025 Jul 24; Vol. 68 (14), pp. 14271-14299. Date of Electronic Publication: 2025 Jul 12.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
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  Data: Discovery of PXR Antagonist MI891 and PXR Degrader MI1013 and Their Roles in Hepatic Gene Regulation.
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  Data: <searchLink fieldCode="AU" term="%22Kamaraj+R%22">Kamaraj R</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Mejdrová+I%22">Mejdrová I</searchLink>; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Krutakova+M%22">Krutakova M</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Smutny+T%22">Smutny T</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Škach+K%22">Škach K</searchLink>; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Dohnalova+K%22">Dohnalova K</searchLink>; Czech Centre for Phenogenomics, Institute of Molecular Genetics of the Czech Academy of Sciences, Vídeňská 1083, 142 20 Prague, Czech Republic.; First Faculty of Medicine, Charles University, Katerinska 32, 112 08 Prague, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Smutna+L%22">Smutna L</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Nellore+DSS%22">Nellore DSS</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Dusek+J%22">Dusek J</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Chalupsky+K%22">Chalupsky K</searchLink>; Czech Centre for Phenogenomics, Institute of Molecular Genetics of the Czech Academy of Sciences, Vídeňská 1083, 142 20 Prague, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Hricová+J%22">Hricová J</searchLink>; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Kronenberger+T%22">Kronenberger T</searchLink>; DZIF Tübingen Partner Site, University Hospital Tübingen, 72076 Tuebingen, Germany.<br /><searchLink fieldCode="AU" term="%22Stahl+A%22">Stahl A</searchLink>; NMI - Natural and Medical Sciences Institute at the University of Tuebingen, Markwiesenstr. 55, 72770 Reutlingen, Germany.<br /><searchLink fieldCode="AU" term="%22Templin+M%22">Templin M</searchLink>; NMI - Natural and Medical Sciences Institute at the University of Tuebingen, Markwiesenstr. 55, 72770 Reutlingen, Germany.<br /><searchLink fieldCode="AU" term="%22Braeuning+A%22">Braeuning A</searchLink>; Department Food Safety, German Federal Institute for Risk Assessment, Max-Dohrn-Str. 8-10, Berlin 10589, Germany.<br /><searchLink fieldCode="AU" term="%22Nencka+R%22">Nencka R</searchLink>; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, 166 10 Prague 6, Czech Republic.<br /><searchLink fieldCode="AU" term="%22Pavek+P%22">Pavek P</searchLink>; Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2025 Jul 24; Vol. 68 (14), pp. 14271-14299. <i>Date of Electronic Publication: </i>2025 Jul 12.
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