Identification of Novel Activators of Constitutive Androstane Receptor from FDA-Approved Drugs by Integrated Computational and Biological Approaches

Purpose The constitutive androstane receptor (CAR, NR1I3) is a xenobiotic sensor governing the transcription of numerous hepatic genes associated with drug metabolism and clearance. Recent evidence suggests that CAR also modulates energy homeostasis and cancer development. Thus, identification of no...

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Veröffentlicht in:	Pharmaceutical research 2013-02, Vol.30 (2), p.489-501
Hauptverfasser:	Lynch, Caitlin, Pan, Yongmei, Li, Linhao, Ferguson, Stephen S., Xia, Menghang, Swaan, Peter W., Wang, Hongbing
Format:	Artikel
Sprache:	eng
Schlagworte:	Aryl Hydrocarbon Hydroxylases - genetics Biochemistry Biological and medical sciences Biomedical and Life Sciences Biomedical Engineering and Bioengineering Biomedicine Cells, Cultured Computational Biology - methods Constitutive Androstane Receptor Cytochrome P-450 CYP2B6 Databases, Pharmaceutical Drug Discovery - methods FDA approval Gene Expression Regulation - drug effects General pharmacology Genes Hep G2 Cells Hepatocytes - drug effects Hepatocytes - metabolism Humans Medical Law Medical sciences Molecular biology Molecular Docking Simulation Oxidoreductases, N-Demethylating - genetics Pharmaceutical Preparations - chemistry Pharmaceutical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology Pharmacology. Drug treatments Pharmacology/Toxicology Pharmacy Protein Transport - drug effects Proteins Receptors, Cytoplasmic and Nuclear - agonists Receptors, Cytoplasmic and Nuclear - metabolism Research Paper United States United States Food and Drug Administration
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