The Major Human Pregnane X Receptor (PXR) Splice Variant, PXR.2, Exhibits Significantly Diminished Ligand-Activated Transcriptional Regulation

The pregnane X receptor (PXR; PXR.1) can be activated by structurally diverse lipophilic ligands. PXR.2, an alternatively spliced form of PXR, lacks 111 nucleotides encoding 37 amino acids in the ligand binding domain. PXR.2 bound a classic CYP3A4 PXR response element (PXRE) in electrophoretic mobil...

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Veröffentlicht in:	Drug metabolism and disposition 2009-06, Vol.37 (6), p.1295-1304
Hauptverfasser:	Lin, Yvonne S., Yasuda, Kazuto, Assem, Mahfoud, Cline, Cynthia, Barber, Joe, Li, Chia-Wei, Kholodovych, Vladyslav, Ai, Ni, Chen, J. Don, Welsh, William J., Ekins, Sean, Schuetz, Erin G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alternative Splicing Biological and medical sciences Catalytic Domain Cytochrome P-450 CYP3A - chemistry Cytochrome P-450 CYP3A - genetics Cytochrome P-450 CYP3A - metabolism Gene Expression Regulation - drug effects Genes, Reporter Humans Medical sciences Microsomes, Liver Pharmacology. Drug treatments Pregnane X Receptor Promoter Regions, Genetic - drug effects Promoter Regions, Genetic - genetics Protein Binding Protein Conformation Protein Isoforms - pharmacology Receptors, Steroid - chemistry Receptors, Steroid - genetics Receptors, Steroid - metabolism Rifampin - pharmacology Transcriptional Activation - drug effects Transfection Tumor Cells, Cultured
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