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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Article DOI: 10.3791/51085-v • 10:51 min • November 15th, 2013
November 15th, 2013 •
*1, *2, 1, 1
1Department of Genetics, Albert Einstein College of Medicine, 2Shanghai Key Laboratory of Complex Prescription and MOE Key Laboratory for Standardization of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine
* These authors contributed equally

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Resumen
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Ketoconazole binds to and antagonizes Pregnane X Receptor (PXR) activation. Yeast high throughput screens of PXR mutants define a unique region for ketoconazole binding. This yeast-based genetic method discovers novel nuclear receptor interactions with ligands that associate with surface binding sites.

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Reverse Yeast Two-hybrid System Mammalian Nuclear Receptor Ligands Antagonists Pregnane X Receptor (PXR) Drug Metabolism Inflammation Hepatic Steatosis Agonist Ligands Drug-like Antagonists Binding Sites Protein Purification Structural Studies Ketoconazole Mutational Libraries AF-2 Surface Genetic Interaction Coactivator SRC-1 Antifungal Drug
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