N-1H-Benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists

…, V Nahoum, A Mallavialle, JF Guichou, J Milhau…

文献索引：Benod, Cindy; Subra, Guy; Nahoum, Virginie; Mallavialle, Aude; Guichou, Jean-Francois; Milhau, Julien; Robles, Samuel; Bourguet, William; Pascussi, Jean-Marc; Balaguer, Patrick; Chavanieu, Alain Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 7 p. 3537 - 3549

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被引用次数: 7

摘要

The Human Pregnane X Receptor (hPXR) is a nuclear receptor that regulates the expression of phase I and phase II drug-metabolizing enzymes, as well as that of drug transporters. Because this receptor plays a critical role in protecting tissues from potentially toxic endo-and xenobiotics, highly active agonists could represent novel therapeutic tools in treating several human diseases. Using an in vitro screening reporter system that allow to ...