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Báo cáo Y học: Identification of residues in the PXR ligand binding domain critical for species specific and constitutive activation

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The cytochrome P450 family of enzymes has long beenknown tometabolize a wide range of compounds, includingmany of today’s most common drugs. A novel nuclearreceptor called PXR has been established as an activator ofseveral of the cytochrome P450 genes, including CYP3A4.This enzyme is believed to account for the metabolism ofmore than 50% of all prescription drugs. PXR is thereforeused as a negative selector target and discriminatory filter inpreclinical drug development.
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Báo cáo Y học: Identification of residues in the PXR ligand binding domain critical for species specific and constitutive activation

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