The Human Nuclear Xenobiotic Receptor PXR: Structural Determinants of Directed Promiscuity

By R. Watkins, G. Wisely, L. Moore, J. Collins, M. Lambert, Shawn P. Williams, T. Willson, S. Kliewer, M. Redinbo. Science, 2001

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Implications of protein flexibility for drug discovery (2003, background): “Another example of directed promiscuity is provided by the pregnane X receptor (PXR), a ligand-activated transcription factor that controls expression of the genes for the cytochrome P450 CYP3A enzyme”
Symbiotic Bacterial Metabolites Regulate Gastrointestinal Barrier Function via the Xenobiotic Sensor PXR and Toll-like Receptor 4 (2014, positive): “…metabolites (e.g., bile acids and farnesoid x receptor (FXR), dietary ligands and aryl hydrocarbon receptor (AhR), we focused on pregnane X receptor (PXR), since its promiscuous ligand binding pocket might well be capable of accomodating diverse small bacterial metabolites (Watkins et al., 2001).”
The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. (2002, background): “Recently, the elucidation of the threedimensional structure of the PXR ligand binding domain (LBD) has provided important insights into the structural basis for the promiscuous ligand binding properties of this unusual NR (17).”
Multidrug Resistance in Bacteria (2009, background): “These features are similar to the binding of ligands to the human pregnane X receptor, a transcriptional regulator that binds to a number of xenobiotics (51).”