As a promiscuous xenobiotic sensor, pregnane X receptor (PXR) plays a crucial role in drug
metabolism. Since dietary phytochemicals exhibit the potential to modulate human PXR, this …

Abstract Pregnane X receptor (PXR, NR1I2) is a prototypical member of the nuclear receptor
superfamily. PXR can be activated by both endobiotics and xenobiotics. As a key xenobiotic …

Emission fluorescence is one of the most versatile and powerful biophysical techniques
used in several scientific subjects. It is extensively applied in the studies of proteins, their …

Citrus fruit has long been considered a healthy food, but its role and detailed mechanism in
lifespan extension are not clear. Here, by using the nematode C. elegans, we identified that …

Nuclear receptors are ligand-activated transcription factors that can often be useful drug
targets. Unfortunately, ligand promiscuity leads to two-thirds of receptors remaining clinically …

Humans are chronically exposed to mixtures of xenobiotics referred to as endocrine-
disrupting chemicals (EDCs). A vast body of literature links exposure to these chemicals with …

Both aryl hydrocarbon receptor (AhR) and pregnane X receptor (PXR) belong among key
regulators of xenobiotic metabolism in the intestinal tissue. AhR in particular is activated by a …

Ligand-binding promiscuity in detoxification systems protects the body from toxicological
harm but is a roadblock to drug development due to the difficulty in optimizing small …

We previously reported a specific inverse agonist (SPA70) of the nuclear receptor pregnane
X receptor (PXR). However, derivatization of SPA70 yielded only agonists and neutral …

The human nuclear receptor (NR) family of transcription factors contains 48 proteins that
bind lipophilic molecules. Approved NR therapies have had immense success treating …