SPA70 is a cell penetrant, potent and highly selective human pregnane X receptor (hPXR) antagonist that inhibits hPXR in humanized mouse models. It inhibits hPXR-mediated drug metabolism in in primary human hepatocytes and in mouse models.
cell penetrant, potent and highly selective human pregnane X receptor (hPXR) antagonist that inhibits hPXR in humanized mouse models.
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are ligand-activated nuclear receptors (NRs) that are notorious for their role in drug metabolism, causing unintended drug-drug interactions and decreasing drug efficacy. They control the xenobiotic detoxification system by
Many drugs bind to and activate human pregnane X receptor (hPXR) to upregulate drug-metabolizing enzymes, resulting in decreased drug efficacy and increased resistance. This suggests that hPXR antagonists have therapeutic value. Here we report that SPA70 is a potent and
Combination of Paclitaxel and PXR Antagonist SPA70 Reverses Paclitaxel-Resistant Non-Small Cell Lung Cancer.
Niu, et al.
Cells, 11 (2022)
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