Discovery of a highly active ligand of human pregnane x receptor: a case study from pharmacophore modeling and virtual screening to in vivo biological activity

The human pregnane X receptor (hPXR) is a nuclear receptor that regulates the expression of phase I and II drug-metabolizing enzymes as well as that of drug transporters. In addition, this receptor plays a critical role in cholesterol homeostasis and in protecting tissues from potentially toxic endobiotics. hPXR is activated by a broad spectrum of […]

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