Laboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.
Br J Pharmacol. 2011 Jun;163(3):461-8. doi: 10.1111/j.1476-5381.2010.01129.x.
Pregnane X receptor (PXR) is a pivotal nuclear receptor modulating xenobiotic metabolism primarily through its regulation of CYP3A4, the most important enzyme involved in drug metabolism in humans. Due to the marked species differences in ligand recognition by PXR, PXR-humanized (hPXR) mice, and mice expressing human PXR and CYP3A4 (Tg3A4/hPXR) were established. hPXR and Tg3A4/hPXR mice are valuable models for investigating the role of PXR in xenobiotic metabolism and toxicity, in lipid, bile acid and steroid hormone homeostasis, and in the control of inflammation.
妊娠相关 X 受体 (PXR) 是一种重要的核受体，主要通过调节 CYP3A4 来调节外源性物质代谢，CYP3A4 是人类药物代谢中最重要的酶。由于 PXR 对配体的识别存在明显的种属差异，因此建立了 PXR 人源化 (hPXR) 小鼠和表达人 PXR 和 CYP3A4 的小鼠 (Tg3A4/hPXR)。hPXR 和 Tg3A4/hPXR 小鼠是研究 PXR 在异生物质代谢和毒性、脂质、胆汁酸和甾体激素稳态以及炎症控制中的作用的有价值的模型。
