Xing Yaqi, Yan Jiong, Niu Yongdong
Department of Pharmacology, Shantou University Medical College, Shantou 515041, China.
Center for Pharmacogenetics, University of Pittsburgh, PA 15261, USA.
Acta Pharm Sin B. 2020 Feb;10(2):197-206. doi: 10.1016/j.apsb.2019.06.012. Epub 2019 Jun 29.
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 receptor, the cellular function of PXR is mostly exerted by its binding to the regulatory gene sequences in a ligand-dependent manner. Classical downstream target genes of PXR participate in xenobiotic responses, such as detoxification, metabolism and inflammation. Emerging evidence also implicates PXR signaling in the processes of apoptosis, cell cycle arrest, proliferation, angiogenesis and oxidative stress, which are closely related to cancer. Here, we discussed, in addition to the characterization of PXR , the biological function and regulatory mechanism of PXR signaling in cancer, and its potential for the targeted prevention and therapeutics.
孕烷X受体(PXR,NR1I2)是核受体超家族的典型成员。PXR可被内源性物质和外源性物质激活。作为关键的外源性物质受体,PXR的细胞功能主要通过其以配体依赖的方式与调控基因序列结合来发挥。PXR的经典下游靶基因参与外源性物质反应,如解毒、代谢和炎症。新出现的证据还表明PXR信号传导参与了凋亡、细胞周期停滞、增殖、血管生成和氧化应激等过程,这些过程与癌症密切相关。在此,我们除了讨论PXR的特征外,还讨论了PXR信号传导在癌症中的生物学功能和调控机制,以及其在靶向预防和治疗方面的潜力。