2024年11月1日 · We found a significant decrease in both mRNA and protein levels of PXR in both human and murine aortic smooth muscle cells from AAA tissues, accompanied with phenotypic switching of vascular smooth muscle cell and increased oxidative stress.

Moreover, PXR overexpression ameliorated the cisplatin-induced inflammatory response and accumulation of mitochondrial ROS and reversed the cisplatin-induced alterations in MMP, mtDNA copy number, ATP production, and reduced …

结果表明，rBMECs 中 PXR 的过表达可以显着抵消连接蛋白的减少，并下调 OGD 损伤引起的增加的 p-IκB-α 和 p-NF-κB。 然而，IPA 的保护作用被 PXR 的拮抗剂逆转。

PXR/AhR 核受体激活实验. 通常采用癌细胞系进行PXR核受体激活实验，例如采用瞬时或者稳定转染PXR和报告基因的HepG2或HuH7癌细胞，报告基因常采用如荧光素酶、氯霉素乙酰转移酶或胎盘分泌碱性磷酸酶。

2023年1月1日 · Fibrosis is a common complication of inflammatory bowel diseases (IBDs). The pregnane X receptor (PXR) (encoded by NR1I2) suppresses intestinal inflammation and has been shown to influence liver fibrosis. In the intestine, PXR signaling is influenced by microbiota-derived indole-3-propionic acid (IPA).

Recently, microRNA (miR)-34a, miR-140-3p, miR-148a and miR-449a were found to downregulate the expression of PXR through the identification and interaction at the 3ʹ-untranslated region (3ʹ-UTR) of PXR mRNA in the hepatocellular carcinoma cell lines, which might augment the sensitivity of anti-cancer medicines30, 31, 32.

2003年7月1日 · A series of N-hydroxyformamide tumor necrosis factor-α converting enzyme (TACE)/matrix metalloprotease (MMP) inhibitors were evaluated for their potential to induce human cytochrome P450 3A (CYP3A). Two in vitro assays were used: 1) a cell-based reporter gene assay for activation of the pregnane X receptor (PXR), and 2) a primary “sandwich ...

Several bile acid transporters (bile salt export pump, Oatp1, Oatp4), catabolism enzymes (Cyp3a11) and upstream nuclear receptors (small heterodimer partner, FXR) appear to be significantly modified in Pxr-null, Car-null or Pxr/Car-null mice by LCA treatment compared with wild-type mice (Uppal et al., 2005).

A series of N-hydroxyformamide tumor necrosis factor-alpha converting enzyme (TACE)/matrix metalloprotease (MMP) inhibitors were evaluated for their potential to induce human cytochrome P450 3A...

new antagonists and their co-crystal structures, revealing molecu-lar determinants of PXR antagonism and paving the way for developing antagonists as therapeutics and pre-venting undesirable PXR activation. P-glycoprotein/MDR1, are …