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. 2021 Nov 2;4(4):946–964. doi: 10.20517/cdr.2021.82

Table 2.

Elevation of cellular drug metabolism in relation to pregnane X receptor or steroid and xenobiotic receptor

Background on PXR/SXR research Materials and methods Results and discussion Ref.
PXR can enhance detoxification of irinotecan in cancer cells PXR cDNA-mediated expression in human colorectal cancer cell lines
Human liver and colon biopsies
PXR cDNA-mediated overexpression led cell-resistance to irinotecan and SN38 Raynal et al.[25]
PXR/SXR is known to be involved in the upregulation of genes associated with the detoxification of irinotecan ChIP with anti-PXR/SXR antibodies. PXR/SXR mediated induction of CYPs and ABC transporters after exposure of LS180 and HepG2 cells to irinotecan or SN-38 PXR enrichment induced by SN-38 treatment to CYP3A4 gene enhancer and promoter regions
SN-38 induced CYP3A4/5 (6-13-fold) and UGT1A1 and MRP2 by 2-3-fold. PXR/SXR decreased irinotecan cytotoxicity in LS180
Basseville et al.[26]

ChIP: Chromatin-immunoprecipitation; PXR: pregnane X receptor; SXR: steroid and xenobiotic receptor; CYPs: cytochrome P-450; ABC: ATP-binding cassette.