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. Author manuscript; available in PMC: 2015 Aug 1.
Published in final edited form as: Cancer Chemother Pharmacol. 2014 Jun 3;74(2):217–227. doi: 10.1007/s00280-014-2494-9

Table 1.

The function of PXR in the chemotherapy of cancer

Drugs PXR PXR target genes Chemotherapeutic effects Models References
Irinotecan Expression ↑ by transfection UGT1A1 ↑ UGT1A9 ↑ UGT1A10 ↑ CYP3A4 ↑ Metabolism ↑
Sensitivity ↓
LS174T cells, HCT116 cells [64, 65]
Expression ↓ by shRNA and siRNA UGT1A1 ↓ Metabolism ↓
Sensitivity ↑
LS174T cells, HCT116 cells [64]
Activation by rifampicin and SN-38 UGT ↑ CYP3A4 ↑ CYP3A5 ↑ MRP2 ↑ P-gp ↑ Metabohsm ↑
Efflux ↓
Mice, LS180 cells, HePG2 cells, HCT116 cells [18, 24, 65, 66, 68]
Tamoxifen Expression ↑ by transfection Ki-67 ↑ ABCC2 ↑ OATP1A2 ↑ Drug resistance ↑ MCF-7 cells, TAMR-MCF-7 cells [19, 73]
Expression ↓ by shRNA Sensitivity ↑ MDA-MB-231 cells, MCF-7 cells [74, 75]
Activation by TAM,4-OH-TAM, SR12813, rifampicin, anandamide and clotrimazole CYP3A4 ↑ MDR1 ↑ MRP2 ↑ OATP1A2 ↑ Metabolism ↑
Efflux ↑
Drug resistance ↑
MCF-7 cells, T-47D cells, ZR-75-1 cells, MCF-7 cells [73-79]
BAX ↑ P21 ↑ Apoptosis ↑ MCF-7 cells, ZR-75-1 cells [50]
Inhibition by A-792611 OATPlA2↓ Sensitivity ↑ T47-D cells [75]
Paclitaxel Expression↓ by siRNA and shRNA CYP3A4 ↓ MDR1 ↓ Apoptosis ↑ Proliferation ↓ HEC-1 cells, MDA-MB-231 cells [22, 74, 86]
Activation by paclitaxel, SR12813, rifampicin CYP3A ↑ CYP2B6 ↑ CYP2C8 ↑ MDR1 ↑ Metabolism ↑
Efflux ↑
Apoptosis ↓
Proliferation ↑
HEC-1 cells, PC-3 cells, MDA-MB-231 cells, SKOV-3 cells [24, 74, 86-89]
Doxorubicin Avtivation by rifampicin and VP-PXR BAG3 ↓ BIRC2 ↓ MCL-1 ↓ BAK1 ↓ TP53/p53 ↓ P-gp ↑ Apoptosis ↓
Sensitivity ↓
HCT116 cells, LS180 cells [52, 77]
Inhibition by ecteinascidin-743 P-gP↓ Sensitivity ↑ Osteosarcoma cells [94]
PXR polymorphisms Patients harboring PXR*1B showed higher CYP3A4 levels compared with PXR*lA and PXR*lC Patients harboring PXR*1B showed higher drug clearance compared with PXR*lA and PXR*lC Patients [95]
Vinblastine Activation by SR12813 and vinblastine ABCC2 ↑ ABCC3 ↑ CYP3A4 ↑ Sensitivity ↓ PC-3 cells, LS174T cells, Patients [86, 101, 102]
Expression↓ by siRNA MDR1 ↑ CYP3A4 ↑ Sensitivity ↑ MCF-7 cells, MDA-MB-231 cells [74]
ATRA Activation by PCN, Rifampin and dexamethasone CYP3A ↑ CYP26 ↑ MDR1 ↑ ABCC3 ↑ OATP ↑ AUC ↓
Sensitivity ↓
Mice [109]
CPA&IFO Activation by rifampin and dexamethasone CYP3A4 ↑ CYP2C8 ↑ CYP2C9 ↑ Metabolism ↑
Sensitivity ↑
Primary cultures hepatocytes [114]