Oxidative Medicine and Cellular Longevity / 2019 / Article / Tab 2

Review Article

Potential Applications of NRF2 Inhibitors in Cancer Therapy

Table 2


DrugPrevious useTumor type/cell linesEffectRef.

ATRA, RAR-α agonistsAPL treatment; neuroblastoma treatment; skin disordersBC/MCF-7; AML/HL60, THP-1; APL/NB4, NB4-R2; NB/HTLA-230; GBM/U251; OC/A2780 CSCDecreases NRF2 binding to ARE sites; decreases NRF2 nuclear translocation[347350]
PHA-767491Cdc7/CDK9 inhibitorPDAC/PANC-1, Capan-1; HCC/HepG2Decreases NRF2 nuclear translocation and activity[351]
SorafenibMulti-Tyrosine kinase inhibitor; antiangiogenic therapyCRC/DLD-1, HCT116; TC/FTC133, BC-PAP, 8505C; RC/ACHN, 786-O; CRC/DLD-1; HCC/HepG2, BEL7402-5FU, HuH-7; BC/MCF7, MDA-MB-231; NSCLC/CALU-3Decreases NRF2 expression and nuclear translocation[352]
AuranofinRheumatoid arthritisNSCLC/Calu-3, Calu-6, H522Decreases NRF2 activation[353]
Clobetasol PropionateSkin disordersNSCLC/A549, H2228Decreases NRF2 nuclear accumulation and promotes β-TrCP-dependent NRF2 degradation[354]
CamptothecinTopoisomerase inhibitor; chemotherapyHCC/HepG2, SMMC-7721; NSCLC/A549Decreases NRF2 expression[23]
Valproic acidHistone deacetylase inhibitor; epilepsy and seizure disorders; chemosensitizerBC/MCF7; TC/BCPAP, TCP1, BHP10-3Decreases NRF2 nuclear content[355]
MetforminAntidiabetic drugBC/MCF-7; CRC/HT-29; EC/RL95–2, Spec-2, Ishikawa; HCC/HepG2; NSCLC/A549; CC/HeLaDecreases NRF2 mRNA and protein content; decreases NRF2 expression[356361]
IsoniazidAntitubercular agentHCC/HepG2Decreases NRF2 nuclear translocation[362]