Table 3 Drugs targeting the KEAP1-NRF2 pathway.
Drug or target | Cancer | Mechanism | Impact | Reference |
|---|---|---|---|---|
BDH2 | GC | Promotes ubiquitination of NRF2 | Exerts tumor-suppressive effects | [96] |
GSTM3 | GC | Inhibition of NRF2 ubiquitination and degradation. | Inhibit the proliferation and migration of GC cells | [97] |
PAQR4 | NSCLC | Inhibition of NRF2 ubiquitination and degradation. | Enhancing the expression of antioxidant genes correlates with chemotherapy resistance. | [100] |
DHT | OT | Promotes ubiquitination of NRF2 | Activating oxidative stress, Exhibiting anti-tumor effects | [102] |
SIT | OC | Trigger NRF2 ubiquitin-dependent degradation. | Promoting OC cell death | [103] |
Brucein D | PDAC | Promote ubiquitin-proteasome-dependent degradation of NRF2. | Enhancing the sensitivity of PDAC cells to GEM | [104] |
TNFAIP2 | HNSCC | Inhibit ubiquitin-proteasome-mediated degradation of NRF2. | Developing resistance to CDDP | [105] |
DDRGK1 | OS | Inhibit ubiquitin-proteasome-mediated degradation of NRF2. | Enhancing osteosarcoma sensitivity to DOX and etoposide. | [106] |
TRIM22 | OS | Promote ubiquitination and degradation of NRF2. | Inhibiting the progression of osteosarcoma. | [108] |
Brusatol | AML | Promotes ubiquitination of NRF2 | Enhancing the sensitivity of AML cells to cytarabine. | [109] |
Brusatol | EC | Promotes ubiquitination of NRF2 | Enhancing the sensitivity of endometrial cancer to progestins. | [110] |
Brusatol | HER2-positive cancer | Promotes ubiquitination of NRF2 | Inhibiting the proliferation of HER2-positive cancer cells. | [111] |
