Table 1.
Pharmacological modulation of ferroptosis induction in cancer therapy.
| Compound | Molecular target(s) | Mechanism of action | Cancer | References (PMID) |
|---|---|---|---|---|
| RSL3 | GPX4 | Inhibits GPX4 through the alkylation of selenocysteine | Fibrosarcoma, NSCLC, pancreatic cancer, leukemia, TNBC, HCC, thyroid cancer, CRC |
24439385 30545638 36257316 30524291 36895980 37596261 |
| FINO2 | GPX4 and iron | Iron and PUFAs oxidation, ROS production and deactivation of GPX4 | Fibrosarcoma | 29610484 |
| Artesunate | GPX4 | Oxidation of iron, depletion of GSH and induction of ferritinophagy | RCC, HCC, non-Hodgkin lymphoma, DLBCL, PDAC |
35028002 38560249 33121039 37326033 26097885 |
| Erastin | SLC7A11 | Inhibition of SLC7A11 and GSH depletion | HCC, melanoma, NSCLC, LUAD, ovarian cancer, thyroid cancer, glioma, breast cancer, RCC, prostate cancer |
31974380 37277863 31897145 33483372 |
| JQ1 | SLC7A11, GPX4 and BRD4 | BRD4 inhibition, induction of ferritinophagy and downregulation of GPX4, SLC7A11 and SLC3A2 | Breast cancer, lung cancer |
30988278 34003467 |
| Sorafenib | SLC7A11and GPX4 | Inhibition of SLC7A11 and TRIM54-mediated FSP1 ubiquitination | AML, HCC, neuroblastoma, NSCLC, RCC, liver cancer |
25368241 37460053 37351514 37695069 27264843 22725255 34768109 |
| Cisplatin | GSH | Reaction with GSH to inhibit GPX4 | Ovarian cancer, pancreatic cancer, NSCLC, urothelial cancer |
27477897 28012440 35534546 35784745 |
| Cyst(e)inase | GSH | Degradation of cysteine and cystine, leading to a decrease in GSH levels | RCC, prostate cancer, chronic lymphocytic leukemia, pancreatic cancer, ovarian cancer |
27869804 35086957 31043744 32241947 |
| Heme | Iron | Upregulation of HMOX1 and increase in LIP | Glioblastoma, leukemia, lung cancer |
36228518 36395526 |
| Lovastatin | HMGCR | Increases the efficacy of ICB by downregulating PD-L1 expression | NSCLC, prostate cancer, ovarian cancer | 35943796 |
| Simvastatin | HMGCR | Downregulation of the mevalonate pathway and GPX4 | TNBC | 34627266 |
| Atorvastatin | HMGCR | Induction of mitochondria-dependent ferroptosis by downregulating GPX4 | CRC |
35309902 34564973 |
| Haloperidol | DRD2 and S1R | Association with autophagy-mediated ferroptosis | Glioblastoma, HCC |
37249604 28756230 37249604 |
| Curcumin derivatives | FTH1 and TFEB | TFEB-mediated lysosome degradation of GPX4 Downregulation of lncRNA H19 |
Lung cancer |
37689240 35224289 |