From: Induction and application of ferroptosis in cancer therapy
Target | Compound/Drug | Mechanism | Tumour type | Refs |
---|---|---|---|---|
Class I FINs | ||||
 SLC7A11 | Erastin | Inhibit SLC7A11 and prevent cystine import, combine with VDAC2/3 | Glioma, lung cancer, fibrosarcoma, melanoma, breast cancer, cervical cancer, RCC | |
Piperazine erastin (PE) | Inhibit SLC7A11 and prevent cystine import | Fibrosarcoma | [33] | |
Imidazole ketone erastin (28) | Inhibit SLC7A11 and prevent cystine import | DLBCL | [20] | |
Sulfasalazine | Inhibit SLC7A11 | Breastcancer, glioblastoma, fibrosarcoma, NSCLC, prostate cancer | ||
Sorafenib | Inhibit SLC7A11 | AML, HCC, neuroblastoma, NSCLC, RCC | [65] | |
Glutamate | Inhibit SLC7A11 | - | ||
 GCL | Buthionine sulfoximine (113) | Inhibit the GCL and reduce GSH synthesis | Melanoma, neuroblastoma | |
 GSH | Cyst(e)inase | Degrade cysteine and cystine, reduce GSH levels | Prostate cancer, chronic lymphocytic leukemia and pancreatic cancer | |
Cisplatin | Combine with GSH to inactivate GPX4 | Ovarian cancer, pancreatic cancer, NSCLC, urothelial cancer | ||
Class II and III FINs | ||||
 GPX4 | RSL3 | Inhibit GPX4 directly | Fibrosarcoma, NSCLC, pancreatic cancer, leukemia | |
FIN56 | Combine and activate SQS to reduce CoQ10 | Fibrosarcoma | ||
ML162(DPI7), DPI12, ML210(DPI10), DPI13 | Inhibit GPX4 covalently | - | [33] | |
Altretamine | Inhibit GPX4 | Lymphoma, sarcoma, ovarian cancer | [77] | |
FINO2 | Oxidize Fe2+ and PUFAs, promote the accumulation of ROS; indirectly inactivate GPX4; | Fibrosarcoma | ||
Class IV FINs | ||||
 Iron | Heme | Up-regulate HMOX1 expression and increase LIP | Glioblastoma, leukemia | |
Withaferin A | Up-regulate HMOX1 expression and increase LIP at middle dose and inactivate GPX4 at high doses | Breast cancer, Neuroblastoma | ||
BAY 11–7085 | Up-regulate HMOX1 expression and increase LIP | CRC, cervical cancer | [83] | |
Artesunate | Oxidize Fe2+, promote the accumulation of ROS, induce ferritinophagy | Pancreatic cancer | ||
Dihydroartemisinin | Oxidize Fe2+, promote the accumulation of ROS, induce ferritinophagy and inhibit ferritin synthesis | Ovarian cancer | ||
Siramesine, lapatinib | Decrease SLC40A1, increase transferrin and LIP | Breast cancer | [113] | |
Neratinib | Decrease SLC40A1, increase transferrin and LIP | Breast cancer, CRC | [127] | |
Salinomycin | Decrease SLC40A1, increase transferrin and LIP | Various solid tumour types | [128] | |
Others | ||||
 ROS | BAY 87–2243 | Combine with mitochondrial respiratory chain complex I | NSCLC | [83] |
 FSP1 | iFSP1 | Inhibit the reduction of CoQ10 by FSP1 | Fibrosarcoma, NSCLC | |
 HMGCR | Statins | Combine as lipid- lowering agent, in oncology phase I trials; CoQ10 deletion | Breast cancer, AML, HCC, MM, Fibrosarcoma, NSCLC | |
 Nrf2 | Trigonelline, brusatol | Nrf2 inhibition | HCC, NSCLC |