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Table 1 Inducers of ferroptosis

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

[7, 29, 30]

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

[7, 97]

Sorafenib

Inhibit SLC7A11

AML, HCC, neuroblastoma, NSCLC, RCC

[65]

Glutamate

Inhibit SLC7A11

-

[7, 17]

 GCL

Buthionine sulfoximine (113)

Inhibit the GCL and reduce GSH synthesis

Melanoma, neuroblastoma

[33, 70, 115]

 GSH

Cyst(e)inase

Degrade cysteine and cystine, reduce GSH levels

Prostate cancer, chronic lymphocytic leukemia and pancreatic cancer

[107, 116]

Cisplatin

Combine with GSH to inactivate GPX4

Ovarian cancer, pancreatic cancer, NSCLC, urothelial cancer

[94, 117,118,119]

Class II and III FINs

 GPX4

RSL3

Inhibit GPX4 directly

Fibrosarcoma, NSCLC, pancreatic cancer,

leukemia

[19, 33, 120]

FIN56

Combine and activate SQS to reduce CoQ10

Fibrosarcoma

[77, 111]

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

[33, 55]

Class IV FINs

 Iron

Heme

Up-regulate HMOX1 expression and increase LIP

Glioblastoma, leukemia

[34, 38]

Withaferin A

Up-regulate HMOX1 expression and increase LIP at middle dose and inactivate GPX4 at high doses

Breast cancer, Neuroblastoma

[82, 121]

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

[122,123,124,125,126]

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

[109, 110]

 HMGCR

Statins

Combine as lipid- lowering agent, in oncology phase I trials; CoQ10 deletion

Breast cancer, AML, HCC, MM, Fibrosarcoma, NSCLC

[111, 127, 129]

 Nrf2

Trigonelline, brusatol

Nrf2 inhibition

HCC, NSCLC

[34, 130]

  1. AML acute myeloid leukaemia, CRC colorectal cancer, GSH glutathione; HCC hepatocellular carcinoma, MM multiple myeloma, NA not available, NSCLC non- small- cell lung cancer, RCC renal cell carcinoma, DLBCL diffuse large B cell lymphoma