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Table 2 Agonists and inhibitors of ferroptosis

From: Role of ferroptosis in chronic kidney disease

Classification

Reagents

Targets

References

Agonists

Erastin

System Xc− (direct), VDAC2/3 (direct), p53 (enhances ferroptosis by activating p53)

[23, 98]

 

RSL3

GPX4 (direct)

[14]

 

Sulfasalazine

System Xc− (a novel, potent inhibitor of System Xc−)

[99]

 

Interleukin-6

System Xc− (activates System Xc− via the JAK2/STAT3 pathway)

[100]

 

Sorafenib

System Xc− (Inhibit System Xc− by upstream)

[101]

 

(R)-DCPP

GSH (unknown), GPX4 (unknown)

[102]

 

Acetaminophen

GSH (direct)

[103]

 

Cisplatin

GSH (direct)

[104]

 

FINO2

GPX4 (indirect), Fe2+ (direct)

[105]

 

Lipopolysaccharide

SLC7A11 (unknown), GPX4 (unknown)

[106]

 

Legumain

GPX4 (promotes chaperone-mediated autophagy of GPX4)

[107]

 

DPI2

GSH (unknown)

[41]

 

Dexamethasone

GSH (indirect)

[108]

 

Siramesine

FPN (unknown), FT (unknown)

[109]

 

Dihydroartemisinin

FT (degradation of ferritin in an autophagy-independent manner)

[110]

 

FIN56

GPX4, CoQ10 (GPX4 degradation and squalene synthase activation inhibit coenzyme Q10 through acetyl-CoA carboxylase activity)

[111]

 

Manganese

ROS (direct), Lipid peroxidation (direct)

[112]

Inhibitors

Fer-1

ROS (direct)

[113]

 

SRS 11–92

ROS (direct)

[114]

 

Vitamin E

ROS (direct)

[115]

 

Nuciferine

ROS (direct)

[116]

 

Liproxstatin-1

ROS (direct)

[117]

 

Irisin

Nrf2 (unknown), GPX4 (unknown)

[118]

 

Platycodin D

GPX4 (unknown) regulates ferroptosis through GPX4

[119]

 

Ginkgolide B

GPX4 (inhibiting the ubiquitination of GPX4.)

[120]

 

Canagliflozin

system Xc− (unknown), GPX4 (unknown), GSH (unknown)

[121]

 

BRD4770

System Xc−-GPX4 (unknown), FSP1-CoQ10 (unknown), GCH1-BH4 (unknown)

[122]

 

Quercetin

ROS (unknown), GSH (unknown)

[123]

 

Hydropersulfides

ROS (direct)

[124]

 

Ginsenoside Rg1

GPX4 (unknown), GSH (unknown), FSP1 (unknown) its antiferroptosis activity was dependent on FSP1

[125]

 

MCTR1

Nrf2 (suppresses ferroptosis the Nrf2 signaling)

[126]

 

Entacapone

Nrf2 (affects the p62-KEAP1-NRF2 pathway, thereby upregulatin NRF2)

[127]

 

Astragaloside-IV

Nrf2 (inhibited miR-138-5p expression, subsequently increasing Sirt1/Nrf2 activity)

[128]

 

Forsythoside A

Nrf2 (unknown), GPX4 (unknown) Nrf2/GPX4 axis plays a key role

[129]

 

Rosiglitazone

ACSL4 (direct)

[130]

 

Pioglitazone

ACSL4 (direct)

[130]

 

Troglitazone

ACSL4 (direct)

[130]