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DRUG CLASS:

Ferroptosis inducer

2d
Dual inhibition of BET and EP300 has antitumor activity in undifferentiated pleomorphic sarcomas and synergizes with ferroptosis induction. (PubMed, Transl Oncol)
Among the three compounds tested, the dual inhibitor NEO2734 was the most potent, decreased the viability of UPS cells in vitro through a regulation of E2F targets and cell cycle and decreased the tumor growth in vivo. Moreover, we identified GPX4 as a gene involved in resistance and showed synergy between BET inhibition and ferroptosis induction. The present study demonstrated that dual BET/EP300 inhibitors have a relevant antitumor activity in a subgroup of UPS characterized by expression of MYC-targets pathway and identified a potent combination therapeutic strategy that deserves further investigation in the clinical setting.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • EP300 (E1A binding protein p300) • GPX4 (Glutathione Peroxidase 4)
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MYC expression
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EP31670
3d
Susceptibility of Mitophagy-Deficient Tumors to Ferroptosis Induction by Relieving the Suppression of Lipid Peroxidation. (PubMed, Adv Sci (Weinh))
Mitophagy-deficient tumors lack this anti-ferroptotic mechanism, unleashing the generation of lipid peroxidation and potent ferroptotic cell death induced by erastin, RSL3, cysteine deprivation, radiotherapy, and immunotherapy. In summary, patient-derived organoids of colorectal cancer patients for screening ferroptosis-sensitive tumors are established, providing a paradigm for identifying that patient-derived tumors are sensitive to ferroptosis-inducing therapies. This study concludes that mitophagy-deficient tumors are vulnerable to ferroptosis induction, which may lead to the development of new therapeutic strategies for tumors deficient in mitophagy.
Journal
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ATF4 (Activating Transcription Factor 4)
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erastin • RSL3
4d
Unlocking the Potential of Traditional Chinese Medicine (TCM): Shipi Xiaoji Formula (SPXJF) as a Novel Ferroptosis Inducer in Hepatocellular Carcinoma. (PubMed, J Ethnopharmacol)
SPXJF exerts anti-tumor effects on HCC cells by inducing ferroptosis, and its mechanism of action involves the regulation of ferroptosis-related genes and proteins. This study provides a theoretical basis for the clinical treatment of HCC and the development of new anti-cancer drugs, offering a valuable contribution to the field of ethnopharmacology.
Journal
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AURKA (Aurora kinase A) • GPX4 (Glutathione Peroxidase 4) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4) • NOX4 (NADPH Oxidase 4) • CDC25A (Cell Division Cycle 25A) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1) • LPCAT3 (Lysophosphatidylcholine Acyltransferase 3)
7d
Dysregulation of Iron Homeostasis Mediated by FTH Increases Ferroptosis Sensitivity in TP53-Mutant Glioblastoma. (PubMed, Neurosci Bull)
Interestingly, we found that Erastin combined with FAC treatment significantly increased ferroptosis. These findings provide new insights for drug development and therapeutic modalities for GBM patients with TP53 mutations from iron metabolism perspectives.
Journal
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TP53 (Tumor protein P53) • UBR5 (Ubiquitin Protein Ligase E3 Component N-Recognin 5)
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TP53 mutation
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erastin
9d
Bone Marrow Stromal Cells Protect Myeloma Cells from Ferroptosis through GPX4 deSUMOylation. (PubMed, Cancer Lett)
Using the NOD-scid IL2Rgammanull (NSG) mouse based xenograft model and intra-bone MM growth model, we validated that target SENP3 enhanced the killing effect of GPX4 inhibitor RSL3, thereby reduced tumor burden, prolonged survival of mice, and alleviated bone disruption of mice bearing MM tumors. Our study deciphers the mechanism of BMSCs preventing MM cells from spontaneous ferroptosis, and clarifies the therapeutic potential of non-apoptosis strategies in managing refractory or relapsed MM patients.
Journal • IO biomarker • Stroma
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SDC1 (Syndecan 1) • GPX4 (Glutathione Peroxidase 4) • CD40LG (CD40 ligand)
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RSL3
10d
Tumor microenvironment-regulated nanoplatform for enhanced chemotherapy, cuproptosis and nonferrous ferroptosis combined cancer therapy. (PubMed, J Mater Chem B)
Herein, a versatile nanoplatform, CeO2@CuO2@DOX-RSL3@HA (CCDRH), was initially constructed for promoting the antitumor efficiency via regulation of the TME...The experimental results revealed that CCDRH exhibited high performance in tumor inhibition, which is attributed to the combined effect of enhanced chemotherapy, ferroptosis and cuproptosis. The study provides a new approach for improving anticancer efficiency via regulation of the TME.
Journal
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GPX4 (Glutathione Peroxidase 4) • DLAT (Dihydrolipoamide S-Acetyltransferase)
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GPX4 expression
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RSL3
10d
Ferroptosis and Intrinsic Drug-induced Liver Injury by Acetaminophen and Other Drugs: A Critical Evaluation and Historical Perspective. (PubMed, J Clin Transl Hepatol)
More recently, ferroptosis-a novel, non-apoptotic form of cell death-was identified in NRAS-mutant HT-1080 fibrosarcoma cells exposed to erastin and other NRLs...Overall, the published data support the idea that multi-layered endogenous antioxidant defense mechanisms in the liver limit the occurrence of pathophysiologically relevant LPO under normal conditions. Only when these defense mechanisms are severely compromised does ferroptosis become a significant mode of drug-induced cell death.
Review • Journal
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GPX4 (Glutathione Peroxidase 4)
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NRAS mutation
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methotrexate • erastin • rifampicin
11d
Lithium Enhances Ferroptosis Sensitivity in Melanoma Cells and Promotes CD8+ T Cell Infiltration and Differentiation. (PubMed, Free Radic Biol Med)
We found that lithium significantly enhanced RSL3-induced ferroptosis in vitro, evidenced by increased mitochondrial peroxide, lipid peroxidation, and mitochondrial abnormalities...Additionally, this combination enhanced CD8+ T cell infiltration and IFN-γ expression in the tumor microenvironment, especially among cytotoxic effector CD8+ T cells. These findings reveal the pro-ferroptotic and immune regulation roles of lithium, broaden our understanding of its biological roles, and propose new strategies for ferroptosis-targeted therapies in melanoma.
Journal
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CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • FTH1 (Ferritin Heavy Chain 1)
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IFNG expression
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RSL3
16d
Inhibition of Oxidative Stress-Induced Ferroptosis Can Alleviate Rheumatoid Arthritis in Human. (PubMed, J Immunol Res)
In cell experiments, erastin or fer-1 regulated the invasion of human synovial fibroblast cells, mitochondrial membrane potential, reactive oxygen species (ROS) expression, marker protein, and so on...There is a nonlinear relationship between human disease manifestations and animal model pathology. Ferroptosis regulating in RA for humans or animals may produce different effects.
Journal
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KEAP1 (Kelch Like ECH Associated Protein 1) • TNFA (Tumor Necrosis Factor-Alpha) • GPX4 (Glutathione Peroxidase 4)
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ROS1 expression
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erastin
16d
Ferroptosis inducer Erastin inhibits proliferation of liver cancer cells in vitro by downregulating ACSL4 (PubMed, Nan Fang Yi Ke Da Xue Xue Bao)
ACSL4 level is significantly overexpressed in liver cancer. Erastin increases MDA contents and down-regulates ACSL4 expression, thereby promoting ferroptosis and inhibiting proliferation of liver cancer cells, and these effects can be reversed by Fer-1.
Preclinical • Journal
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ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4) • PCNA (Proliferating cell nuclear antigen)
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PCNA expression
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erastin
17d
Impact of selenium content in fetal bovine serum on ferroptosis susceptibility and selenoprotein expression in cultured cells. (PubMed, J Toxicol Sci)
Cells cultured in FBS containing higher selenium concentrations exhibited elevated GPx4 expression, and were resistant to ferroptosis induced by erastin and RSL3. These findings suggest that the variability of selenium content in different FBS batches can significantly influence the susceptibility of cells to ferroptosis, highlighting the importance of standardizing these factors to enhance the reproducibility of ferroptosis-related experiments.
Journal
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GPX4 (Glutathione Peroxidase 4)
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GPX4 expression
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erastin • RSL3
21d
Computational Discovery of Novel GPX4 Inhibitors from Herbal Sources as Potential Ferroptosis Inducers in Cancer Therapy. (PubMed, Arch Biochem Biophys)
The computed binding free energies for RSL3, isochondrodendrine, hinokiflavone, irinotecan and ginkgetin were -80.12, -107.31, -132.03, and -137.52 and -91.11 kJ/mol, respectively, indicating their significantly higher inhibitory effects compared to RSL3. These findings highlight the potential for developing novel GPX4 inhibitors to promote ferroptosis, warranting further experimental validation.
Journal
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GPX4 (Glutathione Peroxidase 4)
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irinotecan • RSL3
21d
Therapeutic induction of ferroptosis in tumors using PD-L1 targeting antibody nanogel conjugates. (PubMed, Cell Chem Biol)
Here, we report that tumor cells that express PD-L1 are sensitive to ferroptosis inducers such as imidazole ketone erastin (IKE)...This ANC targets PD-L1-expressing cells in vitro and in vivo and induces ferroptosis, resulting in tumor suppression. Importantly, this approach is superior to systemic administration of IKE because it enables enhanced delivery of IKE specifically to tumor cells and it requires lower drug doses for efficacy.
Journal • PD(L)-1 Biomarker • IO biomarker
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SLC7A11 (Solute Carrier Family 7 Member 11)
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PD-L1 expression • SLC7A11 expression
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erastin
21d
Sulfasalazine-loaded nanoframes: A new frontier in bladder cancer therapy through ferroptosis induction. (PubMed, Colloids Surf B Biointerfaces)
The expeditious reduction of GSH markedly stimulates the accumulation of lipid peroxides (LPO) and suppresses glutathione peroxidase 4 (GPX4), consequently triggering ferroptosis in bladder cancer cells and inhibiting the migration ability of bladder cancer cells effectively. This research contributes to a more profound comprehension of nano-drug-biological interactions and provides a prospective outlook on treating bladder cancer by instigating ferroptosis in tumor cells through GSH depletion.
Journal
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GPX4 (Glutathione Peroxidase 4)
21d
Loss of peroxiredoxin 6 (PRDX6) alters lipid composition and distribution resulting in increased sensitivity to ferroptosis. (PubMed, Biochem J)
Loss of PRDX6 resulted in increased sensitivity to erastin-induced ferroptosis, independent of selenium and GPX4, as a consequence of increased levels of lipid hydroperoxides, that reverted to normal levels upon rescue with PRDX6. The results presented demonstrate that all three enzymatic activities of PRDX6 contribute to the role of this multifunctional enzyme in diverse cellular processes, including membrane phospholipid remodeling and glycerophospholipid functional diversity, resulting in altered lipid peroxides and modulation of AA disposition and traffic. These contributions highlight the complexity of the changes that loss of PRDX6 exerts on cell functionality..
Journal
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GPX4 (Glutathione Peroxidase 4)
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erastin
21d
BRIP1 Induced Ferroptosis to Inhibit Glioma Cells and was Associated with Increased Oxidative Stress. (PubMed, Discov Med)
In this study, we found that down-regulation of BRIP1 could inhibit cell viability and proliferation in glioma cells through the induction of ferroptosis. This process was associated with increased oxidative stress, which was mediated by the down-regulation of SLC7A11 (xCT (Cysteine/glutamate transporter)) expression.
Journal • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • SLC3A2 (Solute Carrier Family 3 Member 2) • GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11)
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SLC7A11 expression
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erastin • chloroquine phosphate
22d
Etomoxir Sodium Salt Promotes Imidazole Ketone Erastin-Induced Myeloid-Derived Suppressor Cell Ferroptosis and Enhances Cancer Therapy. (PubMed, Biology (Basel))
Interestingly, the combination treatment of Eto and IKE blocked MDSCs' immunosuppressive function and accumulation by downregulating the expression of SLC7A11, GPX4, and ARG1 while promoting T-cell proliferation and infiltration into tumor tissues to enhance cancer therapy. These data provide a rationale for the combination therapy of a specific CPT1A inhibitor, Eto, with IKE in clinical settings.
Journal
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GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11) • CPT1A (Carnitine Palmitoyltransferase 1A)
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SLC7A11 expression
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erastin • etomoxir (MIQ-001)
22d
Iberverin Downregulates GPX4 and SLC7A11 to Induce Ferroptotic Cell Death in Hepatocellular Carcinoma Cells. (PubMed, Biomolecules)
In this study, we proved that iberverin can induce intracellular reactive oxygen species (ROS) generation to inhibit cell proliferation and initiate ferroptotic cell death in HCC cells, which can be eradicated by the ferroptosis inhibitor ferrostatin-1 (Fer-1) or deferoxamine mesylate (DFO) and ROS scavenger (GSH or NAC). Significantly, a low dose of iberverin can remarkably increase the sensitivity of HCC cells to ferroptosis induced by canonical ferroptosis inducers RSL3 and imidazole ketone erastin (IKE). This study uncovers a critical function of iberverin in preventing HCC through ferroptosis and provides a promising strategy for HCC treatment either via iberverin alone or in combination with canonical ferroptosis inducers in the future.
Journal
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GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11)
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erastin • RSL3
24d
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma. (PubMed, J Immunother Cancer)
Taken together, our findings suggest that propafenone holds promise as a candidate drug for enhancing the efficacy of immunotherapy and other ferroptosis-targeted therapies in the treatment of melanoma.
Journal
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HMOX1 (Heme Oxygenase 1) • GPX4 (Glutathione Peroxidase 4)
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RSL3
24d
MAZ regulates ferroptosis, apoptosis and differentiation of oligodendrocyte precursor cells. (PubMed, Brain Res)
We also evaluated the susceptibility of MAZ-overexpressing OPCs to ferroptosis inducer, erastin, and demonstrated that MAZ-overexpressing OPCs were resistant to erastin-induced ferroptosis...Moreover, we elucidate the mechanism responsible for MAZ's protective effects on OPC death and differentiation, which may be achieved through transcriptional activation of SOX2. Our findings introduced MAZ as a beneficial modulator of OPC survival and differentiation, and it could serve as a potential therapeutic target for demyelination diseases.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • SOX2
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MYC expression
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erastin
24d
RSL3 sensitizes glioma cells to ionizing radiation by suppressing TGM2-dependent DNA damage repair and epithelial-mesenchymal transition. (PubMed, Redox Biol)
Furthermore, in mice bearing human U87 tumor xenografts, RSL3 administration synergized with IR to inhibit tumor growth, accompanied by TGM2 inhibition, DNA DSBs, and EMT inhibition in tumor tissues. Taken together, we demonstrated that RSL3 sensitizes glioma cells to IR by suppressing TGM2-mediated DNA repair and EMT.
Journal
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GSTP1 (Glutathione S-transferase pi 1) • GPX4 (Glutathione Peroxidase 4) • TGM2 (Transglutaminase 2)
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TGM2 overexpression • TGM2 expression
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RSL3
27d
Discovery of Dual CDK6/BRD4 Inhibitor Inducing Apoptosis and Increasing the Sensitivity of Ferroptosis in Triple-Negative Breast Cancer. (PubMed, J Med Chem)
BC13 demonstrates profound synergistic antitumor effects with ferroptosis inducer in TNBC cells. Therefore, BC13 is a novel dual inhibitor of CDK6/BRD4 for the treatment of TNBC either as a single agent or in combination with RSL3.
Journal
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CDK6 (Cyclin-dependent kinase 6) • BRD4 (Bromodomain Containing 4)
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RSL3
28d
Cascade Bilateral Regulation of Ferroptosis and Immune Activation Conducted by the Electron-Accepting-Inspired Glycopolymer-Based Nanoreactor. (PubMed, ACS Appl Mater Interfaces)
By taking advantage of the sensitivity difference between tumor cells and dendritic cells (DCs) to the ferroptosis inducer erastin (Er) based on varying xCT expression levels, we developed Er-loaded nanoparticles CNP/Er. These nanoparticles not only enhance ferroptosis in 4T1 cells through Gpx4 inhibition by CNP but also promote DC maturation by utilizing CNP's hypoxia-responsive mechanism to increase ROS levels. The CNP/Er was believed to be an ideal candidate for bilateral regulation of ferroptosis and immune activation in one nanoreactor.
Journal
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GPX4 (Glutathione Peroxidase 4)
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erastin
28d
A potent and selective anti-glutathione peroxidase 4 nanobody as a ferroptosis inducer. (PubMed, Chem Sci)
The new GPX4-inhibiting nanobody described here exhibits superior proteome-wide selectivity and a vastly improved safety profile compared to existing GPX4 inhibitors. These incredible features of 12E, as an anti-GPX4 nanobody, may not only contribute to ferroptosis-related anticancer treatment but also establish a new paradigm for nanobodies in drug development for traditionally undruggable targets.
Journal
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GPX4 (Glutathione Peroxidase 4)
28d
Receptor accessory protein 6, a novel ferroptosis suppressor, drives oral squamous cell carcinoma by maintaining endoplasmic reticulum hemostasis. (PubMed, Int J Biol Macromol)
Moreover, REEP6 overexpression conferred resistance to RSL3, a ferroptosis inducer, whereas REEP6 knockdown sensitized OSCC cells to RSL3...In addition, we identified promoter DNA hypomethylation as the underlying cause of REEP6 overexpression in OSCC. Taken together, REEP6 acts as a novel suppressor of ferroptosis, with its overexpression driven by promoter hypomethylation contributing to OSCC progression by ER stress-mediated ferroptosis via ACSL4.
Journal
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ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
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RSL3
30d
Engineered nanoplatform mediated gas therapy enhanced ferroptosis for tumor therapy in vivo. (PubMed, Bioact Mater)
Additionally, Erastin depletes GSH by inhibiting the cystine/glutamate antiporter system, reducing cystine uptake and impairing GPX4, while also increasing intracellular H2O2 levels by activating NOX4 protein expression...Furthermore, this nanoplatform significantly inhibited tumor cell growth and extended the survival time of tumor-bearing mice in vivo. This engineered nanoplatform, which enhances ferroptosis through gas therapy, shows significant promise for ferroptosis-based cancer therapy and offers potential strategies for clinical tumor treatment.
Preclinical • Journal
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GPX4 (Glutathione Peroxidase 4) • NOX4 (NADPH Oxidase 4)
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erastin
1m
Sialic Acid-Targeted Ru(II)/Ir(III)/Re(I) Complexes for Ferroptosis Induction in Triple-Negative Breast Cancer. (PubMed, Langmuir)
Moreover, the complex [LIrcIrh] exhibited mitochondrial dysfunction and membrane damage (diminished MMP, ΔΨm) through the production of copious reactive oxygen species (ROS) in MDA-MB-231 cells upon considerable accumulation in mitochondria (Pearson's coefficient = 0.842). The analysis of the field emission scanning electron microscopy (FE-SEM) image has marked the vivid membrane damage induced by the complex [LIrcIrh], exhibiting ablaze evidence for the destruction of TNBC cells through ferroptosis.
Journal
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GPX4 (Glutathione Peroxidase 4)
1m
CKS2 induces autophagy-mediated glutathione metabolic reprogramming to facilitate ferroptosis resistance in colon cancer. (PubMed, Mol Med)
CKS2 suppresses ferroptosis in CC by modulating GSH metabolism in both in vitro and in vivo settings. These findings offer new insights into targeting CKS2 for CC treatment and shed light on the mechanism of ferroptosis in CC.
Journal
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GPX4 (Glutathione Peroxidase 4) • CKS2 (CDC28 Protein Kinase Regulatory Subunit 2)
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GPX4 expression
|
sorafenib • erastin
1m
The Role of STEAP3 in Pathogenesis of Gliomas: An Independent Prognostic Factor and Regulator of Ferroptosis. (PubMed, Ann Clin Lab Sci)
STEAP3 serves as an independent biomarker for glioma prognosis with significant diagnostic value. High STEAP3 expression was correlated with poor overall outcomes of glioma patients. Knockdown of STEAP3 significantly suppressed the proliferation of glioma cells and increased erastin-induced ferroptosis via Nrf2/GPX4 pathway.
Journal
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GPX4 (Glutathione Peroxidase 4) • STEAP1 (STEAP Family Member 1) • STEAP3 (STEAP3 Metalloreductase)
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erastin
1m
TMOD3 accelerated resistance to immunotherapy in KRAS-mutated pancreatic cancer through promoting autophagy-dependent degradation of ASCL4. (PubMed, Drug Resist Updat)
Mechanistically, TMOD3 promoted F-actin polymerization, thereby facilitating the fusion of autophagosomes with lysosomes, increasing the degradation of the ACSL4 protein, and augmenting the ferroptosis-inducing effects of RSL3...Cangrelor, an FDA-approved drug, can target TMOD3...In conclusion, TMOD3 was found to inhibit ferroptosis and induced the resistance to PD-1 antibody by facilitating the fusion of autophagosomes and lysosomes through the promotion of F-actin polymerization in KRAS-mutant PC. TMOD3 was identified as a novel target for PC therapy.
Journal • PD(L)-1 Biomarker • IO biomarker
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KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
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KRAS mutation • KRAS wild-type • RAS wild-type • KRAS expression
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RSL3
1m
LncRNA MALAT1 promotes Erastin-induced ferroptosis in the HBV-infected diffuse large B-cell lymphoma. (PubMed, Cell Death Dis)
Together, our study identified HBX's role in inhibiting MALAT1 expression, promoting SFPQ-mediated splicing of SLC7A11 pre-mRNA, and reducing the GCB-type DLBCL sensitivity to Erastin-induced ferroptosis. Combined with the recent studies that ferroptosis may be involved in the occurrence and development of DLBCL, these findings explain our clinical data analysis that DLBCL patients with low expression of MALAT1 have poorer prognosis and shorter overall survival, and provide a valuable therapeutic target for the HBV-infected GCB-type DLBCL patients.
Journal
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MALAT1 (Metastasis associated lung adenocarcinoma transcript 1) • SLC7A11 (Solute Carrier Family 7 Member 11)
|
erastin
1m
Cytoglobin augments ferroptosis through autophagic degradation of ferritin in colorectal cancer cells. (PubMed, Mol Cell Biochem)
The autophagy inhibitor bafilomycin or chloroquine alleviated autophagy-dependent degradation of ferritin protein under RSL3 treated condition. Additionally, a colocalization of CYGB with the transferrin receptor (TFR) was confirmed. Our results demonstrate an important functional pathway by which CYGB regulates ferroptosis through TFR-binding and autophagic degradation of ferritin, and provide a potential pathway for the treatment of colorectal cancer.
Journal
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NCOA4 (Nuclear Receptor Coactivator 4) • LAMP1 (Lysosomal Associated Membrane Protein 1)
|
RSL3 • chloroquine phosphate
1m
Rbbp6-Mediated Bmal1 Ubiquitination Inhibits YAP1 Signaling Pathway to Promote Ferroptosis in Diabetes-Induced Testicular Damage. (PubMed, Diabetes Metab J)
In addition, knockdown of YAP1 or treatment with ferroptosis inducer erastin blocked the above effects caused by Bmal1 overexpression. Rbbp6-mediated Bmal1 ubiquitination suppressed YAP1 pathway, promoting ferroptosis in DITD. This study highlighted Rbbp6/Bmal1/YAP1 axis as a potential therapeutic target for mitigating DITD.
Journal
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YAP1 (Yes associated protein 1) • GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11) • ARNTL (Aryl Hydrocarbon Receptor Nuclear Translocator Like)
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erastin
1m
In situ endoscopic photodynamic therapy combined with immature DC vaccination induces a robust T cell response against peritoneal carcinomatosis. (PubMed, J Immunother Cancer)
The combination of in situ PDT locally delivered by an endoscope light and iDC administration induces a durable memory immune response against peritoneal carcinomatosis thereby opening new perspectives for the treatment of a life-threatening condition.
Journal
|
CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • CD4 (CD4 Molecule)
|
RSL3
2ms
Rituximab induces ferroptosis and RSL3 overcomes rituximab resistance in diffuse large B-cell lymphoma cells. (PubMed, Arch Biochem Biophys)
Currently, the first-line treatment regimen for DLBCL is still rituximab plus cyclophosphamide, doxorubicin, vincristine, and prednisolone (R-CHOP), which significantly improves outcomes for DLBCL patients. In conclusion, we report for the first time that rituximab induces ferroptosis in lymphoma cells, at least partially through the SLC7A11/GPX4 axis. We also identify targeting ferroptosis as a promising therapeutic option for both sensitive cells and resistant cells in the treatment of DLBCL.
Journal
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GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11)
|
Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • vincristine • RSL3
2ms
Emerging insights into ferroptosis in cholangiocarcinoma (Review). (PubMed, Oncol Lett)
Inhibitors of ferroptosis include ferrostatin-1, liproxstatin-1, vitamin E and coenzyme Q10. By contrast, compounds such as erastin, RSL3 and FIN56 have been identified as inducers of ferroptosis...The present review focused on molecular targets such as p53 and ACSL4, the process of targeted medications in combination with PDT in CCA and the pathways of lipid peroxidation, the Xc-system and GSH-GPX4 in ferroptosis. The present review thus offered novel perspectives to improve the current understanding of CCA.
Review • Journal
|
GPX4 (Glutathione Peroxidase 4) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
|
erastin • RSL3 • liproxstatin-1
2ms
(-)-Epicatechin regulates endoplasmic reticulum stress and promotes ferroptosis in lung cancer cells via the PERK/eIF2α/ATF4 signaling pathway. (PubMed, PLoS One)
EC therapy activates the PERK-eIF2α-ATF4 signaling pathway to increase ER stress, thereby promoting ferroptosis in lung cancer cells and inhibiting the occurrence and development of lung cancer. Our research suggests that EC may become a drug candidate for treating lung cancer.
Journal
|
ATF4 (Activating Transcription Factor 4)
|
erastin
2ms
Effects of ATG5 and ATG7 Knockout on Ferroptosis Sensitivity of RPMI-8226 Cells (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
Knockout of ATG5 and ATG7 genes can inhibit the ferroptosis of MM cells, and LAP pathway may be involved in the regulation.
Journal
|
ATG5 (Autophagy Related 5) • ATG7 (Autophagy Related 7)
|
RSL3
2ms
Study on the Synergistic Mechanism of Photodynamic Therapy Combined With Ferroptosis Inducer to Induce Ferroptosis in Cholangiocarcinoma. (PubMed, Lasers Surg Med)
Our findings suggest that Erastin or Lenvatinib can enhance the induction of ferroptosis in cholangiocarcinoma cells by photodynamic therapy by increasing intracellular ROS and inhibiting intracellular antioxidant pathways.
Journal
|
GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11) • AIFM2 (Apoptosis Inducing Factor Mitochondria Associated 2)
|
GPX4 expression • SLC7A11 expression
|
Lenvima (lenvatinib) • erastin
2ms
Ginsenoside Rg3 activates the immune function of CD8+ T cells via circFOXP1-miR-4477a-PD-L1 axis to induce ferroptosis in gallbladder cancer. (PubMed, Arch Pharm Res)
Ferroptosis inhibitor Fer-1 administration could reverse the beneficial effects caused by Rg3 treatment while ferroptosis inducer Erastin treatment enhanced the effects...Rg3 inactivated the circFOXP1-miR-4477a-PD-L1 signaling axis to activate the immune function of CD8+ T cells, thereby inducing ferroptosis and apoptosis in GBC cells. This research recognizes the mechanism of Rg3-mediated anti-cancer effect and offers evidence for the potentiality of Rg3 in clinical application for GBC therapy.
Journal • PD(L)-1 Biomarker • IO biomarker
|
CD8 (cluster of differentiation 8)
|
PD-L1 overexpression
|
erastin
2ms
EIF2S1 Silencing Impedes Neuroblastoma Development Through GPX4 Inactivation and Ferroptosis Induction. (PubMed, Int J Genomics)
Our findings indicate that EIF2S1 appears to facilitate the progression of NB by protecting tumor cells from ferroptosis through modulating GPX4 and SLC7A11 expression. Consequently, EIF2S1 may serve as a potential therapeutic target for the management of NB.
Journal
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GPX4 (Glutathione Peroxidase 4) • SLC7A11 (Solute Carrier Family 7 Member 11) • EIF2S1 (Eukaryotic Translation Initiation Factor 2 Subunit Alpha)
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SLC7A11 expression
2ms
PRMT4 Reduced Erastin-Induced Ferroptosis in Nasopharyngeal Carcinoma Cisplatin-Resistant Cells by Nrf2/GPX4 Pathway. (PubMed, J Environ Pathol Toxicol Oncol)
Methylation increased PRMT4 DNA stability. Collectively, our data reveal that PRMT4 reduced erastin-induced ferroptosis in NPC cisplatin-resistant cells by Nrf2/GPX4 pathway, suggesting that targeting PRMT4 may present as a potential strategy against the development of NPC.
Journal
|
GPX4 (Glutathione Peroxidase 4)
|
cisplatin • erastin