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DRUG CLASS:

NRF2 activator

5d
PRMT5 inhibition sensitizes B-cell lymphoma cells to ferroptosis. (PubMed, Leukemia)
Notably, combined treatment with the PRMT5 inhibitor GSK3326595 and DMF synergistically enhances anti-tumor activity in a patient-derived xenograft (PDX) model. These findings reveal a previously unrecognized PRMT5-ATF5-SLC7A11 axis that drives ferroptosis resistance in B-cell lymphomas and provide a strong rationale for targeting PRMT5 to potentiate ferroptosis-based therapies in relapsed or refractory disease.
Journal
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PRMT5 (Protein Arginine Methyltransferase 5) • SLC7A11 (Solute Carrier Family 7 Member 11) • ATF4 (Activating Transcription Factor 4)
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pemrametostat (GSK3326595)
26d
Phase IIb Clinical Trial for the Efficacy and Safety by CU01-1001 for 24 Weeks in Type 2 DM Patients With Albuminuria (clinicaltrials.gov)
P2, N=240, Completed, Curacle Co., Ltd. | Recruiting --> Completed | Phase classification: P2b --> P2 | Trial completion date: Sep 2024 --> Nov 2025 | Trial primary completion date: Sep 2024 --> Nov 2025
Trial completion • Phase classification • Trial completion date • Trial primary completion date
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dimethyl fumarate (CU01)
27d
RRx-001 inhibits G6PD to deplete NADPH and trigger disulfidptosis coupled with DAMP-mediated immunogenic cell death in hepatocellular carcinoma. (PubMed, Cell Death Discov)
In vivo, RRx-001 significantly inhibits tumor growth, enhances T-cell infiltration, promotes M1 macrophage polarization, downregulates PD-L1 expression, and strengthens anti-tumor immunity through T cell-related pathways. With both metabolic and immunomodulatory effects, RRx-001 provides a basis for novel HCC therapies, and future research could explore its synergistic effects with immune checkpoint inhibitors.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • HMGB1 (High Mobility Group Box 1) • G6PD (Glucose-6-Phosphate Dehydrogenase)
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PD-L1 expression
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nibrozetone (RRx-001)
28d
Dimethyl fumarate combined with cisplatin at subcytotoxic doses sensitizes cervical cancer toward ferroptosis and apoptosis through GSH restriction and p53 (re)activation. (PubMed, Mol Oncol)
We found a p53-mediated downregulation of the Solute Carrier Family 7 Member 11 (SLC7A11)/Cystine/Glutamate Transporter (xCT) expression and glutathione levels. Our results suggest that combined administration of DMF and cisplatin, by targeting the dependency of cervical cancer cells on glutathione and (re)activating p53, represents a promising anticancer therapeutic strategy.
Journal
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SLC7A11 (Solute Carrier Family 7 Member 11)
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cisplatin
1m
4‑Acetylantrocamol LT3 suppresses colorectal cancer growth and metastasis via PI3K/AKT and MAPK pathway modulation. (PubMed, Int J Mol Med)
Molecular docking confirmed that LT4 stably occupied the ATP‑binding pocket of PI3Kγ with a binding energy comparable to wortmannin and a conformation similar to antroquinonol. In conclusion, to the best of our knowledge, the present study is the first to comprehensively demonstrate the multi‑target anti‑CRC effects of LT4, highlighting its potential as a therapeutic agent, especially in KRAS‑mutant CRC.
Journal
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KRAS (KRAS proto-oncogene GTPase) • BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • BCL2L1 (BCL2-like 1) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • SLC3A2 (Solute Carrier Family 3 Member 2) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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KRAS mutation
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Hocena (antroquinonol)
1m
Small molecule screening identifies cytotoxic endoplasmic reticulum-associated degradation inhibitors in multiple myeloma. (PubMed, Cell Death Dis)
Notably, ERAD inhibition by RTA408 is cytotoxic to primary malignant plasma cells, including those resistant to proteasome inhibitors, and demonstrates in vivo anti-myeloma activity. Our findings establish a novel ERAD inhibitor, which is a valuable tool to dissect ERAD biology, and provide pre-clinical evidence for RTA408 as a therapeutic agent in MM.
Journal
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CASP8 (Caspase 8)
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Skyclarys (omaveloxolone)
1m
Enrollment change
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IFNB1 (Interferon Beta 1)
2ms
Clinical Study for Dimethyl Fumarate in Preserving Islet β-Cell Function in Type 1 Diabetes Mellitus (clinicaltrials.gov)
P3, N=90, Recruiting, Nanjing Medical University | Not yet recruiting --> Recruiting
Enrollment open
2ms
Dimethyl fumarate and mitochondrial physiology: implications for neurological disorders. (PubMed, Front Pharmacol)
In conclusion, DMF exerts multifaceted and cell type-specific actions on mitochondria. Understanding these mechanisms may guide optimized therapeutic strategies and the identification of biomarkers for precision use in neurological disorders.
Review • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • NQO1 (NAD(P)H dehydrogenase, quinone 1) • NRF1 (Nuclear Respiratory Factor 1) • TFAM (Transcription Factor A, Mitochondrial)
2ms
Aflatoxin and Liver Cancer in China: The Evolving Research Landscape. (PubMed, Toxins (Basel))
Chemoprevention and dietary interception studies (e.g., oltipraz, chlorophyllin, and broccoli sprout beverages) showed that enhancing detoxication pathways can lower biomarker burdens in exposed populations...Nevertheless, regional heterogeneity, multi-mycotoxin co-exposure, and climate variability are expected to increase exposure volatility and complicate surveillance. Here, we translate and synthesize the Chinese evidence base, highlight biomarker-enabled monitoring and policy evaluation, and propose an integrated "5+1" prevention framework spanning source control, process detoxification, tiered governance, short-course interception, precision follow-up of high-risk individuals, and climate-sensitive early warning along the climate-agriculture-storage-processing-population (CAT-CSPP) chain.
Review • Journal
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TP53 (Tumor protein P53)