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DRUG CLASS:

DNA synthesis inhibitor

Related drugs:
22h
Tumor-derived apolipoprotein E confers resistance to temozolomide in pancreatic neuroendocrine tumors. (PubMed, Cell Death Dis)
This study reveals a new functional role of APOE that leads to chemoresistance in patient treatment. Our findings suggest the potential of combined administration of BLT-1 to overcome TMZ chemoresistance and improve treatments for patients with pNETs.
Journal • BRCA Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • APOE (Apolipoprotein E)
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temozolomide
22h
Exosomal SNHG26 mediates immunosuppression by impairing NK cells in tongue cancer. (PubMed, NPJ Precis Oncol)
SNHG26 depletion reversed NK cell suppression and cisplatin resistance in vitro and in vivo. Thus, our study identifies exosomal SNHG26 as a key mediator of cisplatin resistance and NK cell dysfunction in TSCC, suggesting its potential as a promising therapeutic target.
Journal
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IL2 (Interleukin 2) • SOX2 • HLA-DRA (Major Histocompatibility Complex, Class II, DR Alpha) • TGFB1 (Transforming Growth Factor Beta 1) • WWP2 (WW Domain Containing E3 Ubiquitin Protein Ligase 2)
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cisplatin
22h
Pachymic acid suppresses proliferation and invasion in colon cancer by inhibiting glycolysis via PPARγ/ENO1 pathway. (PubMed, Chem Biol Interact)
The present study confirmed that pachymic acid played an inhibitory role in the proliferation and invasion of colon cancer by intervening in the process of glycolysis. PPARγ was identified as the primary target of pachymic acid in regulating the glucose metabolism in colon cancer.
Journal
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LDHA (Lactate dehydrogenase A) • ENO1 (Enolase 1) • PPARG (Peroxisome Proliferator Activated Receptor Gamma) • PGK1 (Phosphoglycerate Kinase 1) • SLC2A1 (Solute Carrier Family 2 Member 1)
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oxaliplatin
22h
NQO1-responsive Trimethyl lock benzoquinone: A cleavable linker strategy for antibody-drug conjugates. (PubMed, J Control Release)
In vivo, NRTL-24 demonstrated superior tumor-targeting ability, significantly prolonging median survival compared to untreated and temozolomide-treated groups while maintaining favorable safety. This NQO1-responsive linker technology enables precise payload activation in tumor while minimizing off-target effects, establishing NRTL-24 as a promising therapeutic candidate. The strategy provides a blueprint for enzyme-targeted ADC development through tumor- selective linker design.
Journal
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EGFR (Epidermal growth factor receptor) • NQO1 (NAD(P)H dehydrogenase, quinone 1)
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temozolomide
1d
Neuroinflammatory Mechanisms and Therapeutic Targets in Oxaliplatin-Induced Peripheral Neuropathy: a Comprehensive Review. (PubMed, Neurotox Res)
Various pharmacological and plant-derived compounds, such as naringin, baicalein, and puerarin, as well as selective inhibitors of inflammatory pathways, have shown promising neuroprotective effects in animal models by attenuating inflammatory responses and alleviating neuropathic symptoms. By synthesizing these converging lines of evidence, this review further outlines potential future directions, including the development of combination therapies targeting multiple inflammatory pathways, microbiome-based interventions, and the translation of preclinical findings into well-designed clinical trials.
Review • Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1) • TLR4 (Toll Like Receptor 4)
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oxaliplatin
1d
Tumor-stromal crosstalk and macrophage enrichment are associated with chemotherapy response in bladder cancer. (PubMed, FEBS Open Bio)
Gemcitabine/Cisplatin (Gem/Cis) chemotherapy is a standard treatment for muscle-invasive bladder cancer (MIBC) but yields suboptimal response rates. Using TCGA bladder cancer data, the transcriptomic gene set was further validated revealing a prognostic signature associated with patients' outcome. These findings uncover a novel mechanism of chemotherapy resistance in bladder cancer driven by tumor-stromal interactions and macrophage recruitment and suggest that targeting macrophage infiltration may improve chemotherapy response in bladder cancer.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • PD-L2 (Programmed Cell Death 1 Ligand 2) • SPP1 (Secreted Phosphoprotein 1) • CXCL1 (Chemokine (C-X-C motif) ligand 1)
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cisplatin • gemcitabine
1d
Dual-targeted bacterial outer membrane vesicles enhance glioblastoma immunotherapy by regulating tumor microenvironment and inducing IFN-γ-mediated ferroptosis. (PubMed, J Nanobiotechnology)
Furthermore, IFN-γ facilitates erastin- and RSL-3-induced ferroptosis of tumor cells, particularly in temozolomide (TMZ)-resistant cells. Additionally, OMV-C-C@RSL-3 synergistically suppresses GBM growth in vivo. Thus, biosynthetically engineered OMV-C-C integrates intrinsic immunomodulatory activity with ferroptosis enhancement to strengthen glioblastoma immunotherapies, offering a versatile platform to overcome limitations in brain tumor immunotherapy.
Journal • IO biomarker
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CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • GPX4 (Glutathione Peroxidase 4)
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temozolomide • erastin
1d
Uncovering functional divergence and cellular clusters with specific gene signatures in HNSCC clonal spheroids. (PubMed, Cell Commun Signal)
Hyperproliferative spheroids (HRPS) showed increased proliferation and tumorigenic potential, whereas hypoproliferative spheroids (HOPS) demonstrated enhanced migration and resistance to cisplatin and radiation...Notably, the gene expression profiles of Cluster 3 in the HOPS and Cluster 1 in the HRPS closely matched the expression patterns observed in the HNSCC-TCGA dataset. These clusters also displayed a high transcriptional correlation between patient tumors and their xenografts, reinforcing the clonal nature of HNSCC's genetic and functional diversity of HNSCC.
Journal • Gene Signature
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TOP2A (DNA topoisomerase 2-alpha) • AURKA (Aurora kinase A) • ALDH3A1 (Aldehyde Dehydrogenase 3 Family Member A1) • ANLN (Anillin Actin Binding Protein) • CKS2 (CDC28 Protein Kinase Regulatory Subunit 2)
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cisplatin
1d
Inflammasome activation contributes to cisplatin resistance in ovarian cancer. (PubMed, J Ovarian Res)
Our findings suggest that inflammasome activation and pyroptosis are mechanisms associated with ovarian cancer chemoresistance to CDDP, contributing to the devastating scenario of this disease. Targeting the NLRP1 and NLRP3 pathways could represent a promising strategy to improve OC treatment.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • ANXA5 (Annexin A5)
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cisplatin
2d
Enrollment closed
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gemcitabine • docetaxel
2d
Personalized chronotherapy in glioblastoma: integrating circadian profiling and PK-PD modelling to optimize temozolomide timing. (PubMed, NPJ Precis Oncol)
A mechanistic pharmacokinetic-pharmacodynamic model incorporating the clock network recapitulated experimental observations and enabled prediction of treatment timing. Our findings highlight the importance of timing in GBM therapy and propose combining circadian profiling with mathematical modeling to personalize GBM chronotherapy.
PK/PD data • Journal
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PER2 (Period Circadian Regulator 2) • ARNTL (Aryl Hydrocarbon Receptor Nuclear Translocator Like) • CLOCK (Clock Circadian Regulator) • NR1D1 (Nuclear Receptor Subfamily 1 Group D Member 1)
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temozolomide
2d
α-Conopeptide From Conus planorbis Inhibits Glioblastoma Stem Cells and Angiogenesis via Sonic Hedgehog and ADAMDEC1-FGF2-FGFR1 Loop Signaling Pathway. (PubMed, Chem Biodivers)
Additional chorioallantoic membrane (CAM) and brine shrimp lethality tests supported its potent bioactivity, with a lower LD50 (50.24 µg/mL) compared to temozolomide (125.82 µg/mL). These findings indicate that the α-conopeptide from C. planorbis possesses multi-target anticancer activity targeting via SHH and FGFR1 loop signaling pathway, structural stability, and superior cytotoxic potency against GBM, highlighting its potential as a novel marine-derived therapeutic agent.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • PTCH1 (Patched 1) • FGF2 (Fibroblast Growth Factor 2)
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temozolomide