ArticleBritish journal of cancer2017
Camptothecin suppresses NRF2-ARE activity and sensitises hepatocellular carcinoma cells to anticancer drugs.
Article in British journal of cancer, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 35 papers.
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35 citing papers in PubMed, 76 citations in OpenAlex.
- Mechanisms of resistance to trastuzumab deruxtecan in breast cancer elucidated by multi-omic molecular profiling.NPJ breast cancer · 2025Article
- The Unfolded Protein Response-Novel Mechanisms, Challenges, and Key Considerations for Therapeutic Intervention.Cancers · 2025Review
- Impact of proteostasis workload on sensitivity to proteasome inhibitors in multiple myeloma.Clinical and experimental medicine · 2025Review
- Redox-Sensitive Camptothecin Prodrug: A Promising Drug Delivery Strategy with Ultrahigh Drug Loading and Tunable Drug Release.Nano TransMed · 2025Article
- Engineered nanoparticles for imaging and targeted drug delivery in hepatocellular carcinoma.Experimental hematology & oncology · 2025Review
- Co-delivery of camptothecin and MiR-145 by lipid nanoparticles for MRI-visible targeted therapy of hepatocellular carcinoma.Journal of experimental & clinical cancer research : CR · 2024Article
- Article
- Identification of key molecules in the formation of portal vein tumor thrombus in hepatocellular carcinoma based on single cell transcriptomics andTranslational cancer research · 2024Article
- Camptothecin enhances the anti-tumor effect of low-dose apatinib combined with PD-1 inhibitor on hepatocellular carcinoma.Scientific reports · 2024Article
- Dual role of Nrf2 signaling in hepatocellular carcinoma: promoting development, immune evasion, and therapeutic challenges.Frontiers in immunology · 2024Review
- Immunohistochemical expression of NRF2 is correlated with the magnitude of inflammation and fibrosis in chronic liver disease.Cancer medicine · 2023Article
- Camptothecin Sensitizes Hepatocellular Carcinoma Cells to Sorafenib- Induced Ferroptosis Via Suppression of Nrf2.Inflammation · 2023Article
- Phenolic compounds as Nrf2 inhibitors: potential applications in cancer therapy.Cell communication and signaling : CCS · 2023Review
- Camptothecin improves sorafenib sensitivity by inhibiting Nrf2‑ARE pathway in hepatocellular carcinoma.Oncology reports · 2023Article
- New Transcriptomic Biomarkers of 5-Fluorouracil Resistance.International journal of molecular sciences · 2023Article
- Iron accumulation and lipid peroxidation: implication of ferroptosis in hepatocellular carcinoma.Frontiers in endocrinology · 2023Review
- Alkaloid fromFrontiers in pharmacology · 2022Article
- Experimental study of camptothecin combined with drug-eluting bead transarterial chemoembolization in the rabbit VX2 liver tumor model.Frontiers in oncology · 2022Article
- Targeting NLRP3 Inflammasome With Nrf2 Inducers in Central Nervous System Disorders.Frontiers in immunology · 2022Review
- The impact of mitochondria on cancer treatment resistance.Cellular oncology (Dordrecht, Netherlands) · 2021Review
Corrections and comments
- Erratum issued
Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
Abstract
backgroundResistance to chemotherapy is a major obstacle in the treatment of human hepatocellular carcinoma (HCC). Despite playing an important role in chemoprevention, nuclear factor erythroid 2-related factor 2 (NRF2) also contributes to chemo- and radio-resistance. The current study focusses on camptothecin as a novel NRF2 inhibitor to sensitise HCC to chemotherapy.
methodsThe expression and transcriptional activity of NRF2 in human HCC biopsies and camptothecin-treated culture cells were determined using immunostaining, western blot, reverse-transcription quantitative real-time PCR (RT-qPCR) and luciferase reporter assay. The effect of camptothecin on chemosensitivity of cancer cells was assessed in vitro and in xenografts.
resultsThe expression and transcriptional activity of NRF2 were substantially elevated in HCC biopsies compared with corresponding adjacent tissues, and positively correlated with serum α-fetoprotein, a clinical indicator of pathological progression. In searching chemicals targeting NRF2 for chemotherapy, we discovered that camptothecin is a potent NRF2 inhibitor. Camptothecin markedly suppressed NRF2 expression and transcriptional activity in different types of cancer cells including HepG2, SMMC-7721 and A549. As a result, camptothecin sensitised these cells to chemotherapeutic drugs in vitro and in xenografts.
conclusionsCamptothecin is a novel NRF2 inhibitor that may be repurposed in combination with other chemotherapeutics to enhance their efficacy in treating high NRF2-expressing cancers.
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