ArticleCancer science2018
Antimalarial drug mefloquine inhibits nuclear factor kappa B signaling and induces apoptosis in colorectal cancer cells.
Article in Cancer science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 65 citations in OpenAlex.
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- Niosomal mefloquine and cisplatin in breast cancer: comparative effects on apoptosis and angiogenesis via in vitro and in silico analysis.BMC cancer · 2025Article
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- Progress in the study of mefloquine as an antibiotic adjuvant for combination bacterial inhibition treatment.Frontiers in cellular and infection microbiology · 2024Review
- MicroRNA-26b inhibits cardiac remodeling after myocardial infarction by targeting ring finger protein 6 expression.Archives of medical science : AMS · 2024Article
- Pharmacology Progresses and Applications of Chloroquine in Cancer Therapy.International journal of nanomedicine · 2024Review
- Current trends and future prospects of drug repositioning in gastrointestinal oncology.Frontiers in pharmacology · 2023Review
- Mefloquine induces ER stress and apoptosis in BRAFi-resistant A375-BRAFMolecular carcinogenesis · 2022Article
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- Hotspot ESR1 Mutations Are Multimodal and Contextual Modulators of Breast Cancer Metastasis.Cancer research · 2022Article
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- Alkaloid leonurine exerts anti-inflammatory effects via modulating MST1 expression in trophoblast cells.Immunity, inflammation and disease · 2021Article
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- Differential Stabilities of Mefloquine-Bound Human andACS omega · 2021Article
- Dihydroartemisinin Suppresses the Tumorigenesis and Cycle Progression of Colorectal Cancer by Targeting CDK1/CCNB1/PLK1 Signaling.Frontiers in oncology · 2021Article
- Long non-coding RNA H19 regulates Bcl-2, Bax and phospholipid hydroperoxide glutathione peroxidase expression in spontaneous abortion.Experimental and therapeutic medicine · 2021Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nuclear factor kappa B (NF-κB) signaling pathway is activated in many colorectal cancer (CRC) cells and in the tumor microenvironment, which plays a critical role in cancer initiation, development, and response to therapies. In the present study, we found that the widely used antimalarial drug mefloquine was a NF-κB inhibitor that blocked the activation of IκBα kinase, leading to reduction of IκBα degradation, decrease of p65 phosphorylation, and suppressed expression of NF-κB target genes in CRC cells. We also found that mefloquine induced growth arrest and apoptosis of CRC cells harboring phosphorylated p65 in culture and in mice. Furthermore, expression of constitutive active IKKβ kinase significantly attenuated the cytotoxic effect of the compound. These results showed that mefloquine could exert antitumor action through inhibiting the NF-κB signaling pathway, and indicated that the antimalarial drug might be repurposed for anti-CRC therapy in the clinic as a single agent or in combination with other anticancer drugs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.