ArticleCells2023
Oral Squamous Cell Carcinoma Cells with Acquired Resistance to Erlotinib Are Sensitive to Anti-Cancer Effect of Quercetin via Pyruvate Kinase M2 (PKM2).
Article in Cells, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 32 citations in OpenAlex.
- Plant-Derived Modulators of Tumor Metabolism as Novel, Efficacious, and Low-Toxicity Therapeutic Agents for Cancer Treatment.Molecules (Basel, Switzerland) · 2026Review
- Natural compounds for non-small cell lung cancer treatment: focus on the EGFR signaling pathway.Frontiers in pharmacology · 2026Review
- Phytochemicals as Emerging Antiproliferative Agents in Head and Neck Cancer: Molecular Mechanisms and Therapeutic Strategies.Pharmacology · 2026Review
- Integrating polyphenols and exercise in cancer prevention, treatment, and rehabilitation: cellular and molecular mechanisms linking the injury-recovery-musculoskeletal resilience axis.Frontiers in oncology · 2026Review
- Review
- Dietary Polyphenol Combinations Have a Multifaceted Inhibitory Effect on Metabolic Rewiring and Signaling Pathways in Neuroblastoma.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Mechanism of action ofOncology letters · 2025Article
- Review
- Warburg effect and lactylation in cancer: mechanisms for chemoresistance.Molecular medicine (Cambridge, Mass.) · 2025Review
- An Integrated Approach of Network Pharmacology, Bioinformatics, Molecular Docking, and Experimental Verification UncoversCurrent pharmaceutical design · 2025Article
- Recent Developments in Tyrosine Kinase Inhibitor-based Nanotherapeutics for EGFR-resistant Non-small Cell Lung Cancer.Current drug delivery · 2025Review
- Quercetin and Nano-Derivatives: Potential and Challenges in Cancer Therapy.International journal of nanomedicine · 2025Review
- Momordicine-I suppresses head and neck cancer growth by modulating key metabolic pathways.Cell communication and signaling : CCS · 2024Article
- Cancer Prevention and Treatment with Polyphenols: Type IV Collagenase-Mediated Mechanisms.Cancers · 2024Review
- Epigenetic regulation of mRNA mediates the phenotypic plasticity of cancer cells during metastasis and therapeutic resistance (Review).Oncology reports · 2024Review
- Effects of Topoisomerase II alpha Inhibition on Oral Cancer Cell Metabolism and Cancer Stem Cell Function.Dental research and oral health · 2024Article
- Decoding the research landscape of drug resistance and therapeutic approaches in head and neck cancer: a bibliometric analysis from 2000 to 2023.Frontiers in pharmacology · 2024Article
- Quercetin in Oncology: A Phytochemical with Immense Therapeutic Potential.Current drug targets · 2024Review
- Phytochemicals Target Multiple Metabolic Pathways in Cancer.Antioxidants (Basel, Switzerland) · 2023Review
- Anti-Cancer Potential of Phytochemicals: The Regulation of the Epithelial-Mesenchymal Transition.Molecules (Basel, Switzerland) · 2023Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oral squamous cell carcinoma (OSCC) frequently carries high epidermal growth factor receptor (EGFR) expression. Erlotinib, a small molecule tyrosine kinase inhibitor (TKI), is an effective inhibitor of EGFR activity; however, resistance to this drug can occur, limiting therapeutic outcomes. Therefore, in the current study, we aimed to unveil key intracellular molecules and adjuvant reagents to overcome erlotinib resistance. First, two HSC-3-derived erlotinib-resistant cell lines, ERL-R5 and ERL-R10, were established; both exhibited relatively higher growth rates, glucose utilization, epithelial-mesenchymal transition (EMT), and invasiveness compared with parental cells. Cancer aggressiveness-related proteins, such as N-cadherin, Vimentin, Twist, MMP-2, MMP-9, and MMP-13, and the glycolytic enzymes PKM2 and GLUT1 were upregulated in ERL-R cells. Notably, ERL-R cells were sensitive to quercetin, a naturally-existing flavonol phytochemical with anti-cancer properties against various cancer cells. At a concentration of 5 μM, quercetin effectively arrested cell growth, reduced glucose utilization, and inhibited cellular invasiveness. An ERL-R5-derived xenograft mouse model confirmed the growth-inhibitory efficacy of quercetin. Additionally, knock-down of PKM2 by siRNA mimicked the effect of quercetin and re-sensitized ERL-R cells to erlotinib. Furthermore, adding quercetin blocked the development of erlotinib-mediated resistance by enhancing apoptosis. In conclusion, our data support the application of quercetin in anti-erlotinib-resistant OSCC and indicate that PKM2 is a determinant factor in erlotinib resistance and quercetin sensitivity.
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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.