ArticleCellular oncology (Dordrecht, Netherlands)2019
Inhibition of CBP/β-catenin and porcupine attenuates Wnt signaling and induces apoptosis in head and neck carcinoma cells.
Article in Cellular oncology (Dordrecht, Netherlands), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed.
- miRNA-195-5p modulates cell proliferation and stemness by targeting the Wnt signalling network in breast cancer.Non-coding RNA research · 2025Article
- Article
- Evolutionary conservation and cancer implications of the WNT signaling pathway.Medical oncology (Northwood, London, England) · 2025Review
- Porcupine expression promotes the progression of oral carcinogenesis.Neoplasia (New York, N.Y.) · 2025Article
- Review
- Mature neurons from iPSCs unveil neurodegeneration-related pathways in mucopolysaccharidosis type II: GSK-3β inhibition for therapeutic potential.Cell death & disease · 2024Article
- Article
- The β-catenin C terminus links Wnt and sphingosine-1-phosphate signaling pathways to promote vascular remodeling and atherosclerosis.Science advances · 2024Article
- The acetyltransferase BmCBP changes the acetylation modification of BmSP3 and affects its protein expression in silkworm, Bombyx mori.Molecular biology reports · 2023Article
- Review
- PORCN promotes hepatocellular carcinogenesis via Wnt/β-catenin-dependent manner.Translational cancer research · 2023Article
- Combinations of PRI-724 Wnt/β-Catenin Pathway Inhibitor with Vismodegib, Erlotinib, or HS-173 Synergistically Inhibit Head and Neck Squamous Cancer Cells.International journal of molecular sciences · 2023Article
- The role of Evi/Wntless in exporting Wnt proteins.Development (Cambridge, England) · 2023Review
- From Basic Science to Clinical Practice: The Role of Cancerous Inhibitor of Protein Phosphatase 2A (CIP2A)/p90 in Cancer.Frontiers in genetics · 2023Review
- Review
- The Wnt Signaling Pathway Inhibitors Improve the Therapeutic Activity of Glycolysis Modulators against Tongue Cancer Cells.International journal of molecular sciences · 2022Article
- WDR5 promotes the tumorigenesis of oral squamous cell carcinoma via CARM1/β-catenin axis.Odontology · 2022Article
- MicroRNA-934 promotes colorectal cancer cell proliferation by directly targeting Dickkopf-related protein 2.Experimental and therapeutic medicine · 2021Article
- Wnt/β-catenin signaling in cancers and targeted therapies.Signal transduction and targeted therapy · 2021Review
- Targeting of Deregulated Wnt/β-Catenin Signaling by PRI-724 and LGK974 Inhibitors in Germ Cell Tumor Cell Lines.International journal of molecular sciences · 2021Article
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Authors and funding
5 authors.
Funding
Abstract
purposeActivation of the Wnt pathway contributes to the development of head and neck squamous cell carcinomas (HNSCC) and its inhibition has recently emerged as a promising therapeutic strategy. Here, we aimed at identifying suitable molecular targets for down-regulation of canonical Wnt signaling in HNSCC cells.
methodsCandidate target genes (PORCN, WNT3A, FZD2, FZD5, LRP5, DVL1, CIP2A, SET, KDM1A, KDM4C, KDM6A, CBP, CARM1, KMT2A, TCF7, LEF1, PYGO1, XIAP) were silenced using siRNA and selected targets were subsequently blocked using small molecule inhibitors. The effect of this treatment on the expression of β-catenin-dependent genes was assessed by qRT-PCR. The effect of the inhibitors on cell viability was evaluated using a resazurin assay in HNSCC-derived cell lines. A luciferase reporter assay was used for confirmation of the inhibition of Wnt-dependent gene expression. Cell migration was evaluated using a scratch wound healing assay. Cytometric analysis of propidium iodide stained cells was used for cell cycle distribution evaluation, whereas cytometric analysis of caspase 3/7 activity was used for apoptosis induction evaluation.
resultsWe found that inhibition of Porcupine and CBP/β-catenin interaction by IWP-2 and PRI-724, respectively, most strongly affected β-catenin-dependent gene expression in HNSCC cells. These inhibitors also induced apoptosis and affected HNSCC cell migration.
conclusionsTargeting Porcupine or the CBP/β-catenin interaction seems to be an effective strategy for the inhibition of canonical Wnt signaling in HNSCC cells. Further studies are required to confirm the possible therapeutic effect of IWP-2 and PRI-724 in HNSCC.
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