ArticleJournal of medicinal chemistry2019
Drug Design Targeting T-Cell Factor-Driven Epithelial-Mesenchymal Transition as a Therapeutic Strategy for Colorectal Cancer.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 17 citations in OpenAlex.
- Integrated bioinformatics and experimental validation reveal that CENPF activates mTORC1 signaling to promote colorectal cancer progression.Cancer cell international · 2026Article
- Targeting DNA Topoisomerase IIα in Retinoblastoma: Implications in EMT and Therapeutic Strategies.Biologics : targets & therapy · 2025Article
- Targeting EMT using low-dose Teniposide by downregulating ZEB2-driven activation of RNA polymerase I in breast cancer.Cell death & disease · 2024Article
- Understanding Cancer's Defense against Topoisomerase-Active Drugs: A Comprehensive Review.Cancers · 2024Review
- The validation of new CHD1L inhibitors as a therapeutic strategy for cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024Article
- miR-30c-2-3p suppresses the proliferation of human renal cell carcinoma cells by targeting TOP2A.Asian biomedicine : research, reviews and news · 2023Article
- Design, Synthesis, and Biological Evaluation of the First Inhibitors of Oncogenic CHD1L.Journal of medicinal chemistry · 2022Article
- Discovering Innate Driver Variants for Risk Assessment of Early Colorectal Cancer Metastasis.Frontiers in oncology · 2022Article
- Isolating and targeting the real-time plasticity and malignant properties of epithelial-mesenchymal transition in cancer.Oncogene · 2021Article
- First-in-Class Inhibitors of Oncogenic CHD1L with Preclinical Activity against Colorectal Cancer.Molecular cancer therapeutics · 2020Article
- High Throughput Screen Identifies the DNMT1 (DNA Methyltransferase-1) Inhibitor, 5-Azacytidine, as a Potent Inducer of PTEN (Phosphatase and Tensin Homolog): Central Role for PTEN in 5-Azacytidine Protection Against Pathological Vascular Remodeling.Arteriosclerosis, thrombosis, and vascular biology · 2020Article
Corrections and comments
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Authors and funding
19 authors at 3 institutions in 1 country.
Funding
Abstract
Metastasis is the cause of 90% of mortality in cancer patients. For metastatic colorectal cancer (mCRC), the standard-of-care drug therapies only palliate the symptoms but are ineffective, evidenced by a low survival rate of ∼11%. T-cell factor (TCF) transcription is a major driving force in CRC, and we have characterized it to be a master regulator of epithelial-mesenchymal transition (EMT). EMT transforms relatively benign epithelial tumor cells into quasi-mesenchymal or mesenchymal cells that possess cancer stem cell properties, promoting multidrug resistance and metastasis. We have identified topoisomerase IIα (TOP2A) as a DNA-binding factor required for TCF-transcription. Herein, we describe the design, synthesis, biological evaluation, and in vitro and in vivo pharmacokinetic analysis of TOP2A ATP-competitive inhibitors that prevent TCF-transcription and modulate or reverse EMT in mCRC. Unlike TOP2A poisons, ATP-competitive inhibitors do not damage DNA, potentially limiting adverse effects. This work demonstrates a new therapeutic strategy targeting TOP2A for the treatment of mCRC and potentially other types of cancers.
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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.