ArticleCell death & disease2015
Identification of thiostrepton as a novel therapeutic agent that targets human colon cancer stem cells.
Article in Cell death & disease, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 39 citations in OpenAlex.
- Targeting FOXM1 regulates metabolic signatures through ROS-dependent JNK/Bmi1/Skp2 axis in human cutaneous T-cell lymphoma.Cell death & disease · 2026Article
- Drug-Repurposing Screen Identifies Thiostrepton as a Novel Regulator of the Tumor Suppressor DAB2IP.Biomolecules · 2025Article
- Thiostrepton induces apoptotic cell death at the level of BCL-2/CED-9 in C. elegans.Scientific reports · 2025Article
- Senescent lung-resident mesenchymal stem cells drive pulmonary fibrogenesis through FGF-4/FOXM1 axis.Stem cell research & therapy · 2024Article
- Article
- KCNJ14 knockdown significantly inhibited the proliferation and migration of colorectal cells.BMC medical genomics · 2022Article
- Emerging agents that target signaling pathways to eradicate colorectal cancer stem cells.Cancer communications (London, England) · 2021Review
- Integrative transcriptomics analysis of lung epithelial cells and identification of repurposable drug candidates for COVID-19.European journal of pharmacology · 2020Article
- FOXM1 modulates docetaxel resistance in prostate cancer by regulating KIF20A.Cancer cell international · 2020Article
- G Protein-Coupled Receptor GPR87 Promotes the Expansion of PDA Stem Cells through Activating JAK2/STAT3.Molecular therapy oncolytics · 2020Article
- A preclinical evaluation of thiostrepton, a natural antibiotic, in nasopharyngeal carcinoma.Investigational new drugs · 2020Article
- FOXM1 and Cancer: Faulty Cellular Signaling Derails Homeostasis.Frontiers in oncology · 2020Review
- In silico identification of thiostrepton as an inhibitor of cancer stem cell growth and an enhancer for chemotherapy in non-small-cell lung cancer.Journal of cellular and molecular medicine · 2019Article
- FOXM1-Mediated LINC-ROR Regulates the Proliferation and Sensitivity to Sorafenib in Hepatocellular Carcinoma.Molecular therapy. Nucleic acids · 2019Article
- Epigenetically modulated FOXM1 suppresses dendritic cell maturation in pancreatic cancer and colon cancer.Molecular oncology · 2019Article
- FoxM1 is an independent poor prognostic marker and therapeutic target for advanced Middle Eastern breast cancer.Oncotarget · 2018Article
- Identification of claudin-4 binder that attenuates tight junction barrier function by TR-FRET-based screening assay.Scientific reports · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Accumulating evidence shows that colorectal cancer stem cells (CRSCs) are largely responsible for the metastasis and relapse of colorectal cancer (CRC) after therapy. Hence, identifying new agents that specifically target CRSCs would help improve the effectiveness of current CRC therapies. To accelerate identification of agents targeting CRSCs, the Connectivity Map (CMap) approach was used. Among the top-ranked candidates, thiostrepton, a thiazole antibiotic, was selected for further investigation because of its known tumoricidal activity. Thiostrepton could selectively induce apoptosis in CRSC subpopulations in both parental HCT-15 and HT-29 human CRC lines as well as in EMT and chemoresistant clones derived from them. Further, we investigated its inhibitory effects on the sphere- and colony-forming capabilities of the aforementioned CRC lines. The in vitro inhibition of sphere and colony formation was associated with downregulation of various modulators of the stem cell phenotype. The combination of thiostrepton and oxaliplatin eradicated both CD44(+) HCT-15 and HT-29 cells more efficiently than either drug alone. FoxM1, an oncogenic transcription factor, was identified as a critical positive modulator of stemness and as the main target of thiostrepton in the CRC lines. This is the first report showing the selective killing of CRSCs by thiostrepton, which has been proposed to be a promising anti-neoplastic agent. On the basis of its synergism with oxaliplatin in killing CRSCs in vitro, if this activity is confirmed in vivo, thiostrepton may be a promising agent to be used clinically in combination with current chemotherapies to improve the efficacy of these regimens.
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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.