ArticleScientific reports2019
Anti-cancer activity of the novel 2-hydroxydiarylamide derivatives IMD-0354 and KRT1853 through suppression of cancer cell invasion, proliferation, and survival mediated by TMPRSS4.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 29 citations in OpenAlex.
- TMPRSS4 as a prognostic biomarker after gastric cancer surgery in a multicenter retrospective study.Scientific reports · 2025Article
- Identification of potent TMPRSS4 inhibitors through structural modeling and molecular dynamics simulations.Scientific reports · 2025Article
- Nanomaterials modulate tumor-associated macrophages for the treatment of digestive system tumors.Bioactive materials · 2024Review
- Utilization of Existing Human Kinase Inhibitors as Scaffolds in the Development of New Antimicrobials.Antibiotics (Basel, Switzerland) · 2023Review
- TMPRSS4, a type II transmembrane serine protease, as a potential therapeutic target in cancer.Experimental & molecular medicine · 2023Review
- Salicylanilides and Their Anticancer Properties.International journal of molecular sciences · 2023Review
- Review
- Targeting HDAC6 to Overcome Autophagy-Promoted Anti-Cancer Drug Resistance.International journal of molecular sciences · 2022Review
- Utility of TMPRSS4 as a Prognostic Biomarker and Potential Therapeutic Target in Patients with Gastric Cancer.Journal of gastrointestinal surgery : official journal of the Society for Surgery of the Alimentary Tract · 2022Article
- Integrative Analysis for Identification of Therapeutic Targets and Prognostic Signatures in Non-Small Cell Lung Cancer.Bioinformatics and biology insights · 2022Article
- A New NF-κB Inhibitor, MEDS-23, Reduces the Severity of Adverse Post-Ischemic Stroke Outcomes in Rats.Brain sciences · 2021Article
- TMPRSS4 promotes cancer stem-like properties in prostate cancer cells through upregulation of SOX2 by SLUG and TWIST1.Journal of experimental & clinical cancer research : CR · 2021Article
- Metastasis Prevention: Focus on Metastatic Circulating Tumor Cells.Molecular diagnosis & therapy · 2021Review
- Transmembrane Protease TMPRSS4 Promotes the Formation and Development of Mismatch Repair Deficient Colon Cancer Liver Metastasis.Bulletin of experimental biology and medicine · 2021Article
- LncRNA PAINT is associated with aggressive prostate cancer and dysregulation of cancer hallmark genes.International journal of cancer · 2021Article
- TMEM52B suppression promotes cancer cell survival and invasion through modulating E-cadherin stability and EGFR activity.Journal of experimental & clinical cancer research : CR · 2021Article
- Inhibition of kinase IKKβ suppresses cellular abnormalities induced by the human papillomavirus oncoprotein HPV 18E6.Scientific reports · 2021Article
- New Antimicrobial Bioactivity against Multidrug-Resistant Gram-Positive Bacteria of Kinase Inhibitor IMD0354.Antibiotics (Basel, Switzerland) · 2020Article
- Clinical study of colorectal cancer operation: Survival analysis.Korean journal of clinical oncology · 2020Article
- Therapeutic Targeting of Signaling Pathways Related to Cancer Stemness.Frontiers in oncology · 2020Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Elevated expression of transmembrane serine protease 4 (TMPRSS4) correlates with poor prognosis in non-small cell lung cancer, gastric cancer, colorectal cancer, prostate cancer, and other cancer patients. Previously, we demonstrated that TMPRSS4 mediates tumor cell invasion, migration, proliferation, and metastasis. In addition, we reported novel 2-hydroxydiarylamide derivatives, IMD-0354 and KRT1853, as TMPRSS4 serine protease inhibitors. Here, we further evaluated the effects of the representative derivatives on TMPRSS4-mediated cellular function and signaling. IMD-0354 and KRT1853 inhibited cancer cell invasion, migration, and proliferation in TMPRSS4-expressing prostate, colon, and lung cancer cells. Both compounds suppressed TMPRSS4-mediated induction of Sp1/3, AP-1, and NF-κB transcription factors. Furthermore, TMPRSS4 promoted cancer cell survival and drug resistance, and both compounds enhanced anoikis sensitivity as well as reduced bcl-2 and survivin levels. Importantly, KRT1853 efficiently reduced tumor growth in prostate and colon cancer xenograft models. These results strongly recommend KRT1853 for further development as a novel anti-cancer agent.
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