ArticleScientific reports2017
Development of Erasin: a chromone-based STAT3 inhibitor which induces apoptosis in Erlotinib-resistant lung cancer cells.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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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
12 citing papers in PubMed, 26 citations in OpenAlex.
- Fluorinated Chromone Derivatives: Synthesis, Theoretical Study, and Evaluation of Their Biological Potential.ACS omega · 2026Article
- Ultrahigh-Throughput Virtual Screening Strategies against PPI Targets: A Case Study of STAT Inhibitors.Journal of chemical information and modeling · 2025Article
- Design, synthesis,Future medicinal chemistry · 2025Article
- Evolving cognition of the JAK-STAT signaling pathway: autoimmune disorders and cancer.Signal transduction and targeted therapy · 2023Review
- Acylhydrazones and Their Biological Activity: A Review.Molecules (Basel, Switzerland) · 2022Review
- Leptin Gene Protects Against Cold Stress in Antarctic Toothfish.Frontiers in physiology · 2021Article
- Towards the Inhibition of Protein-Protein Interactions (PPIs) in STAT3: Insights into a New Class of Benzothiadiazole Derivatives.Molecules (Basel, Switzerland) · 2020Article
- Trichothecin Inhibits Cancer-Related Features in Colorectal Cancer Development by Targeting STAT3.Molecules (Basel, Switzerland) · 2020Article
- Transcription Factor Inhibition: Lessons Learned and Emerging Targets.Trends in molecular medicine · 2020Review
- Targeting STAT3 in Cancer with Nucleotide Therapeutics.Cancers · 2019Review
- Expression profile and prognostic values of STAT family members in non-small cell lung cancer.American journal of translational research · 2019Article
- Lycorine Displays Potent Antitumor Efficacy in Colon Carcinoma by Targeting STAT3.Frontiers in pharmacology · 2018Article
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Authors and funding
11 authors at 2 institutions in 2 countries.
Funding
Abstract
Inhibition of protein-protein interactions by small molecules offers tremendous opportunities for basic research and drug development. One of the fundamental challenges of this research field is the broad lack of available lead structures from nature. Here, we demonstrate that modifications of a chromone-based inhibitor of the Src homology 2 (SH2) domain of the transcription factor STAT5 confer inhibitory activity against STAT3. The binding mode of the most potent STAT3 inhibitor Erasin was analyzed by the investigation of structure-activity relationships, which was facilitated by chemical synthesis and biochemical activity analysis, in combination with molecular docking studies. Erasin inhibits tyrosine phosphorylation of STAT3 with selectivity over STAT5 and STAT1 in cell-based assays, and increases the apoptotic rate of cultured NSCLC cells in a STAT3-dependent manner. This ability of Erasin also extends to HCC-827 cells with acquired resistance against Erlotinib, a clinically used inhibitor of the EGF receptor. Our work validates chromone-based acylhydrazones as privileged structures for antagonizing STAT SH2 domains, and demonstrates that apoptosis can be induced in NSCLC cells with acquired Erlotinib resistance by direct inhibition of STAT3.
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Registered trials
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