ArticleOncotarget2016
A novel small molecule STAT3 inhibitor, LY5, inhibits cell viability, colony formation, and migration of colon and liver cancer cells.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 40 citations in OpenAlex.
- MAGI3 inhibits renal clear cell carcinoma progression through the JAK-STAT3 pathway.Translational andrology and urology · 2026Article
- TTI-101 targets STAT3/c-Myc signaling pathway to suppress cervical cancer progression: an integrated experimental and computational analysis.Cancer cell international · 2024Article
- Unraveling the complexity of STAT3 in cancer: molecular understanding and drug discovery.Journal of experimental & clinical cancer research : CR · 2024Review
- Research Progress on the Relationship Between Inflammation and Colorectal Cancer.Annals of gastroenterological surgery · 2022Review
- Shikonin suppresses colon cancer cell growth and exerts synergistic effects by regulating ADAM17 and the IL‑6/STAT3 signaling pathway.International journal of oncology · 2021Article
- LLL12B, a small molecule STAT3 inhibitor, induces growth arrest, apoptosis, and enhances cisplatin-mediated cytotoxicity in medulloblastoma cells.Scientific reports · 2021Article
- Combination of Auranofin and ICG-001 Suppress the Proliferation and Metastasis of Colon Cancer.Frontiers in oncology · 2021Article
- Review
- Targeting STAT3 anti-apoptosis pathways with organic and hybrid organic-inorganic inhibitors.Organic & biomolecular chemistry · 2020Article
- Antitumor activity of a novel oral signal transducer and activator of transcription 3 inhibitor YHO-1701.Cancer science · 2020Article
- Article
- CircZFR functions as a sponge of miR-578 to promote breast cancer progression by regulating HIF1A expression.Cancer cell international · 2020Article
- Changes in expression of p53 and inflammatory factors in patients with ulcerative colitis.Experimental and therapeutic medicine · 2019Article
- MicroRNA-204 inhibits the proliferation, migration and invasion of human lung cancer cells by targeting PCNA-1 and inhibits tumor growth in vivo.International journal of molecular medicine · 2019Article
- Bazedoxifene exhibits growth suppressive activity by targeting interleukin-6/glycoprotein 130/signal transducer and activator of transcription 3 signaling in hepatocellular carcinoma.Cancer science · 2019Article
- Article
- Comparative STAT3-Regulated Gene Expression Profile in Renal Cell Carcinoma Subtypes.Frontiers in oncology · 2019Article
- Structural Biology of STAT3 and Its Implications for Anticancer Therapies Development.International journal of molecular sciences · 2018Review
- Two novel SHP-1 agonists, SC-43 and SC-78, are more potent than regorafenib in suppressing the in vitro stemness of human colorectal cancer cells.Cell death discovery · 2018Article
- Growth-suppressive activity of raloxifene on liver cancer cells by targeting IL-6/GP130 signaling.Oncotarget · 2017Article
Corrections and comments
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Authors and funding
14 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Signal Transducer and Activator of Transcription 3 (STAT3) is persistently activated in human liver and colon cancer cells and is required for cancer cell viability, survival and migration. Therefore, inhibition of STAT3 signaling may be a viable therapeutic approach for these two cancers. We recently designed a non-peptide small molecule STAT3 inhibitor, LY5, using in silico site-directed Fragment-based drug design (FBDD). The inhibitory effect on STAT3 phosphorylation, cell viability, migration and colony forming ability by LY5 were examined in human liver and colon cancer cells. We demonstrated that LY5 inhibited constitutive Interleukin-6 (IL-6)-induced STAT3 phosphorylation, STAT3 nuclear translocation, decreased STAT3 downstream targeted gene expression and induced apoptosis in liver and colon cancer cells. LY5 had little effect on STAT1 phosphorylation mediated by IFN-γ. Inhibition of persistent STAT3 phosphorylation by LY5 also inhibited colony formation, cell migration, and decreased the viability of liver cancer and colon cancer cells. Furthermore, LY5 inhibited STAT3 phosphorylation and suppressed colon tumor growth in a mouse model in vivo. Our results suggest that LY5 is a potent STAT3 inhibitor and may be a potential drug candidate for liver and colon cancer therapy.
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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.