ArticleOncotarget2016
Signal transducer and activator of transcription 3 (STAT3) inhibitor, S3I-201, acts as a potent and non-selective alkylating agent.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- The structural influence of the oncogenic driver mutation N642H in the STAT5B SH2 domain.Protein science : a publication of the Protein Society · 2025Article
- Review
- Expression analysis and mapping of Viral-Host Protein interactions of Poxviridae suggests a lead candidate molecule targeting Mpox.BMC infectious diseases · 2024Article
- Licochalcone H Induces Cell Cycle Arrest and Apoptosis in Human Skin Cancer Cells by Modulating JAK2/STAT3 Signaling.Biomolecules & therapeutics · 2022Article
- DRUGGING "UNDRUGGABLE" DISEASE-CAUSING PROTEINS: FOCUS ON SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION (STAT) 3.Transactions of the American Clinical and Climatological Association · 2022Article
- TTI-101: A competitive inhibitor of STAT3 that spares oxidative phosphorylation and reverses mechanical allodynia in mouse models of neuropathic pain.Biochemical pharmacology · 2021Article
- STAT3 as a Potential Target for Tumor Suppressive Effects of 15-Deoxy-ΔJournal of cancer prevention · 2021Article
- The transcription factor reservoir and chromatin landscape in activated plasmacytoid dendritic cells.BMC genomic data · 2021Article
- Review
- Anti-Tumor Effects of Astaxanthin by Inhibition of the Expression of STAT3 in Prostate Cancer.Marine drugs · 2020Article
- Towards the Inhibition of Protein-Protein Interactions (PPIs) in STAT3: Insights into a New Class of Benzothiadiazole Derivatives.Molecules (Basel, Switzerland) · 2020Article
- Case report for an adolescent with germline RET mutation and alveolar rhabdomyosarcoma.Cold Spring Harbor molecular case studies · 2020Article
- Trichothecin Inhibits Cancer-Related Features in Colorectal Cancer Development by Targeting STAT3.Molecules (Basel, Switzerland) · 2020Article
- Tubular STAT3 Limits Renal Inflammation in Autosomal Dominant Polycystic Kidney Disease.Journal of the American Society of Nephrology : JASN · 2020Article
- Targeting Janus Kinases and Signal Transducer and Activator of Transcription 3 to Treat Inflammation, Fibrosis, and Cancer: Rationale, Progress, and Caution.Pharmacological reviews · 2020Review
- Irreversible TrxR1 inhibitors block STAT3 activity and induce cancer cell death.Science advances · 2020Article
- Research Progress of Sirtuin4 in Cancer.Frontiers in oncology · 2020Review
- miRNA551b-3p Activates an Oncostatin Signaling Module for the Progression of Triple-Negative Breast Cancer.Cell reports · 2019Article
- SIRT4 enhances the sensitivity of ER-positive breast cancer to tamoxifen by inhibiting the IL-6/STAT3 signal pathway.Cancer medicine · 2019Article
- Oncostatin M inhibits differentiation of rat stem Leydig cells in vivo and in vitro.Journal of cellular and molecular medicine · 2019Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The Signal Transducer and Activator of Transcription 3 (STAT3) oncogene is a master regulator of many human cancers, and a well-recognized target for therapeutic intervention. A well known STAT3 inhibitor, S3I-201 (NSC 74859), is hypothesized to block STAT3 function in cancer cells by binding the STAT3 SH2 domain and disrupt STAT3 protein complexation events. In this study, liquid chromatography tandem mass spectrometry analysis revealed that STAT3, in the presence of S3I-201, showed a minimum of five specific sites of modification, cysteine's 108, 259, 367, 542, and 687. Moreover, a prepared fluorescently labeled chemical probe of S3I-201 (DB-6-055) revealed that S3I-201 non-specifically and globally alkylated intracellular proteins at concentrations consistent with S3I-201's reported IC50. These data are consistent with the hypothesis that S3I-201 is a sub-optimal probe for interrogating STAT3-related cell biology.
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Registered trials
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