ArticleScientific reports2016
Antagonizing STAT5B dimerization with an osmium complex.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 16 citations in OpenAlex.
- Stafiba: A STAT5-Selective Small-Molecule Inhibitor.Chembiochem : a European journal of chemical biology · 2023Article
- A small molecule HIF-1α stabilizer that accelerates diabetic wound healing.Nature communications · 2021Article
- Review
- Fine-Tuning Cytokine Signals.Annual review of immunology · 2019Review
- Eucalyptal D Enhances the Antifungal Effect of Fluconazole on Fluconazole-ResistantFrontiers in cellular and infection microbiology · 2019Article
- Inhibition of the Ras/Raf interaction and repression of renal cancer xenograftsChemical science · 2017Article
- Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b.Scientific reports · 2017Article
- Anticancer osmium complex inhibitors of the HIF-1α and p300 protein-protein interaction.Scientific reports · 2017Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Targeting STAT5 is an appealing therapeutic strategy for the treatment of hematologic malignancies and inflammation. Here, we present the novel osmium(II) complex 1 as the first metal-based inhibitor of STAT5B dimerization. Complex 1 exhibited superior inhibitory activity against STAT5B DNA binding compared to STAT5A DNA binding. Moreover, 1 repressed STAT5B transcription and blocked STAT5B dimerization via binding to the STAT5B protein, thereby inhibiting STAT5B translocation to the nucleus. Furthermore, 1 was able to selectively inhibit STAT5B phosphorylation without affecting the expression level of STAT5B.
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Registered trials
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