ArticleThe Journal of clinical investigation2017
Pharmacological inhibition of the transcription factor PU.1 in leukemia.
Article in The Journal of clinical investigation, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 83 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
83 citing papers in PubMed, 121 citations in OpenAlex.
- Review
- Quantitative molecular cartography of emergency myelopoiesis reveals conserved modules of hematopoietic activation.Cell stem cell · 2026Article
- Article
- Spi-1 proto-oncogene regulates mRNA hypertranscription and malignant progression in head and neck cancer.Signal transduction and targeted therapy · 2026Article
- PU.1 inhibition sensitizes stem-monocytic AML to BCL2 blockade.bioRxiv : the preprint server for biology · 2026Article
- A conserved monocyte activation program links brain injury to systemic immune adaptation and clinical outcomes.Frontiers in immunology · 2026Article
- Rapid genome-wide introgression reveals fitness advantage of immigrant genotypes.bioRxiv : the preprint server for biology · 2025Article
- Article
- MMP9Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Article
- PSPC1 exerts an oncogenic role in AML by regulating a leukemic transcription program in cooperation with PU.1.Cell stem cell · 2025Article
- Alternative Approach to Sequence-Specific Recognition of DNA: Cooperative Stacking of Dication Dimers─Sensitivity to Compound Curvature, Aromatic Structure, and DNA Sequence.ACS chemical biology · 2025Article
- Transcription factors in the development and treatment of immune disorders.Transcription · 2025Review
- Case Report: A novelFrontiers in immunology · 2025Article
- Pharmacologic Blockade of a Pioneer Transcription Factor.Cancer research · 2024Article
- Redistribution of PU.1 partner transcription factor RUNX1 binding secures cell survival during leukemogenesis.The EMBO journal · 2024Article
- Chemical restriction of PU.1 genomic binding sites activates alternate gene networks.Nature genetics · 2024Article
- Pharmacological restriction of genomic binding sites redirects PU.1 pioneer transcription factor activity.Nature genetics · 2024Article
- Single GC base pair recognition by a heterocyclic diamidine: structures, affinities, and dynamics.RSC advances · 2024Article
- The roles of ubiquitination in AML.Annals of hematology · 2024Review
23 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
23 authors at 4 institutions in 2 countries.
Funding
Abstract
The transcription factor PU.1 is often impaired in patients with acute myeloid leukemia (AML). Here, we used AML cells that already had low PU.1 levels and further inhibited PU.1 using either RNA interference or, to our knowledge, first-in-class small-molecule inhibitors of PU.1 that we developed specifically to allosterically interfere with PU.1-chromatin binding through interaction with the DNA minor groove that flanks PU.1-binding motifs. These small molecules of the heterocyclic diamidine family disrupted the interaction of PU.1 with target gene promoters and led to downregulation of canonical PU.1 transcriptional targets. shRNA or small-molecule inhibition of PU.1 in AML cells from either PU.1lo mutant mice or human patients with AML-inhibited cell growth and clonogenicity and induced apoptosis. In murine and human AML (xeno)transplantation models, treatment with our PU.1 inhibitors decreased tumor burden and resulted in increased survival. Thus, our study provides proof of concept that PU.1 inhibition has potential as a therapeutic strategy for the treatment of AML and for the development of small-molecule inhibitors of PU.1.
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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.