ArticleNature chemical biology2016
Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.
Article in Nature chemical biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 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.
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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
27 citing papers in PubMed, 48 citations in OpenAlex.
- Single-molecule imaging reveals RNA polymerase II dynamics and TAF1-dependent promoter-proximal pause release.Nature communications · 2026Article
- TAF1 acetyltransferase promotes colorectal carcinoma metastasis by catalyzing β-hydroxybutyrylation of KCTD9.Oncogene · 2026Article
- Development and comparison of single FLT3-inhibitors to dual FLT3/TAF1-inhibitors as an anti-leukemic approach.PloS one · 2025Article
- Development of a PET Probe Targeting Bromodomain and Extra-Terminal Proteins for In Vitro and In Vivo Visualization.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Regulation of the RNA polymerase II pre-initiation complex by its associated coactivators.Nature reviews. Genetics · 2023Review
- DOT1L regulates lung developmental epithelial cell fate and adult alveolar stem cell differentiation after acute injury.Stem cell reports · 2023Article
- Targeting bromodomain-containing proteins: research advances of drug discovery.Molecular biomedicine · 2023Review
- Deciphering Selectivity Mechanism of BRD9 and TAF1(2) toward Inhibitors Based on Multiple Short Molecular Dynamics Simulations and MM-GBSA Calculations.Molecules (Basel, Switzerland) · 2023Article
- The era of high-quality chemical probes.RSC medicinal chemistry · 2022Article
- Dual-target inhibitors of bromodomain and extra-terminal proteins in cancer: A review from medicinal chemistry perspectives.Medicinal research reviews · 2022Review
- A combination approach of pseudotime analysis and mathematical modeling for understanding drug-resistant mechanisms.Scientific reports · 2021Article
- Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.ACS medicinal chemistry letters · 2021Article
- Article
- Cell-surface SLC nucleoside transporters and purine levels modulate BRD4-dependent chromatin states.Nature metabolism · 2021Article
- Review
- Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.ACS medicinal chemistry letters · 2019Article
- Bromodomains: a new target class for drug development.Nature reviews. Drug discovery · 2019Review
- MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation.Nature genetics · 2019Article
- The ERBB-STAT3 Axis Drives Tasmanian Devil Facial Tumor Disease.Cancer cell · 2019Article
- Identification of highly penetrant Rb-related synthetic lethal interactions in triple negative breast cancer.Oncogene · 2018Article
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Authors and funding
17 authors at 4 institutions in 3 countries.
Funding
Abstract
Bromodomain-containing proteins of the BET family recognize histone lysine acetylation and mediate transcriptional activation of target genes such as the MYC oncogene. Pharmacological inhibitors of BET domains promise therapeutic benefits in a variety of cancers. We performed a high-diversity chemical compound screen for agents capable of modulating BRD4-dependent heterochromatization of a generic reporter in human cells. In addition to known and new compounds targeting BRD4, we identified small molecules that mimic BRD4 inhibition without direct engagement. One such compound was a potent inhibitor of the second bromodomain of TAF1. Using this inhibitor, we discovered that TAF1 synergizes with BRD4 to control proliferation of cancer cells, making TAF1 an attractive epigenetic target in cancers driven by MYC.
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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.