ArticleMolecular pharmacology2011
Histone deacetylase inhibitors stimulate histone H3 lysine 4 methylation in part via transcriptional repression of histone H3 lysine 4 demethylases.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 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
59 citing papers in PubMed, 111 citations in OpenAlex.
- Trial
- Histone Deacetylase Inhibitors orchestrate epigenetic signalling and alter the nucleoporins and nuclear envelope in cervical cancer.Translational oncology · 2025Article
- Suv39h1 Silencing Recovers Memory Decline in Scopolamine-Induced Amnesic Mouse Model.Molecular neurobiology · 2024Article
- Review
- Current understanding of epigenetics role in melanoma treatment and resistance.Cancer cell international · 2022Review
- PaDef (Frontiers in molecular biosciences · 2022Article
- HDAC inhibitors with potential to overcome drug resistance in castration-resistant prostate cancer.Cancer drug resistance (Alhambra, Calif.) · 2022Review
- Expression, Prognostic Value, and Functional Mechanism of the KDM5 Family in Pancreatic Cancer.Frontiers in cell and developmental biology · 2022Article
- The emerging role of KDM5A in human cancer.Journal of hematology & oncology · 2021Review
- Maintenance of HDACs and H3K9me3 Prevents Arterial Flow-Induced Venous Endothelial Damage.Frontiers in cell and developmental biology · 2021Article
- Epigenetic Mechanisms of Learning and Memory: Implications for Aging.International journal of molecular sciences · 2020Review
- KMT2C/D COMPASS complex-associated diseases [KClinical epigenetics · 2020Review
- Article
- Sulforaphane protects against ethanol-induced apoptosis in neural crest cells through restoring epithelial-mesenchymal transition by epigenetically modulating the expression of Snail1.Biochimica et biophysica acta. Molecular basis of disease · 2019Article
- The LDL1/2-HDA6 Histone Modification Complex Interacts With TOC1 and Regulates the Core Circadian Clock Components inFrontiers in plant science · 2019Article
- The Arabidopsis LDL1/2-HDA6 histone modification complex is functionally associated with CCA1/LHY in regulation of circadian clock genes.Nucleic acids research · 2018Article
- Targeting class I histone deacetylases by the novel small molecule inhibitor 4SC-202 blocks oncogenic hedgehog-GLI signaling and overcomes smoothened inhibitor resistance.International journal of cancer · 2018Article
- Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors.Nature communications · 2018Article
- Parasite-Related Genetic and Epigenetic Aspects and Host Factors InfluencingFrontiers in cellular and infection microbiology · 2018Review
- JARID1 Histone Demethylases: Emerging Targets in Cancer.Trends in cancer · 2017Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
Abstract
This study investigates the mechanism by which histone deacetylase (HDAC) inhibitors up-regulate histone H3 lysine 4 (H3K4) methylation. Exposure of LNCaP prostate cancer cells and the prostate tissue of transgenic adenocarcinoma of the mouse prostate mice to the pan- and class I HDAC inhibitors (S)-(+)-N-hydroxy-4-(3-methyl-2-phenyl-butyrylamino)-benzamide (AR42), N-(2-aminophenyl)-4-[N-(pyridine-3-yl-methoxycarbonyl)-aminomethyl]-benzamide (MS-275), and vorinostat led to differential increases in H3K4 methylation. Chromatin immunoprecipitation shows that this accumulation of methylated H3K4 occurred in conjunction with decreases in the amount of the H3K4 demethylase RBP2 at the promoter of genes associated with tumor suppression and differentiation, including KLF4 and E-cadherin. This finding, together with the HDAC inhibitor-induced up-regulation of KLF4 and E-cadherin, suggests that HDAC inhibitors could activate the expression of these genes through changes in histone methylation status. Evidence indicates that this up-regulation of H3K4 methylation was attributable to the suppressive effect of these HDAC inhibitors on the expression of RBP2 and other JARID1 family histone demethylases, including PLU-1, SMCX, and LSD1, via the down-regulation of Sp1 expression. Moreover, shRNA-mediated silencing of the class I HDAC isozymes 1, 2, 3, and 8, but not that of the class II isozyme HDAC6, mimicked the drug effects on H3K4 methylation and H3K4 demethylases, which could be reversed by ectopic Sp1 expression. These data suggest a cross-talk mechanism between HDACs and H3K4 demethylases via Sp1-mediated transcriptional regulation, which underlies the complexity of the functional role of HDACs in the regulation of histone modifications.
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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.