ArticleThe Journal of biological chemistry2015
Molecular Insights into Inhibition of the Methylated Histone-Plant Homeodomain Complexes by Calixarenes.
Article in The Journal of biological chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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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
13 citing papers in PubMed, 41 citations in OpenAlex.
- The upregulation of GDF15 is controlled epigenetically by oncogenic TCF19 signaling in human hepatocellular carcinoma.iScience · 2025Article
- N-Terminal Protein Binding and Disorder-to-Order Transition by a Synthetic Receptor.Biochemistry · 2025Article
- Deciphering the dual roles of PHD finger proteins from oncogenic drivers to tumor suppressors.Frontiers in cell and developmental biology · 2024Review
- Modulation of the functional interfaces between retroviral intasomes and the human nucleosome.mBio · 2023Article
- Non-histone binding functions of PHD fingers.Trends in biochemical sciences · 2023Review
- Chemical tools targeting readers of lysine methylation.Current opinion in chemical biology · 2023Review
- Targeting Epigenetic Regulatory Enzymes for Cancer Therapeutics: Novel Small-Molecule Epidrug Development.Frontiers in oncology · 2022Review
- Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy.Molecules (Basel, Switzerland) · 2020Review
- NMR Spectroscopy of supramolecular chemistry on protein surfaces.Beilstein journal of organic chemistry · 2020Review
- Direct measurement of the mechanical properties of a chromatin analog and the epigenetic effects of para-sulphonato-calix[4]arene.Scientific reports · 2019Article
- Milestones in transcription and chromatin published in theThe Journal of biological chemistry · 2019Review
- Curcumin: a calixarene derivative micelle potentiates anti-breast cancer stem cells effects in xenografted, triple-negative breast cancer mouse models.Drug delivery · 2017Article
- Toward development of epigenetic drugs for central nervous system disorders: Modulating neuroplasticity via H3K4 methylation.Psychiatry and clinical neurosciences · 2016Review
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
Plant homeodomain (PHD) finger-containing proteins are implicated in fundamental biological processes, including transcriptional activation and repression, DNA damage repair, cell differentiation, and survival. The PHD finger functions as an epigenetic reader that binds to posttranslationally modified or unmodified histone H3 tails, recruiting catalytic writers and erasers and other components of the epigenetic machinery to chromatin. Despite the critical role of the histone-PHD interaction in normal and pathological processes, selective inhibitors of this association have not been well developed. Here we demonstrate that macrocyclic calixarenes can disrupt binding of PHD fingers to methylated lysine 4 of histone H3 in vitro and in vivo. The inhibitory activity relies on differences in binding affinities of the PHD fingers for H3K4me and the methylation state of the histone ligand, whereas the composition of the aromatic H3K4me-binding site of the PHD fingers appears to have no effect. Our approach provides a novel tool for studying the biological roles of methyllysine readers in epigenetic signaling.
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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.