ArticleProceedings of the National Academy of Sciences of the United States of America2021
Live-cell epigenome manipulation by synthetic histone acetylation catalyst system.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 37 citations in OpenAlex.
- Chemical reactions for the ligand-directed modification of native proteins.Chemical Society reviews · 2026Review
- Progress and challenges in traceless ligand-directed labelling chemistry.Communications chemistry · 2026Review
- Precision Chemistry for Protein Lysine Modification.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
- OptoChaperone─A Biohybrid Tool for Regulating Protein Condensates in Cells and In Vitro.Journal of the American Chemical Society · 2026Article
- Real-Time and Spatially Resolved Epigenetic Dynamics Tracking Beyond DNA Methylation via Live-Cell Epigenetic Sensors in 3D Systems.Biosensors · 2026Review
- Polyethylene glycol incorporation to reduce the cytotoxicity associated with cationic cell-penetrating-peptide conjugation.RSC medicinal chemistry · 2025Article
- Catalysis in Chemical Modification of Proteins.ChemCatChem · 2025Article
- Chemical catalyst manipulating cancer epigenome and transcription.Nature communications · 2025Article
- Designer Adaptor Proteins for Functional Conversion of Peptides to Small-Molecule Ligands toward In-Cell Catalytic Protein Modification.ACS central science · 2023Article
- Interactions of Nucleosomes with Acidic Patch-Binding Peptides: A Combined Structural Bioinformatics, Molecular Modeling, Fluorescence Polarization, and Single-Molecule FRET Study.International journal of molecular sciences · 2023Article
- A chemical catalyst enabling histone acylation with endogenous acyl-CoA.Nature communications · 2023Article
- Actin filaments accumulated in the nucleus remain in the vicinity of condensing chromosomes in the zebrafish early embryo.Biology open · 2023Article
- Overcoming the Limitations of CRISPR-Cas9 Systems inMicroorganisms · 2023Review
- Catalytic covalent inhibition of cyclooxygenase-1 by a biomimetic acyltransferase.Bioorganic & medicinal chemistry · 2022Article
- Development of Artificial System to Induce Chromatin Loosening inBiomolecules · 2022Article
- Synthetic Proteins behind the Plasma Barrier: Molecular Spies.Accounts of chemical research · 2022Article
- Multiplexed Delivery of Synthetic (Un)Conjugatable Ubiquitin and SUMO2 Enables Simultaneous Monitoring of Their Localization and Function in Live Cells.Chembiochem : a European journal of chemical biology · 2022Article
- Targeted Protein Acetylation in Cells Using Heterobifunctional Molecules.Journal of the American Chemical Society · 2021Article
- Live-cell imaging probes to track chromatin modification dynamics.Microscopy (Oxford, England) · 2021Article
- Histone acylations and chromatin dynamics: concepts, challenges, and links to metabolism.EMBO reports · 2021Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chemical modifications of histones, such as lysine acetylation and ubiquitination, play pivotal roles in epigenetic regulation of gene expression. Methods to alter the epigenome thus hold promise as tools for elucidating epigenetic mechanisms and as therapeutics. However, an entirely chemical method to introduce histone modifications in living cells without genetic manipulation is unprecedented. Here, we developed a chemical catalyst, PEG-LANA-DSSMe 11, that binds with nucleosome's acidic patch and promotes regioselective, synthetic histone acetylation at H2BK120 in living cells. The size of polyethylene glycol in the catalyst was a critical determinant for its in-cell metabolic stability, binding affinity to histones, and high activity. The synthetic acetylation promoted by 11 without genetic manipulation competed with and suppressed physiological H2B ubiquitination, a mark regulating chromatin functions, such as transcription and DNA damage response. Thus, the chemical catalyst will be a useful tool to manipulate epigenome for unraveling epigenetic mechanisms in living cells.
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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.