ArticleJournal of proteome research2010
Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry.
Article in Journal of proteome research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 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
31 citing papers in PubMed, 57 citations in OpenAlex.
- 5-Substituted Pyridine-2,4-dicarboxylate Derivatives Have Potential for Selective Inhibition of Human Jumonji-C Domain-Containing Protein 5.Journal of medicinal chemistry · 2023Article
- JMJD family proteins in cancer and inflammation.Signal transduction and targeted therapy · 2022Review
- Fluorinated derivatives of pyridine-2,4-dicarboxylate are potent inhibitors of human 2-oxoglutarate dependent oxygenases.Journal of fluorine chemistry · 2021Article
- Allosteric regulation of protein 14-3-3ζ scaffold by small-molecule editing modulates histone H3 post-translational modifications.Theranostics · 2020Article
- Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina.Molecular neurobiology · 2019Article
- Jumonji C Demethylases in Cellular Senescence.Genes · 2019Review
- Histone Lysine Demethylase Inhibitors.Cold Spring Harbor perspectives in medicine · 2017Review
- Model for the architecture of caveolae based on a flexible, net-like assembly of Cavin1 and Caveolin discs.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Two distinct trimeric conformations of natively membrane-anchored full-length herpes simplex virus 1 glycoprotein B.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- DNA-PKcs and PARP1 Bind to Unresected Stalled DNA Replication Forks Where They Recruit XRCC1 to Mediate Repair.Cancer research · 2016Article
- Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity.Drug discovery today. Technologies · 2015Review
- Hypoxic regulation of RIOK3 is a major mechanism for cancer cell invasion and metastasis.Oncogene · 2015Article
- Drawbacks in the use of unconventional hydrophobic anhydrides for histone derivatization in bottom-up proteomics PTM analysis.Proteomics · 2015Article
- Quantitative proteomic analysis of histone modifications.Chemical reviews · 2015Review
- Quantification of histone H3 Lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors.Journal of biomolecular screening · 2015Article
- Targeting histone lysine demethylases - progress, challenges, and the future.Biochimica et biophysica acta · 2014Review
- Extracellular vesicles: a platform for the structure determination of membrane proteins by Cryo-EM.Structure (London, England : 1993) · 2014Article
- KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor.Journal of medicinal chemistry · 2014Article
- The full-length cell-cell fusogen EFF-1 is monomeric and upright on the membrane.Nature communications · 2014Article
- Structure of human RNA N⁶-methyladenine demethylase ALKBH5 provides insights into its mechanisms of nucleic acid recognition and demethylation.Nucleic acids research · 2014Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Post-translational modifications on histones are an important mechanism for the regulation of gene expression and are involved in all aspects of cell growth and differentiation, as well as pathological processes including neurodegeneration, autoimmunity, and cancer. A major challenge within the chromatin field is to develop methods for the quantitative analysis of histone modifications. Here we report a mass spectrometry (MS) approach based on ultraperformance liquid chromatography high/low collision switching (UPLC-MS(E)) to monitor histone modifications in cells. This approach is exemplified by the analysis of trimethylated lysine-9 levels in histone H3, following a simple chemical derivatization procedure with d(6)-acetic anhydride. This method was used to study the inhibition of histone demethylases with pyridine-2,4-dicarboxylic acid (PDCA) derivatives in cells. Our results show that the PDCA-dimethyl ester inhibits JMJD2A catalyzed demethylation of lysine-9 on histone H3 in human HEK 293T cells. Demethylase inhibition, as observed by MS analyses, was supported by immunoblotting with modification-specific antibodies. The results demonstrate that PDCA derived small molecules are cell permeable demethylase inhibitors and reveal that quantitative MS is a useful tool for measuring post-translational histone modifications in 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.