ArticleChemical science2015
Real-time detection of histone deacetylase activity with a small molecule fluorescent and spectrophotometric probe.
Article in Chemical science, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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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
7 citing papers in PubMed.
- Continuous Fluorescent Sirtuin Activity Assay Based on Fatty Acylated Lysines.International journal of molecular sciences · 2023Article
- Fluorogenic probes for detecting deacylase and demethylase activity towards post-translationally-modified lysine residues.Chemical science · 2021Article
- Design of Fluorescent Coumarin-Hydroxamic Acid Derivatives as Inhibitors of HDACs: Synthesis, Anti-Proliferative Evaluation and Docking Studies.Molecules (Basel, Switzerland) · 2020Article
- A novel fluorescent off-on probe for the sensitive and selective detection of fluoride ions.RSC advances · 2019Article
- A 2-aza-Cope reactivity-based platform for ratiometric fluorescence imaging of formaldehyde in living cells.Chemical science · 2017Article
- Targeting biomolecules with reversible covalent chemistry.Current opinion in chemical biology · 2016Review
- Single near-infrared fluorescent probe with high- and low-sensitivity sites for sensing different concentration ranges of biological thiols with distinct modes of fluorescence signals.Chemical science · 2016Article
Corrections and comments
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Histone deacetylases (HDACs) are central players in transcription regulation and important targets in cancer treatment. Activity assays are critical tools for the study of the function and regulation of these enzymes, as well as for the screening of potential inhibitors. We report a small-molecule probe for single-step, continuous detection of deacetylase activity based on an acetyl-lysine mimic functionalized with an amine-reactive fluorophore, designed to undergo rapid intramolecular imine formation upon deacetylation. The probe exhibits a bathochromic shift in the absorption spectrum and changes in fluorescence emission intensity that enable unprecedented real-time detection of HDAC activity of purified enzymes or in cell lysates, and offers a means to evaluate HDAC inhibitors
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Registered trials
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