ReviewQuarterly reviews of biophysics2013
Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases.
Review in Quarterly reviews of biophysics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- A Live-Cell Epigenome Manipulation by Photo-Stimuli-Responsive Histone Methyltransferase Inhibitor.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- A novel screening strategy to identify histone methyltransferase inhibitors reveals a crosstalk between DOT1L and CARM1.RSC chemical biology · 2022Article
- Allosteric regulation of histone lysine methyltransferases: from context-specific regulation to selective drugs.Biochemical Society transactions · 2021Review
- Lysine Methyltransferase Inhibitors Impair H4K20me2 and 53BP1 Foci in Response to DNA Damage in Sarcomas, a Synthetic Lethality Strategy.Frontiers in cell and developmental biology · 2021Article
- Monocyte and haematopoietic progenitor reprogramming as common mechanism underlying chronic inflammatory and cardiovascular diseases.European heart journal · 2018Review
- 3H-pyrazolo[4,3-f]quinoline haspin kinase inhibitors and anticancer properties.Bioorganic chemistry · 2018Article
- Inhibitors of Protein Methyltransferases and Demethylases.Chemical reviews · 2018Review
- Epigenetic actions of environmental factors and promising drugs for cancer therapy.Oncology letters · 2018Article
- Inhibition of Histone Demethylases Offers a Novel and Promising Approach for the Treatment of Cancer and Other Diseases.ACS medicinal chemistry letters · 2016Article
- Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy.Clinical epigenetics · 2016Review
- Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity.Drug discovery today. Technologies · 2015Review
- KDM1 class flavin-dependent protein lysine demethylases.Biopolymers · 2015Review
- Selective inhibitors of protein methyltransferases.Journal of medicinal chemistry · 2015Article
- Chemical probes of histone lysine methyltransferases.ACS chemical biology · 2015Review
- Synthesis of lysine methyltransferase inhibitors.Frontiers in chemistry · 2015Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 2 countries.
Funding
Abstract
Altered chromatin structures and dynamics are responsible for a range of human malignancies, among which the status of histone lysine methylation remains of paramount importance. Histone lysine methylation is maintained by the relative activities of sequence-specific methyltransferase (KMT) writers and demethylase (KDM) erasers, with aberrant enzymatic activities or expression profiles closely correlated with multiple human diseases. Hence, targeting these epigenetic enzymes should provide a promising avenue for pharmacological intervention of aberrantly marked sites within the epigenome. Here we present an up-to-date critical evaluation on the development and optimization of potent small molecule inhibitors targeted to histone KMTs and KDMs, with the emphasis on contributions of structural biology to development of epigenetic drugs for therapeutic intervention. We anticipate that ongoing advances in the development of epigenetic inhibitors should lead to novel drugs that site-specifically target KMTs and KDMs, key enzymes responsible for maintenance of the lysine methylation landscape in the epigenome.
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What OpenQuestion holds
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.