ArticleAnalytical biochemistry2008
A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression.
Article in Analytical biochemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 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.
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Who cites it
23 citing papers in PubMed, 39 citations in OpenAlex.
- Small molecule splicing modulators that disrupt O-GlcNAc homeostasis.Nature communications · 2026Article
- Dual-directional epi-genotoxicity assay for assessing chemically induced epigenetic effects utilizing the housekeeping TK gene.Scientific reports · 2025Article
- Improving the power of drug toxicity measurements by quantitative nuclei imaging.Cell death discovery · 2024Article
- Article
- Integration of Epigenetic Mechanisms into Non-Genotoxic Carcinogenicity Hazard Assessment: Focus on DNA Methylation and Histone Modifications.International journal of molecular sciences · 2021Review
- Nuisance compounds in cellular assays.Cell chemical biology · 2021Review
- HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes.PloS one · 2021Article
- Epigenetic Applications in Adverse Outcome Pathways and Environmental Risk Evaluation.Environmental health perspectives · 2018Article
- Circulating tumor cells and CDX models as a tool for preclinical drug development.Translational lung cancer research · 2017Review
- Generation of a Cellular Reporter for Functional BRD4 Inhibition.Bio-protocol · 2017Article
- A trichostatin A expression signature identified by TempO-Seq targeted whole transcriptome profiling.PloS one · 2017Article
- Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.Nature chemical biology · 2016Article
- Article
- Identification of small molecule modulators of gene transcription with anticancer activity.ACS chemical biology · 2014Article
- Pre-clinical studies of epigenetic therapies targeting histone modifiers in lung cancer.Frontiers in oncology · 2013Review
- A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.Nature communications · 2013Article
- Anthraquinones from a marine-derived Streptomyces spinoverrucosus.Journal of natural products · 2012Article
- Erythrazoles A-B, cytotoxic benzothiazoles from a marine-derived Erythrobacter sp.Organic letters · 2011Article
- Identification of four potential epigenetic modulators from the NCI structural diversity library using a cell-based assay.Journal of biomedicine & biotechnology · 2011Article
- Apparent activity in high-throughput screening: origins of compound-dependent assay interference.Current opinion in chemical biology · 2010Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Epigenetic regulation of gene expression is essential in embryonic development and contributes to cancer pathology. We used a cell-based imaging assay that measures derepression of a silenced green fluorescent protein (GFP) reporter to identify novel classes of compounds involved in epigenetic regulation. This locus derepression (LDR) assay was screened against a 69,137-member chemical library using quantitative high-throughput screening (qHTS), a titration-response method that assays compounds at multiple concentrations. From structure-activity relationships of the 411 actives recovered from the qHTS, 6 distinct chemical series were chosen for further study. A total of 48 qHTS actives and analogs were counterscreened using the parental line of the LDR cells, which lack the GFP reporter. Three series-8-hydroxy quinoline, quinoline-8-thiol, and 1,3,5-thiadiazinane-2-thione-were not fluorescent and reconfirmed activity in the LDR cells. The three active series did not inhibit histone deacetylase activity in nuclear extracts or reactivate the expression of the densely methylated p16 gene in cancer cells. However, one series induced expression of the methylated CDH13 gene and inhibited the viability of several lung cancer lines at submicromolar concentrations. These results suggest that the identified small molecules act on epigenetic or transcriptional components and validate our approach of using a cell-based imaging assay in conjunction with qHTS.
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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.