ArticleJournal of biomedicine & biotechnology2011
Identification of four potential epigenetic modulators from the NCI structural diversity library using a cell-based assay.
Article in Journal of biomedicine & biotechnology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 12 citations in OpenAlex.
- Article
- Generation of a Cellular Reporter for Functional BRD4 Inhibition.Bio-protocol · 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
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Authors and funding
5 authors at 4 institutions in 1 country.
Funding
Abstract
Epigenetic pathways help control the expression of genes. In cancer and other diseases, aberrant silencing or overexpression of genes, such as those that control cell growth, can greatly contribute to pathogenesis. Access to these genes by the transcriptional machinery is largely mediated by chemical modifications of DNA or histones, which are controlled by epigenetic enzymes, making these enzymes attractive targets for drug discovery. Here we describe the characterization of a locus derepression assay, a fluorescence-based mammalian cellular system which was used to screen the NCI structural diversity library for novel epigenetic modulators using an automated imaging platform. Four structurally unique compounds were uncovered that, when further investigated, showed distinct activities. These compounds block the viability of lung cancer and melanoma cells, prevent cell cycle progression, and/or inhibit histone deacetylase activity, altering levels of cellular histone acetylation.
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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.