2011
DOI: 10.1177/1087057111417871
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Screening for Compounds That Modulate Epigenetic Regulation of the Transcriptome: An Overview

Abstract: Epigenetic control of the transciptome is a complex and highly coordinated cellular process. One critical mechanism involves DNA methylation, mediated by distinct but related DNA methyltransferases (DNMTs). Although several DNMT inhibitors are available, most are nonselective; selective DNMT inhibitors, therefore, could be optimal as therapeutics, as well acting as chemical probes to elucidate the fundamental biology of individual DNMTs. DNA methylation is a stable chemical modification, yet posttranslational … Show more

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Cited by 22 publications
(13 citation statements)
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References 97 publications
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“…55 Several virtual screening programs have also been performed, which were not systematically followed by confirmation of inhibitory ability in biochemical assays. A few HTS campaigns selected among the most representative in the literature are reported here below.…”
Section: / Update On the Identified Inhibitorsmentioning
confidence: 99%
“…55 Several virtual screening programs have also been performed, which were not systematically followed by confirmation of inhibitory ability in biochemical assays. A few HTS campaigns selected among the most representative in the literature are reported here below.…”
Section: / Update On the Identified Inhibitorsmentioning
confidence: 99%
“…A combination of regional promoter hypermethylation with the concomitant silencing of important genes involved in cell death, surveillance and proliferation is always present. However, demethylation per se is not sufficient to induce gene expression, as it is regulated by a combination of different epi‐mutations (Choo, 2011; Eglen and Reisine, 2011). DNA methylation and histone modifications are tightly correlated because inactive chromatin is enriched with hypermethylated DNA and active chromatin is associated with hypomethylated DNA.…”
Section: Dna Methyltransferases Enzymes and Their Inhibitorsmentioning
confidence: 99%
“…azacytidine and 5-aza-20-deoxycitidine, are now in use for myeloid cancers and cutaneous T cell lymphoma[108]. With emerging data showing the importance of epigenetics in the development of diabetic retinopathy, prevention of such modifications could also prove an avenue to inhibit the development of retinopathy in diabetic patients.Conclusion and perspectiveVision is the most indispensable means of communication, and diabetic retinopathy remains the leading cause of robbing a young patient of this valuable mean.…”
mentioning
confidence: 97%