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- W2802993346 endingPage "20170069" @default.
- W2802993346 startingPage "20170069" @default.
- W2802993346 abstract "Within the past two decades, seven epigenetic drugs have received regulatory approval and numerous other candidates are currently in clinical trials. Among the epigenetic targets are the writer and eraser enzymes that are, respectively, responsible for the reversible introduction and removal of structural modifications in the nucleosome. This review discusses the progress achieved in the design and development of inhibitors against the key writer and eraser pairs: DNA methyltransferases and Tet demethylases; lysine/arginine methyltransferases and lysine demethylases; and histone acetyltransferases and histone deacetylases. A common theme for the successful inhibition of these enzymes in a potent and selective manner is the targeting of the cofactors present in the active site, namely zinc and iron cations, S -adenosylmethione, nicotinamide adenine dinucleotide, flavin adenine dinucleotide and acetyl Coenzyme A. This article is part of a discussion meeting issue ‘Frontiers in epigenetic chemical biology’." @default.
- W2802993346 created "2018-05-17" @default.
- W2802993346 creator A5000189394 @default.
- W2802993346 date "2018-04-23" @default.
- W2802993346 modified "2023-10-10" @default.
- W2802993346 title "Epigenetic drug discovery: a success story for cofactor interference" @default.
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- W2802993346 doi "https://doi.org/10.1098/rstb.2017.0069" @default.
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