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This resource presents new targets and strategies in the dynamic field of pharmaceutical research focused on epigenetic drug discovery. It offers a comprehensive overview of epigenetic approaches, integrating methods and strategies with specific targets, organized into three parts: Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes. The second section highlights recently developed methods for investigating epigenetic targets, including structural biology and computational techniques. Key topics include the structural biology of epigenetic targets, computer-based methods, mass spectrometry, peptide microarrays, and the development of chemical probes. The final section revisits early epigenetic targets while introducing new and largely unexplored ones, such as sirtuins, methyl-lysine reader proteins, and parasitic targets. It also discusses HDAC inhibitors, methyltransferases, demethylases (LSD1 and JMJD), histone acetyltransferases, BRD bromodomains, and DNA-modifying enzymes. This work is tailored for drug developers in both small and large pharmaceutical companies and serves as a vital resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists, providing extensive coverage of techniques and applications in the field.
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Epigenetic drug discovery, Wolfgang Sippl
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- Année de publication
- 2019
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