Epigenetic Drug Discovery

This broad view of epigenetic approaches in drug discovery combines methods and strategies with individual targets, including new and largely unexplored ones such as sirtuins and methyl-lysine reader proteins. Presented in three parts - Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes - it covers everything any drug researcher would need in order to know about targeting epigenetic mechanisms of disease. Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.

Presents new targets and strategies for one of the most exciting frontiers in pharmaceutical researchEpigenetic Drug Discovery provides a broad overview of epigenetic approaches in drug research, combining methods and strategies with individual targets. Presented in three parts - Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes - it covers everything any drug researcher would need in order to know about targeting epigenetic mechanisms of disease.The second part of Epigenetic Drug Discovery discusses recently developed methods for examining epigenetic targets, as well as new structural biology and computational approaches. Topics include the structural biology of epigenetic targets, computer-based approaches, mass spectrometry approaches, peptide microarrays for epigenetic targets, and chemical probe development. The third part revisits some of the early epigenetic targets and adds a number of new and still largely unexplored targets, such as sirtuins, methyl-lysine reader proteins, and parasitic targets. It also covers HDAC inhibitors, methyltransferases, demethylases LSD1 and JMJD, histone acetyltransferases, BRD bromodomains, and DNA modifying enzymes.The latest strategies and targets for epigenetic drug discoveryTailored to the needs of drug developers working in small and large pharmaceutical companiesOffers comprehensive coverage of the subject and all the techniques and applications within the fieldEpigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.

PART I. Introduction - EpigeneticsEpigenetics: moving forwardPART II. General Aspects / MethodologiesStructural Biology of Epigenetic Targets: Exploiting ComplexityComputer-based lead identification for epigenetic targetsMass spectrometry and chemical biology in epigenetics drug discoveryPeptide Microarrays for Epigenetic TargetsChemical ProbesPART III. Epigenetic Target ClassesInhibitors of the Zinc-dependent Histone DeacetylasesSirtuins as Drug TargetsSelective, Small-Molecule Inhibitors of Protein MethyltransferasesLSD1 (Lysine-specific demethylase): A Decade-long Trip from Discovery to Clinical TrialsJmjC-domain Containing Histone DemethylasesHistone AcetyltransferasesBromodomains: promising targets for drug discoveryLysine Reader ProteinsDNA Modifying EnzymesParasitic Epigenetic Targets