Presents new targets and strategies for one of the most exciting frontiers in pharmaceutical research
Epigenetic 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 discovery
-Tailored to the needs of drug developers working in small and large pharmaceutical companies
-Offers comprehensive coverage of the subject and all the techniques and applications within the field
Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.
Inhoudsopgave
PART I. Introduction – Epigenetics
Epigenetics: moving forward
PART II. General Aspects / Methodologies
Structural Biology of Epigenetic Targets: Exploiting Complexity
Computer-based lead identification for epigenetic targets
Mass spectrometry and chemical biology in epigenetics drug discovery
Peptide Microarrays for Epigenetic Targets
Chemical Probes
PART III. Epigenetic Target Classes
Inhibitors of the Zinc-dependent Histone Deacetylases
Sirtuins as Drug Targets
Selective, Small-Molecule Inhibitors of Protein Methyltransferases
LSD1 (Lysine-specific demethylase): A Decade-long Trip from Discovery to Clinical Trials
Jmj C-domain Containing Histone Demethylases
Histone Acetyltransferases
Bromodomains: promising targets for drug discovery
Lysine Reader Proteins
DNA Modifying Enzymes
Parasitic Epigenetic Targets
Over de auteur
Wolfgang Sippl, Ph D, holds the chair in Medicinal Chemistry at the Institute of Pharmacy at the Martin Luther University of Halle-Wittenberg.
Manfred Jung, Ph D, is a full professor for Pharmaceutical Chemistry at the University of Freiburg and the co-chairman of the SFB research project ‘Medical Epigenetics’.
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