Fueled by the expertise of a team of international specialist authors, this
first reference on the booming topic covers everything a drug researcher needs
to know about targeting epigenetic mechanisms of disease.
The first part of the book surveys current methodologies for finding and validating drug candidates that act via epigenetic mechanisms. The second part systematically surveys known and suspected drug targets within the epigenetic machinery, including the discovery and development of vorinostat, the first marketed epigenetic drug.
Table of Contents
PART I: General aspects and methodologies.
- 1 New Frontiers in Epigenetic Modifications.
- 2 Structural Biology of Epigenetic Targets.
- 3 Computer- and Structure-based Lead Identification for Epigenetic Targets.
- 4 Histone Modification Analysis Using Mass Spectrometry.
- 5 In-vitro Assays for Histone Modifying Enzymes.
- 6 Epigenetic Targets in Drug Discovery: Cell-based assays for HDAC inhibitor hit validation.
- 7 Chromatin Immuno Precipitation ChIP: wet lab meets in silico.
PART II: Epigenetic Target Classes and Inhibitor Development.
- 8 DNA Methyltransferase Inhibitors.
- 9 Histone Deacetylase Inhibitors.
- 10 NAD-Dependent Deacetylases as Therapeutic Targets.
- 11 Inhibitors of Histone Acetyltransferases: Discovery and Biomedical Perspectives.
- 12 Histone Methyltransferases as Novel Drug Targets.
- 13 Histone Demethylases.
Wolfgang Sippl is the head of Pharmaceutical and Medicinal Chemistry at the Martin-Luther University of Halle-Wittenberg (Germany). He obtained his Ph.D. in pharmaceutical chemistry at University of Düsseldorf and was a post-doctoral fellow at the Université Louis-Pasteur in Strasbourg (France), where he worked with Camille G. Wermuth. He then took a senior researcher position in Düsseldorf before moving to the University of Halle-Wittenberg as a full professor in 2003. His main interests are focussed on medicinal chemistry, computational chemistry and drug design
Manfred Jung is Professor for Pharmaceutical and Medicinal Chemistry at the Albert-Ludwigs University of Freiburg (Germany). He obtained a Ph. D. in Pharmaceutical Chemistry from the University of Marburg, working subsequently as a postdoctoral fellow with T. Durst at the University of Ottawa (Canada). In 1994 he started his own group at the Institute of Pharmaceutical Chemistry at the University of Münster and in 2003 he moved to Freiburg to his current position. His main research focus is the synthesis of enzyme inhibitors and in-vitro assay development in the field of histone modifying enzymes.