Epigenetic Targets in Drug Discovery

by Sippl, Wolfgang; Jung, Manfred; Mannhold, Raimund; Kubinyi, Hugo; Folkers, Gerd

• ISBN13: 9783527323555
• ISBN10: 3527323554
• Edition: 1st
• Format: Hardcover
• Copyright: 2009-08-03
• Publisher: Wiley-VCH

Summary

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.

Author Biography

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 D++sseldorf and was a post-doctoral fellow at the Universit+¬ Louis-Pasteur in Strasbourg (France), where he worked with Camille G. Wermuth. He then took a senior researcher position in D++sseldorf 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 M++nster 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.

Table of Contents

General aspects and methodologies

New Frontiers in Epigenetic Modifications

Structural Biology of Epigenetic Targets

Computer- and Structure-based Lead Identification for Epigenetic Targets

Histone Modification Analysis Using Mass Spectrometry

In-vitro Assays for Histone Modifying Enzymes

Epigenetic Targets in Drug Discovery: Cell-based assays for HDAC inhibitor hit validation

Chromatin Immuno Precipitation ChIP: wet lab meets in silico

Epigenetic Target Classes and Inhibitor Development

DNA Methyltransferase Inhibitors

Histone Deacetylase Inhibitors

NAD-Dependent Deacetylases as Therapeutic Targets

Inhibitors of Histone Acetyltransferases: Discovery and Biomedical Perspectives

Histone Methyltransferases as Novel Drug Targets

Histone Demethylases

Table of Contents provided by Publisher. All Rights Reserved.