Epigenetic Targets in Drug Discovery

Cover......Page 1
Frontmatter......Page 2
Contents......Page 6
List of Contributors......Page 13
Preface......Page 16
A Personal Foreword......Page 19
Part One
General Aspects and Methodologies......Page 22
1 New Frontiers in Epigenetic Modifications......Page 23
2 Structural Biology of Epigenetic Targets......Page 43
3 Computer- and Structure-Based Lead Identification for Epigenetic Targets......Page 77
4 Histone Modification Analysis Using Mass Spectrometry......Page 106
5 In Vitro Assays for Histone-Modifying Enzymes......Page 117
6 Epigenetic Targets in Drug Discovery: Cell-Based Assays for HDAC Inhibitor Hit Validation......Page 137
7 Chromatin Immunoprecipitation ChIP: Wet Lab Meets In Silico......Page 156
Part Two
Epigenetic Target Classes and Inhibitor Development......Page 177
8 DNA Methyltransferase Inhibitors......Page 178
9 Histone Deacetylase Inhibitors......Page 199
10 NAD-Dependent Deacetylases as Therapeutic Targets......Page 238
11 Inhibitors of Histone Acetyltransferases: Discovery and Biomedical Perspectives......Page 256
12 Histone Methyltransferases as Novel Drug Targets......Page 264
13 Histone Demethylases......Page 282
Index......Page 304