Drug Discovery in Cancer Epigenetics is a practical resource for scientists involved in the discovery, testing, and development of epigenetic cancer drugs. Epigenetic modifications can have significant implications for translational science as biomarkers for diagnosis, prognosis or therapy prediction. Most importantly, epigenetic modifications are reversible and epigenetic players are found mutated in different cancers; therefore, they provide attractive therapeutic targets. There has been great interest in developing and testing epigenetic drugs, which inhibit DNA methyltransferases, histone modifying enzymes or chromatin reader proteins. The first few drugs are already FDA approved and have made their way into clinical settings. This book provides a comprehensive summary of the epigenetic drugs currently available and aims to increase awareness in this area to foster more rapid translation of epigenetic drugs into the clinic.

PrefaceI. Introduction 1: Basic Epigenetic Mechanisms and Phenomena2: Cancer EpigeneticsII. Methods and Tools for Epigenetic Drug Development3: Drug Discovery Methods4: Preclinical Cancer Models with the Potential to Predict Clinical Response5: Discovery of Biomarkers for Drug Development6: Networks and Consortia for Epigenetic Drug DiscoveryIII. Classes of Epigenetic Drugs7: DNA Methyltransferase Inhibitors8: Small Molecule Inhibitors of Histone Deacetylases and Acetyltransferases as Potential Therapeutics in Oncology9: Targeting histone methylation. The development of selective methyltransferase and demethylase inhibitors10: Bromodomains as Anti-Cancer Targets11: Epigenetic Readers Interpreting the Lysine Methylome - Biological Roles and Drug Discovery12: Non coding RNAs: Clinical and Therapeutic ApplicationsIV. Clinical Implications of Epigenetic Therapy13: Clinical Applications of Epigenetic Drugs14: Efficacy of Combined Epigenetic Therapies15: Predicting and Monitoring Responses to Epigenetic Drugs16: Episensitization: A New Word for A New Concept17: The Emerging Potential for Epigenetic Therapeutics in Non-Cancer Disorders