Drug Discovery in Cancer Epigenetics

Drug Discovery in Cancer Epigenetics

1st Edition - November 19, 2015

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  • Editors: Gerda Egger, Paola Arimondo
  • Hardcover ISBN: 9780128022085
  • eBook ISBN: 9780128024928

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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.

Key Features

  • Highlights the potential of epigenetic alterations in cancer for drug development
  • Covers the tools and methods for epigenetic drug discovery, preclinical and clinical testing, and clinical implications of epigenetic therapy
  • Provides important information regarding putative epigenetic targets, epigenetic technologies, networks and consortia for epigenetic drug discovery and routes for translation


scientists in the academic and industrial sector aiming to test and develop epigenetic cancer drugs; oncologists; geneticists; clinical researchers; clinicians interested in adopting clinical trial drugs.

Table of Contents

  • Preface
    I. Introduction
    1: Basic Epigenetic Mechanisms and Phenomena
    2: Cancer Epigenetics
    II. Methods and Tools for Epigenetic Drug Development
    3: Drug Discovery Methods
    4: Preclinical Cancer Models with the Potential to Predict Clinical Response
    5: Discovery of Biomarkers for Drug Development
    6: Networks and Consortia for Epigenetic Drug Discovery
    III. Classes of Epigenetic Drugs
    7: DNA Methyltransferase Inhibitors
    8: Small Molecule Inhibitors of Histone Deacetylases and Acetyltransferases as Potential Therapeutics in Oncology
    9: Targeting histone methylation. The development of selective methyltransferase and demethylase inhibitors
    10: Bromodomains as Anti-Cancer Targets
    11: Epigenetic Readers Interpreting the Lysine Methylome – Biological Roles and Drug Discovery
    12: Non coding RNAs: Clinical and Therapeutic Applications
    IV. Clinical Implications of Epigenetic Therapy
    13: Clinical Applications of Epigenetic Drugs
    14: Efficacy of Combined Epigenetic Therapies
    15: Predicting and Monitoring Responses to Epigenetic Drugs
    16: Episensitization: A New Word for A New Concept
    17: The Emerging Potential for Epigenetic Therapeutics in Non-Cancer Disorders

Product details

  • No. of pages: 498
  • Language: English
  • Copyright: © Academic Press 2015
  • Published: November 19, 2015
  • Imprint: Academic Press
  • Hardcover ISBN: 9780128022085
  • eBook ISBN: 9780128024928

About the Editors

Gerda Egger

Dr. Gerda Egger is an Associate Professor of Epigenetics at the Clinical Institute of Pathology, Medical University of Vienna.

Affiliations and Expertise

Associate Professor of Epigenetics, Clinical Institute of Pathology, Medical University of Vienna

Paola Arimondo

Dr. Paola Barbara Arimondo is the Director of the Unité de Service et de Recherche (USR n°3388) entitled “Epigenetic Targeting of Cancer –ETaC-“ which brings together basic and applied research – a joint laboratory of the Institut de Recherche Pierre Fabre (IRPF) and the CNRS. She is extremely experienced in researching regulatory pharmaceuticals and cancer epigenetics.

Affiliations and Expertise

Director of the Unité de Service et de Recherche, Pierre Fabre Recherche et Developpement, Castres, France

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  • Antonis T. Mon Mar 12 2018

    Drug Discovery in Cancer Epigenetics

    Very comprehensive and fulfilling from the bench to the bedside.