Drug Discovery in Cancer Epigenetics 1st Edition by Gerda Egger, Paola Arimondo ISBN 0128024925 9780128024928

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ISBN 10: 0128024925 
ISBN 13: 9780128024928
Author: Gerda Egger, Paola Arimondo

Drug Discovery in Cancer Epigenetics 1st Table of contents:

Part I: Introduction
Chapter 1. Basic Epigenetic Mechanisms and Phenomena

• Abstract

• 1.1 Introduction

• 1.2 Basic Epigenetic Mechanisms

• 1.3 Epigenetic (Re)Programming

• 1.4 Genomic Imprinting as a Model of Epigenetic Silencing

• 1.5 Dosage Compensation in Mammals

• 1.6 PEV in Drosophila

• 1.7 Transgenerational and Intergenerational Epigenetic Inheritance

• 1.8 Epigenetics and Disease

• References

Chapter 2. Cancer Epigenetics

• Abstract

• 2.1 Background

• 2.2 DNA Methylation

• 2.3 Histone Modifications

• 2.4 Nucleosome Positions and Higher-Order Structures

• 2.5 Noncoding RNAs

• 2.6 Mutation of Epigenetic Enzymes

• 2.7 Conclusion

• References

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Part II: Methods and Tools for Epigenetic Drug Development
Chapter 3. Drug Discovery Methods

• Abstract

• 3.1 Introduction

• 3.2 Hit Discovery

• 3.3 Lead Optimization and Identification

• 3.4 Pharmacological Profiling and Drug–Target Engagement

• 3.5 General Conclusions

• Acknowledgments

• References

Chapter 4. Preclinical Cancer Models with the Potential to Predict Clinical Response

• Abstract

• 4.1 Introduction

• 4.2 Remodeling Human Cancers and Their Use as Preclinical Models

• 4.3 Assessing Drug Response in Complex Models

• 4.4 Conclusions

• Acknowledgments

• References

Chapter 5. Biomarker Development in Targeting Cancer Epigenetic

• Abstract

• 5.1 Introduction

• 5.2 Why Do We Need Biomarkers?

• 5.3 Monitoring Target Engagement

• 5.4 Predictive Biomarkers

• 5.5 Challenges in Method Validation

• 5.6 Clinically Validating Biomarkers

• 5.7 The Challenges of Cancer Epigenetics for Biomarker Development

• 5.8 Conclusion

• References

Chapter 6. Networks and Consortia for Epigenetic Drug Discovery

• Abstract

• 6.1 Introduction

• 6.2 Epigenetics Defined

• 6.3 Utility of Epigenetic Drug Inhibitors for Cancer Therapy

• 6.4 Human Epigenome Project (HEP)

• 6.5 Encyclopedia of DNA Elements (ENCODE)

• 6.6 NIH Roadmap Epigenomics Initiative (NREI)

• 6.7 International Human Epigenome Consortium (IHEC)

• 6.8 The Cancer Genome Atlas (TCGA)

• 6.9 Therapeutically Applicable Research to Generate Effective Treatments (TARGET)

• 6.10 International Cancer Genomics Consortium (ICGC)

• 6.11 Structural Genomics Consortium (SGC)

• 6.12 Stand Up to Cancer (SU2C) Epigenetics Dream Team

• 6.13 Summary and Conclusions

• Acknowledgments and Disclosure

• References

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Part III: Classes of Epigenetic Drugs
Chapter 7. DNA Methyltransferase Inhibitors

• Abstract

• 7.1 Discovery of aza-Analogs and Historical Highlight

• 7.2 The Pharmacology of DNMT Inhibitors

• 7.3 The Clinical Trials in Hematological Malignancies Leading to Approval of DNMT Inhibitors

• 7.4 Biomarkers of Clinical Outcome with DNMT Inhibitor Therapy

• 7.5 Lack of Efficacy of DNMT Inhibitors in Solid Tumors

• 7.6 Second Generation of DNMT Inhibitors

• 7.7 Conclusions and Perspectives

• References

Chapter 8. Small Molecule Inhibitors of Histone Deacetylases and Acetyltransferases as Potential Therapeutics in Oncology

• Abstract

• 8.1 Introduction

• 8.2 Classes of HATs

• 8.3 HATi in Cancer

• 8.4 Classes of HDACs

• 8.5 HDACi in Cancer

• 8.6 Mechanisms of Action of HDACi

• 8.7 Role of Acetylation and Deacetylation in NF-κB Mediated Signaling

• 8.8 HDAC–NF-κB Interactions in NF-κB Signaling

• 8.9 Alternative Area of Application: HDACi as Anti-Inflammatory Drugs for the Treatment of (NF-κB-Mediated) Inflammation

• 8.10 Concluding Remarks

• Acknowledgments

• References

Chapter 9. Targeting Histone Methylation: The Development of Selective Methyltransferase and Demethylase Inhibitors

• Abstract

• 9.1 Global and Locus-Specific Control of Histone Lysine Methylation

• 9.2 Assaying Histone Methylation

• 9.3 Ten Ways to Target Histone Methylation

• 9.4 The Hottest Therapeutic Targets in Histone Methylation

• References

Chapter 10. Bromodomains as Anticancer Targets

• Abstract

• 10.1 Introduction

• 10.2 Acetylation and Transcription

• 10.3 Architecture of BRDs

• 10.4 Linear Sequence Motifs Recognized by BRDs

• 10.5 Functional Roles of BRD-Containing Proteins

• 10.6 Deregulation of BRD Function(s) in Cancer

• 10.7 BRDs as Regulators of Tumor-Promoting Genes

• 10.8 BRD-Containing Proteins as Tumor Suppressors

• 10.9 Oncogenic Fusions Involving BRDs

• 10.10 Inhibition of BRDs by Small Molecules

• 10.11 Better Tools for Clinical Applications

• 10.12 Conclusion

• Acknowledgments

• References

Chapter 11. Epigenetic Readers Interpreting the Lysine Methylome—Biological Roles and Drug Discovery

• Abstract

• 11.1 Introduction

• 11.2 Methyl-Lysine Readers

• 11.3 The Royal Family of Epigenetic Reader Proteins

• 11.4 The PHD Finger Family of Epigenetic Reader Proteins

• 11.5 The WD40 Repeat Domain Family

• 11.6 Computational Methods

• 11.7 Conclusion

• Acknowledgment and Funding

• References

Chapter 12. Noncoding RNAs: Clinical and Therapeutic Applications

• Abstract

• 12.1 Introduction

• 12.2 Different Classes of Noncoding RNAs: Their Biogenesis and Mode of Actions

• 12.3 Altered ncRNA Expression and Biological Consequence in Human Pathologies

• 12.4 Utility of ncRNA Biomarkers for Human Diseases

• 12.5 ncRNA Targeting Strategies for Treatment of Human Diseases

• 12.6 Conclusion

• References

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Part IV: Clinical Implications of Epigenetic Therapy
Chapter 13. Clinical Applications of Epigenetic Drugs

• Abstract

• 13.1 Introduction

• 13.2 Epigenetic Drugs in Hematological Malignancies

• 13.3 Epigenetic Therapies in Solid Tumors

• 13.4 Why Are Epigenetic Therapies More Active in Hematological Malignancies Than in Solid Tumors?

• 13.5 Conclusions

• References

Chapter 14. Efficacy of Combined Epigenetic Therapies

• Abstract

• 14.1 Scientific Rationale to Combine Epigenetic Drugs

• 14.2 Combinations Between DNMT and HDACi

• 14.3 Epigenetic Combinations with HMTi

• 14.4 Epigenetic Combinations with HDMi

• 14.5 Epigenetic Reader Drug Combinations

• 14.6 Combinations Between Epigenetic Drugs and Standard Chemotherapy

• 14.7 Emerging Combinations Between Epigenetic Drugs and Targeted Chemotherapy Kinase Inhibitors

• 14.8 Using Epigenetic Drugs in Combination with Immunotherapy

• 14.9 Combination with Nontoxic Agents

• 14.10 Conclusion and Perspectives

• References

Chapter 15. Predicting and Monitoring Responses to Epigenetic Drugs

• Abstract

• 15.1 Introduction

• 15.2 Epigenetics and Cancer

• 15.3 Epigenetic Therapies

• 15.4 Biomarkers

• 15.5 Conclusion

• References

Chapter 16. Episensitization: A New Word for a New Concept

• Abstract

• 16.1 Introduction

• 16.2 The Cancer Ecosystem

• 16.3 Epigenetic Modulation and the Butterfly Effect

• 16.4 Resistance Is Energetically Expensive and Inefficient

• 16.5 Epi-Resensitization Trials

• 16.6 Discussion

• Acknowledgments

• References

Chapter 17. The Emerging Potential for Epigenetic Therapeutics in Noncancer Disorders

• Abstract

• 17.1 Introduction

• 17.2 Epigenetic Targets for Therapeutics

• 17.3 Neurological Diseases

• 17.4 Autoimmune and Inflammatory Disease

• 17.5 Metabolic and Cardiovascular Disease

• 17.6 Precise Manipulation of the Epigenome

• 17.7 Conclusion and Outlook

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Tags: Gerda Egger, Paola Arimondo, Drug Discovery, Cancer Epigenetics