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Table of Contents
Intro
Preface
Contents
1 Lysine Demethylation in Pathogenesis
Abstract
1.1 Epigenetic Regulation and Human Health
1.2 Histone and Histone Methylation
1.3 Histone Demethylases
1.4 Functions of Histone Demethylases
1.5 KDMs and Human Diseases
1.6 Targeting KDMs in Human Diseases
1.7 Conclusion
References
2 Targeting the LSD1/KDM1 Family of Lysine Demethylases in Cancer and Other Human Diseases
Abstract
2.1 Introduction: Discovery of the First Histone Demethylase, LSD1/KDM1A
2.2 Structure, Mechanism, and Biological Function of the KDM1 Family
2.2.1 Domain Organization and Structural Features of the KDM1 Family
2.2.2 Enzymatic Mechanism of Action of the KDM1 Family
2.2.3 KDM1 Substrates and Protein Interactions
2.2.3.1 Histone Substrates
2.2.3.2 Non-histone Substrates
2.2.4 Functional Interactions of KDM1 Demethylases with Other Biomolecules in Different Cellular Complexes
2.3 Involvement of the KDM1 Family in Different Biological Processes
2.3.1 Role of KDM1A in Stem Cells
2.3.2 Role of KDM1A in Hematopoietic Cell Differentiation
2.3.3 Role of KDM1A in Maternal Trophoblast Stem Cell Differentiation
2.3.4 Role of KDM1A in Adipose Differentiation and Metabolism
2.3.5 Role of KDM1A in Skeletal Muscle Differentiation
2.3.6 Role of KDM1A in Neurogenesis
2.3.7 Emerging Biological Roles for KDM1B
2.4 KDM1A and Cancer Development
2.4.1 AR and Prostate Cancer
2.4.2 Estrogen Receptor (ER) and Breast Cancer
2.4.3 Acute Myeloid Leukemia (AML)
2.4.4 Small Cell Lung Cancer (SCLC) and Non-small Cell Lung Cancer (NSCLC)
2.4.5 Other Tumors
2.4.6 Emerging Role of KDM1 in Cancer Cell Evasion of Immune Surveillance
2.5 KDM1 Demethylase as a Target in Cancer Therapy
2.6 Classes of KDM1 Inhibitors
2.6.1 MAO Inhibitors and Derivatives
2.6.2 Peptide-Based KDM1A Inhibitors
2.6.3 Polyamine-Based KDM1A Inhibitors
2.6.4 Natural Products as KDM1A Inhibitors
2.6.5 Multifunctional Inhibitors
2.6.6 Other KDM1A Inhibitors
2.6.7 KDM1A Inhibitors in Clinical Trials
2.7 Conclusions and Future Perspectives
References
3 Biological Functions of the KDM2 Family of Histone Demethylases
Abstract
3.1 Introduction
3.2 Structure and Function of KDM2 Demethylases
3.3 KDM2 Demethylases in Polycomb-Mediated Gene Silencing
3.4 Non-histone Targets of KDM2 Demethylases
3.5 Role of KDM2 Demethylases in Replicative Senescence, Stem Cell Biology and Somatic Cell Reprogramming
3.6 KDM2 Demethylases in Normal Development and Tissue Homeostasis
3.7 KDM2 Demethylases in Cancer
3.8 Targeting KDM2 Demethylases with Small Molecule Inhibitors
References
4 Histone Demethylase KDM3 (JMJD1) in Transcriptional Regulation and Cancer Progression
Abstract
4.1 Introduction
4.2 Discovery of KDM3A as an H3K9me1/2 Demethylase
4.3 KDM3 in the Demethylation of Non-histone Proteins
Preface
Contents
1 Lysine Demethylation in Pathogenesis
Abstract
1.1 Epigenetic Regulation and Human Health
1.2 Histone and Histone Methylation
1.3 Histone Demethylases
1.4 Functions of Histone Demethylases
1.5 KDMs and Human Diseases
1.6 Targeting KDMs in Human Diseases
1.7 Conclusion
References
2 Targeting the LSD1/KDM1 Family of Lysine Demethylases in Cancer and Other Human Diseases
Abstract
2.1 Introduction: Discovery of the First Histone Demethylase, LSD1/KDM1A
2.2 Structure, Mechanism, and Biological Function of the KDM1 Family
2.2.1 Domain Organization and Structural Features of the KDM1 Family
2.2.2 Enzymatic Mechanism of Action of the KDM1 Family
2.2.3 KDM1 Substrates and Protein Interactions
2.2.3.1 Histone Substrates
2.2.3.2 Non-histone Substrates
2.2.4 Functional Interactions of KDM1 Demethylases with Other Biomolecules in Different Cellular Complexes
2.3 Involvement of the KDM1 Family in Different Biological Processes
2.3.1 Role of KDM1A in Stem Cells
2.3.2 Role of KDM1A in Hematopoietic Cell Differentiation
2.3.3 Role of KDM1A in Maternal Trophoblast Stem Cell Differentiation
2.3.4 Role of KDM1A in Adipose Differentiation and Metabolism
2.3.5 Role of KDM1A in Skeletal Muscle Differentiation
2.3.6 Role of KDM1A in Neurogenesis
2.3.7 Emerging Biological Roles for KDM1B
2.4 KDM1A and Cancer Development
2.4.1 AR and Prostate Cancer
2.4.2 Estrogen Receptor (ER) and Breast Cancer
2.4.3 Acute Myeloid Leukemia (AML)
2.4.4 Small Cell Lung Cancer (SCLC) and Non-small Cell Lung Cancer (NSCLC)
2.4.5 Other Tumors
2.4.6 Emerging Role of KDM1 in Cancer Cell Evasion of Immune Surveillance
2.5 KDM1 Demethylase as a Target in Cancer Therapy
2.6 Classes of KDM1 Inhibitors
2.6.1 MAO Inhibitors and Derivatives
2.6.2 Peptide-Based KDM1A Inhibitors
2.6.3 Polyamine-Based KDM1A Inhibitors
2.6.4 Natural Products as KDM1A Inhibitors
2.6.5 Multifunctional Inhibitors
2.6.6 Other KDM1A Inhibitors
2.6.7 KDM1A Inhibitors in Clinical Trials
2.7 Conclusions and Future Perspectives
References
3 Biological Functions of the KDM2 Family of Histone Demethylases
Abstract
3.1 Introduction
3.2 Structure and Function of KDM2 Demethylases
3.3 KDM2 Demethylases in Polycomb-Mediated Gene Silencing
3.4 Non-histone Targets of KDM2 Demethylases
3.5 Role of KDM2 Demethylases in Replicative Senescence, Stem Cell Biology and Somatic Cell Reprogramming
3.6 KDM2 Demethylases in Normal Development and Tissue Homeostasis
3.7 KDM2 Demethylases in Cancer
3.8 Targeting KDM2 Demethylases with Small Molecule Inhibitors
References
4 Histone Demethylase KDM3 (JMJD1) in Transcriptional Regulation and Cancer Progression
Abstract
4.1 Introduction
4.2 Discovery of KDM3A as an H3K9me1/2 Demethylase
4.3 KDM3 in the Demethylation of Non-histone Proteins