Targeting lysine demethylases in cancer and other human diseases / Qin Yan, editor.
Yan, Qin.
2023
QP562.L8
Available Online

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Title Targeting lysine demethylases in cancer and other human diseases / Qin Yan, editor.
ISBN 9783031381768 (electronic bk.)
3031381769 (electronic bk.)
3031381750
9783031381751
DOI https://doi.org/10.1007/978-3-031-38176-8
Publication Details Cham : Springer, 2023.
Language English
Description 1 online resource (187 p.).
Item Number 10.1007/978-3-031-38176-8 doi
Call Number QP562.L8
Dewey Decimal Classification 615.35
Summary This book provides a comprehensive summary of our current knowledge on lysine demethylases, a class of epigenetic regulators. It takes the reader on an exciting journey spanning the past two decades, starting from the initial discovery and characterization of these enzymes and leading up to the development of their small molecule modulators. These modulators have shown promise in clinical trials and hold great potential to improve patient outcomes. The book captures the progress made in this field and highlights the significant advancements that have paved the way for potential therapeutic applications. The book covers a wide range of topics, spanning both basic biology and clinical implications associated with lysine demethylases. It offers a comprehensive historical and conceptual framework for the discovery and characterization of similar epigenetic enzymes or modulators. Chapter one serves as an introductory overview, providing insights into the general characteristics and functions of lysine demethylases. In subsequent chapters, specifically chapters two to eight, each major family of lysine demethylases is individually explored in depth. By providing in-depth insights into the functional aspects of these enzymes, the book allows readers to grasp their significance in regulating cellular processes and influencing pathogenesis. Moreover, the book goes beyond fundamental knowledge and also explores the development of diagnostic and therapeutic strategies related to lysine demethylases. It highlights the potential for utilizing these enzymes as therapeutic targets for the treatment of various diseases, including cancer and infectious diseases. Additionally, the book highlights future directions aimed at further unraveling the roles of lysine demethylases and translating these findings into the clinic.
Note 4.4 Physiological Functions of KDM3A
Access Note Access limited to authorized users.
Source of Description Online resource; title from PDF title page (SpringerLink, viewed October 12, 2023).
Added Author Yan, Qin.
Series Advances in experimental medicine and biology ; v. 1433.
Available in Other Form Targeting Lysine Demethylases in Cancer and Other Human Diseases
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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

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