Drug Discovery in Cancer Epigenetics

Drug Discovery in Cancer Epigenetics

Author: Gerda Egger

Publisher: Academic Press

Published: 2015-11-19

Total Pages: 499

ISBN-13: 0128024925

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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. - 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


Epigenetics for Drug Discovery

Epigenetics for Drug Discovery

Author: Nessa Carey

Publisher: Royal Society of Chemistry

Published: 2015-11-20

Total Pages: 338

ISBN-13: 1849738823

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This book will provide an invaluable guide to epigenetics, one of the fastest moving fields in drug discovery, for medicinal chemists working in academia and in the pharmaceutical industry.


Epigenetic Cancer Therapy

Epigenetic Cancer Therapy

Author: Steven Gray

Publisher: Academic Press

Published: 2015-07-01

Total Pages: 748

ISBN-13: 0128002247

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Epigenetic Cancer Therapy unites issues central to a translational audience actively seeking to understand the topic. It is ideal for cancer specialists, including oncologists and clinicians, but also provides valuable information for researchers, academics, students, governments, and decision-makers in the healthcare sector. The text covers the basic background of the epigenome, aberrant epigenetics, and its potential as a target for cancer therapy, and includes individual chapters on the state of epigenome knowledge in specific cancers (including lung, breast, prostate, liver). The book encompasses both large-scale intergovernmental initiatives as well as recent findings across cancer stem cells, rational drug design, clinical trials, and chemopreventative strategies. As a whole, the work articulates and raises the profile of epigenetics as a therapeutic option in the future management of cancer. - Concisely summarizes the therapeutic implications of recent, large-scale epigenome studies, including the cancer epigenome atlas - Discusses targeted isoform specific versus pan-specific inhibitors, a rational drug design approach to epigenetics relevant to pharmacoepigenetic clinical applications - Covers new findings in the interplay between cancer stem cells (CSCs) and drug resistance, demonstrating that epigenetic machinery is a candidate target for the eradication of these CSCs


Structural Biology in Drug Discovery

Structural Biology in Drug Discovery

Author: Jean-Paul Renaud

Publisher: John Wiley & Sons

Published: 2020-01-09

Total Pages: 1437

ISBN-13: 1118900502

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With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins


Chemical Epigenetics

Chemical Epigenetics

Author: Antonello Mai

Publisher: Springer Nature

Published: 2020-03-31

Total Pages: 569

ISBN-13: 3030429822

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This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.


Epigenetic Therapy of Cancer

Epigenetic Therapy of Cancer

Author: Michael Lübbert

Publisher: Springer Science & Business Media

Published: 2013-12-12

Total Pages: 332

ISBN-13: 3642384048

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The growing knowledge about disturbances of epigenetic gene regulation in hematopoietic stem cell disorders is now being translated into treatment approaches that target the epigenetic defects pharmacologically. This book first presents the latest evidence regarding the epigenetic regulation of hematopoietic stem cell differentiation and hemoglobin production. The significance of DNA methylation abnormalities in hematopoietic disorders and of epigenetic disturbances in lung cancer and other solid tumors is then discussed. A major part of the book, however, relates specifically to the translation of basic research and drug development to clinical applications, and in this context both present and future clinical strategies are considered. Individual chapters are devoted to the use of DNA hypomethylating agents and chromatin-modifying agents, and the treatment of hematologic malignancies and solid tumors by means of epigenetic agents is discussed in detail.


Epigenetic Biomarkers and Diagnostics

Epigenetic Biomarkers and Diagnostics

Author: Jose Luis Garcia-Gimenez

Publisher: Academic Press

Published: 2015-12-07

Total Pages: 698

ISBN-13: 0128019212

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Epigenetic Biomarkers and Diagnostics comprises 31 chapters contributed by leading active researchers in basic and clinical epigenetics. The book begins with the basis of epigenetic mechanisms and descriptions of epigenetic biomarkers that can be used in clinical diagnostics and prognostics. It goes on to discuss classical methods and next generation sequencing-based technologies to discover and analyze epigenetic biomarkers. The book concludes with an account of DNA methylation, post-translational modifications and noncoding RNAs as the most promising biomarkers for cancer (i.e. breast, lung, colon, etc.), metabolic disorders (i.e. diabetes and obesity), autoimmune diseases, infertility, allergy, infectious diseases, and neurological disorders. The book describes the challenging aspects of research in epigenetics, and current findings regarding new epigenetic elements and modifiers, providing guidance for researchers interested in the most advanced technologies and tested biomarkers to be used in the clinical diagnosis or prognosis of disease. - Focuses on recent progress in several areas of epigenetics, general concepts regarding epigenetics, and the future prospects of this discipline in clinical diagnostics and prognostics - Describes the importance of the quality of samples and clinical associated data, and also the ethical issues for epigenetic diagnostics - Discusses the advances in epigenomics technologies, including next-generation sequencing based tools and applications - Expounds on the utility of epigenetic biomarkers for diagnosis and prognosis of several diseases, highlighting the study of these biomarkers in cancer, cardiovascular and metabolic diseases, infertility, and infectious diseases - Includes a special section that discusses the relevance of biobanks in the maintenance of high quality biosamples and clinical-associated data, and the relevance of the ethical aspects in epigenetic studies


DNA and Histone Methylation as Cancer Targets

DNA and Histone Methylation as Cancer Targets

Author: Atsushi Kaneda

Publisher: Springer

Published: 2017-09-04

Total Pages: 616

ISBN-13: 3319597868

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This book will focus on DNA and histone methylation in epigenetics and describe how it is involved in the molecular mechanisms responsible for the development of cancer. Chapters will summarize the current knowledge of the molecular basis of DNA and histone methylation and explain how it is involved in cancer, describe the features of DNA and histone methylation associated with particular types of cancer, diagnostic/therapeutic applications, and future directions of DNA and histone methylation as cancer targets.


MicroRNAs in Cancer

MicroRNAs in Cancer

Author: Cesar Lopez-Camarillo

Publisher: CRC Press

Published: 2013-02-22

Total Pages: 426

ISBN-13: 1466576774

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MicroRNA (miRNA) biology is a cutting-edge topic in basic as well as biomedical research. This is a specialized book focusing on the current understanding of the role of miRNAs in the development, progression, invasion, and metastasis of diverse types of cancer. It also reviews their potential for applications in cancer diagnosis, prognosis, and th


Introduction to Epigenetics

Introduction to Epigenetics

Author: Renato Paro

Publisher: Springer Nature

Published: 2021-03-23

Total Pages: 215

ISBN-13: 3030686701

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This open access textbook leads the reader from basic concepts of chromatin structure and function and RNA mechanisms to the understanding of epigenetics, imprinting, regeneration and reprogramming. The textbook treats epigenetic phenomena in animals, as well as plants. Written by four internationally known experts and senior lecturers in this field, it provides a valuable tool for Master- and PhD- students who need to comprehend the principles of epigenetics, or wish to gain a deeper knowledge in this field. After reading this book, the student will: Have an understanding of the basic toolbox of epigenetic regulation Know how genetic and epigenetic information layers are interconnected Be able to explain complex epigenetic phenomena by understanding the structures and principles of the underlying molecular mechanisms Understand how misregulated epigenetic mechanisms can lead to disease