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Drug discovery in cancer epigenetics

Arimondo, Paola,

Drug discovery in cancer epigenetics

紀錄類型:	書目-電子資源 : Monograph/item
正題名/作者:	Drug discovery in cancer epigeneticsedited by Gerda Egger and Paola Arimondo.
其他作者:	Egger, Gerda,
出版者:	Oxford ;Academic Press, an imprint of Elsevier,©2016.
面頁冊數:	1 online resource (xxi, 475 p.).
標題:	CancerGenetic aspects.
電子資源:	https://www.sciencedirect.com/science/book/9780128022085
ISBN:	9780128024928 (electronic bk.)

Drug discovery in cancer epigenetics
Drug discovery in cancer epigenetics[electronic resource] /edited by Gerda Egger and Paola Arimondo. - Oxford ;Academic Press, an imprint of Elsevier,©2016. - 1 online resource (xxi, 475 p.). - Translational epigenetics series. - Translational epigenetics series..

Includes bibliographical references and index.

Front Cover; Drug Discovery in Cancer Epigenetics; Copyright Page; Contents; List of Contributors; Preface; I. Introduction; 1 Basic Epigenetic Mechanisms and Phenomena; 1.1 Introduction; 1.2 Basic Epigenetic Mechanisms; 1.2.1 DNA Methylation; 1.2.2 DNA Demethylation; 1.2.3 Histone Modifications; 1.2.3.1 Histone Acetylation and Deacetylation; 1.2.3.2 Histone Phosphorylation; 1.2.3.3 Histone Methylation and Demethylation; 1.2.3.4 Chromatin-Remodeling Complexes and Histone Variants; 1.2.4 Noncoding RNAs; 1.3 Epigenetic (Re)Programming; 1.3.1 Epigenetic Asymmetry in the Zygote.

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.

ISBN: 9780128024928 (electronic bk.)Subjects--Topical Terms:

189391
Cancer
--Genetic aspects.Index Terms--Genre/Form:

214472
Electronic books.

LC Class. No.: RC268.4

Dewey Class. No.: 616.99/4042

National Library of Medicine Call No.: QZ 267

Drug discovery in cancer epigenetics
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505 0 $a Front Cover; Drug Discovery in Cancer Epigenetics; Copyright Page; Contents; List of Contributors; Preface; I. Introduction; 1 Basic Epigenetic Mechanisms and Phenomena; 1.1 Introduction; 1.2 Basic Epigenetic Mechanisms; 1.2.1 DNA Methylation; 1.2.2 DNA Demethylation; 1.2.3 Histone Modifications; 1.2.3.1 Histone Acetylation and Deacetylation; 1.2.3.2 Histone Phosphorylation; 1.2.3.3 Histone Methylation and Demethylation; 1.2.3.4 Chromatin-Remodeling Complexes and Histone Variants; 1.2.4 Noncoding RNAs; 1.3 Epigenetic (Re)Programming; 1.3.1 Epigenetic Asymmetry in the Zygote.
505 8 $a 1.3.2 Reprogramming in the Germline1.3.3 Induced Pluripotency; 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; 1.8.1 Selected Monogenetic Diseases; 1.8.2 Selected Neurodegenerative Diseases; 1.8.3 Selected Autoimmune Diseases; References; 2 Cancer Epigenetics; 2.1 Background; 2.2 DNA Methylation; 2.3 Histone Modifications; 2.4 Nucleosome Positions and Higher-Order Structures; 2.5 Noncoding RNAs; 2.5.1 microRNAs.
505 8 $a 2.5.2 Long Noncoding RNAs2.5.3 Other Noncoding RNAs; 2.6 Mutation of Epigenetic Enzymes; 2.6.1 Chromatin-Remodeling Enzymes; 2.6.2 Histone Modifiers; 2.6.3 DNA Methyltransferases; 2.6.4 ncRNA Machinery; 2.7 Conclusion; References; II. Methods and Tools for Epigenetic Drug Development; 3 Drug Discovery Methods; 3.1 Introduction; 3.2 Hit Discovery; 3.2.1 In Silico Screening and Molecular Docking; 3.2.2 Fragment-Based Drug Discovery; 3.2.3 Structure-Based Approaches; 3.2.4 Hybrid Inhibitor Design; 3.2.5 Drug Repurposing; 3.2.6 Exploring Natural Products; 3.2.7 High-Throughput Screening.
505 8 $a 3.3 Lead Optimization and Identification3.3.1 Lead Optimization in the Absence of Structural Information; 3.3.1.1 Lead optimization guided by SAR data; 3.3.1.2 Lead optimization based on docking or modeling studies; 3.3.2 Lead Optimization Using Structural Information; 3.3.2.1 Lead optimization using a structure-based design approach; 3.3.2.2 Lead optimization using a mechanism- or ligand-based approach; 3.3.3 Lead Generation Using Other Approaches; 3.3.3.1 Lead optimization using parallel or combinatorial chemistry tools.
505 8 $a 3.3.3.2 Lead optimization by transposition of key pharmacophores from known inhibitors3.3.3.3 Lead optimization by introduction of group isosteres or surrogates; 3.3.3.4 Lead identification starting from literature compounds ("lit-to-lead"); 3.3.3.5 Lead generation via target hopping approaches; 3.4 Pharmacological Profiling and Drug-Target Engagement; 3.4.1 Pharmacological Profiling of DNMT Inhibitors; 3.4.1.1 Special considerations; 3.4.2 Pharmacological Profiling of HMT Inhibitors; 3.4.2.1 Special considerations; 3.4.3 Drug-Target Engagement; 3.5 General Conclusions; Acknowledgments.
520 $a 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.
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