UID:
almafu_9960074024902883
Umfang:
1 online resource (499 p.)
ISBN:
9780128024928
,
0128024925
Serie:
Translational Epigenetics Series
Anmerkung:
Description based upon print version of record.
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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
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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
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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
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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
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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
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References
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English
Weitere Ausg.:
ISBN 9780128022085
Weitere Ausg.:
ISBN 0128022086
Sprache:
Englisch
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