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Drug discovery in cancer epigenetics /
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 predictio...
| Clasificación: | Libro Electrónico |
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| Otros Autores: | , |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Oxford ; Waltham, MA :
Academic Press, an imprint of Elsevier,
[2016]
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| Colección: | Translational epigenetics series.
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| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- 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.
- 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.
- 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.
- 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.
- 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.